Query Query HO
Results
Date
5 substances in Reaxys
2018-08-03 18h:10m:14s (UTC)
N O
1. Query NH 2
Search as: As drawn ) AND (IDE.XRN=606417) OR (IDE.XRN=3998136) OR (IDE.XRN=4547459) OR (IDE.XRN=9899888) OR (IDE.XRN=9899889))
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
1/181
2018-08-03 18:12:50
Reaxys ID 606417 View in Reaxys
HO
1/5 CAS Registry Number: 2763-96-4 Chemical Name: muscimol; Muscimol; 5-aminomethyl-3-hydroxyisoxazole; 5-(aminomethyl)isoxazol-3-ol; [3H]muscimol; 3-Hydroxy-5-aminomethyl-isoxazole; 5-Aminomethyl-3-hydroxy-isoxazol Linear Structure Formula: C4H6N2O2 Molecular Formula: C4H6N2O2 Molecular Weight: 114.104 Type of Substance: heterocyclic InChI Key: ZJQHPWUVQPJPQT-UHFFFAOYSA-N Note:
N O
NH 2
Substance Label (20) Label References 1
Gagneux,A.R. et al.; Tetrahedron Letters; (1965); p. 2077 - 2079, View in Reaxys; Brehm; Hjeds; Krogsgaard-Larsen; Acta chemica Scandinavica; vol. 26; nb. 3; (1972); p. 1298 - 1299, View in Reaxys; Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys; Oster, Timothy A.; Harris, Thomas M.; Journal of Organic Chemistry; vol. 48; nb. 23; (1983); p. 4307 - 4311, View in Reaxys; Pevarello; Varasi; Synthetic Communications; vol. 22; nb. 13; (1992); p. 1939 - 1948, View in Reaxys; Nakamura, Norio; Tajima, Yawara; Sakai, Kiyoshi; Heterocycles; vol. 17; (1982); p. 235 - 245, View in Reaxys; Nordmann; Graff; Maurer; Gahwiler; Journal of Medicinal Chemistry; vol. 28; nb. 8; (1985); p. 1109 - 1111, View in Reaxys; Abdul Manan, Mohd Abdul Fatah; Cordes, David B.; Slawin, Alexandra M. Z.; Bühl, Michael; Liao, Vivian W. Y.; Chua, Han. C.; Chebib, Mary; O'Hagan, David; Chemistry - A European Journal; vol. 23; nb. 45; (2017); p. 10848 - 10852, View in Reaxys
MUS
Nielsen; Witt; Ebert; Krogsgaard-Larsen; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 289; nb. 1; (1995); p. 109 - 112, View in Reaxys; Deja; Jawie; Jasicka-Misiak; Halama; Wieczorek; Kafarski; Mlynarz; Magnetic Resonance in Chemistry; vol. 52; nb. 11; (2014); p. 711 - 714, View in Reaxys; Nikolaus, Susanne; Beu, Markus; de Souza Silva, Maria Angelica; Huston, Joseph P.; Antke, Christina; Müller, Hans-Wilhelm; Hautzel, Hubertus; Pharmacology Biochemistry and Behavior; vol. 153; (2017); p. 76 - 87, View in Reaxys; Umino, Asami; Ishiwata, Sayuri; Iwama, Hisayuki; Nishikawa, Toru; Frontiers in Molecular Neuroscience; vol. 10; (2017); Art.No: 240, View in Reaxys
Musc
Heubl, Martin; Zhang, Jinwei; Pressey, Jessica C.; Al Awabdh, Sana; Renner, Marianne; Gomez-Castro, Ferran; Moutkine, Imane; Eugène, Emmanuel; Russeau, Marion; Kahle, Kristopher T.; Poncer, Jean Christophe; Lévi, Sabine; Nature Communications; vol. 8; nb. 1; (2017); Art.No: 1776, View in Reaxys
muscimol
Patent; THE JOHNS HOPKINS UNIVERSITY; BOSMANS, Frank; WO2014/120994; (2014); (A1) English, View in Reaxys
MUSC
Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki; European Journal of Pharmacology; vol. 341; nb. 1; (1998); p. 45 - 56, View in Reaxys
M
Suh; Song; Kim; Choi; Yoo; Tseng; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 352; nb. 6; (1995); p. 614 - 619, View in Reaxys
4
Melikian; Schlewer; Chambon; Wermuth; Journal of Medicinal Chemistry; vol. 35; nb. 22; (1992); p. 4092 - 4097, View in Reaxys
Tab. I
Arnoldi; Merlini; Quadri; Bonsignori; Melloni; Varasi; Farmaco; vol. 46; nb. 5; (1991); p. 629 - 638, View in Reaxys
7
Chiarino, D.; Napoletano, M.; Sala, A.; Tetrahedron Letters; vol. 27; nb. 27; (1986); p. 3181 - 3182, View in Reaxys
6a
Frey; Jager; Synthesis; vol. NO. 12; (1985); p. 1100 - 1164, View in Reaxys
1a
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys
3
Welch, W. M.; Synthetic Communications; vol. 12; nb. 14; (1982); p. 1089 - 1091, View in Reaxys
10
McCarry; Savard; Tetrahedron Letters; vol. 22; nb. 51; (1981); p. 5153 - 5156, View in Reaxys
8
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys
II
Nakamura,N.; Chemical and Pharmaceutical Bulletin; vol. 19; (1971); p. 46 - 51, View in Reaxys; Eugster et al.; Tetrahedron Letters; (1965); p. 1813, View in Reaxys
I
Loev; Wilson; Goodman; Journal of medicinal chemistry; vol. 13; nb. 4; (1970); p. 738 - 741, View in Reaxys; Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys; Patent; Gagneux et al.; CH443300; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys; Patent; Gagneux et al.; CH443301; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys
21
Eugster; Naturwissenschaften; vol. 55; (1968); p. 305,310, View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
2/181
2018-08-03 18:12:50
IV
Patent; Geigy; CH443302; (1964); Chem.Abstr.; vol. 69; nb. 67367t; (1968), View in Reaxys; Patent; Gagneux et al.; CH443301; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys
V
Patent; Geigy; CH443298; (1964); Chem.Abstr.; vol. 69; nb. 67364q; (1968), View in Reaxys
III
Patent; Geigy, I.R., AG; CH443303; (1964); Chem.Abstr.; vol. 69; nb. 43904q; (1968), View in Reaxys
Patent-Specific Data (1) References Patent; PFIZER INC.; CABRAL, SHAWN; FUTATSUGI, KENTARO; HEPWORTH, DAVID; HUARD, KIM; KUNG, DANIEL WEI-SHUNG; ORR, SUVI TUULA MARJUKKA; SONG, KUN; US2015/259323; (2015); (A1) English, View in Reaxys Druglikeness (1) 1 of 1
LogP
-0.473
H Bond Donors
2
H Bond Acceptors
1
Rotatable Bonds
1
TPSA
72.28
Lipinski Number
4
Veber Number
2
Related Structure (2) Related Structure Referenced Compound
References Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys; Eugster; Takemoto; Helvetica chimica acta; vol. 50; nb. 1; (1967); p. 126 - 127, View in Reaxys
The author investi- 4-aminomethyl-iso- Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys gated the constitu- xazol-3-one tion. The author has doubts about the constitution/configuration of the title compound. The following alternatives are discussed/ proposed: /BRN= 606422/ Derivative (2) Comment (Derivative)
Derivative
References
muscimol hydrobromide
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys
HCl: F 160grad (Zers.)
Patent; Geigy, I.R., AG; CH443303; (1964); Chem.Abstr.; vol. 69; nb. 43904q; (1968), View in Reaxys
Melting Point (9) 1 of 9
Melting Point [°C]
172 - 174
Comment (Melting Point)
Decomposition
Chiarino, D.; Napoletano, M.; Sala, A.; Tetrahedron Letters; vol. 27; nb. 27; (1986); p. 3181 - 3182, View in Reaxys 2 of 9
Melting Point [°C]
174 - 176
Solvent (Melting Point)
ethanol
Comment (Melting Point)
Decomposition
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys 3 of 9
Melting Point [°C]
176 - 178
Comment (Melting Point)
Crystallization with 0.25 Mol(s) H2O
Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys 4 of 9
Melting Point [°C]
172 - 175
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
3/181
2018-08-03 18:12:50
Solvent (Melting Point)
methanol
Comment (Melting Point)
Decomposition
Nakamura, Norio; Tajima, Yawara; Sakai, Kiyoshi; Heterocycles; vol. 17; (1982); p. 235 - 245, View in Reaxys 5 of 9
Melting Point [°C]
174 - 176
Solvent (Melting Point)
H2O; ethanol
Comment (Melting Point)
Crystallization with 0.25 Mol(s) H2O
Welch, W. M.; Synthetic Communications; vol. 12; nb. 14; (1982); p. 1089 - 1091, View in Reaxys 6 of 9
Melting Point [°C]
172 - 174
Nakamura,N.; Chemical and Pharmaceutical Bulletin; vol. 19; (1971); p. 46 - 51, View in Reaxys; Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys 7 of 9
Melting Point [°C]
174 - 175
Eugster; Naturwissenschaften; vol. 55; (1968); p. 305,310, View in Reaxys; Eugster et al.; Tetrahedron Letters; (1965); p. 1813, View in Reaxys 8 of 9
Melting Point [°C]
155 - 156
Eugster; Naturwissenschaften; vol. 55; (1968); p. 305,310, View in Reaxys 9 of 9
Melting Point [°C]
175
Gagneux,A.R. et al.; Tetrahedron Letters; (1965); p. 2077 - 2079, View in Reaxys; Patent; Geigy; CH443302; (1964); Chem.Abstr.; vol. 69; nb. 67367t; (1968), View in Reaxys; Patent; Gagneux et al.; CH443300; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys; Patent; Gagneux et al.; CH443301; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys; Patent; Gagneux; Haflinger; US3397209; (1966); Chem.Abstr.; vol. 69; nb. 106696w; (1968), View in Reaxys Boiling Point (1) Boiling Point [°C]
Pressure (Boiling Point) [Torr]
References
70
0.01
Patent; Gagneux et al.; CH443301; (1964); Chem.Abstr.; vol. 69; nb. 106697x; (1968), View in Reaxys
Crystal Phase (1) Description (Crystal Phase)
References
Crystal structure determination
Brehm; Hjeds; Krogsgaard-Larsen; Acta chemica Scandinavica; vol. 26; nb. 3; (1972); p. 1298 - 1299, View in Reaxys
Decomposition (1) 1 of 1
Patent; Geigy; CH443298; (1964); Chem.Abstr.; vol. 69; nb. 67364q; (1968), View in Reaxys
Dissociation Exponent (2) 1 of 2
Dissociation Exponent (pK)
4.8
Temperature (Dissociation Exponent) [°C]
25
Type (Dissociation Exponent)
a1/apparent
Honore; Hjeds; European Journal of Medicinal Chemistry; vol. 14; nb. 3; (1979); p. 285 - 287, View in Reaxys 2 of 2
Dissociation Exponent (pK)
8.4
Temperature (Dissociation Exponent) [°C]
25
Type (Dissociation Exponent)
a2/apparent
Honore; Hjeds; European Journal of Medicinal Chemistry; vol. 14; nb. 3; (1979); p. 285 - 287, View in Reaxys NMR Spectroscopy (7) 1 of 7
Description (NMR Spectroscopy)
NOESY (Nuclear Overhauser Enhanced Spectroscopy); Chemical shifts; Spectrum
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
4/181
2018-08-03 18:12:50
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
water; water-d2
Frequency (NMR Spectro- 600.6 scopy) [MHz] Deja; Jawie; Jasicka-Misiak; Halama; Wieczorek; Kafarski; Mlynarz; Magnetic Resonance in Chemistry; vol. 52; nb. 11; (2014); p. 711 - 714, View in Reaxys 2 of 7
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
various solvent(s)
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys 3 of 7
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
various solvent(s)
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys 4 of 7
Description (NMR Spectroscopy)
Spin-spin coupling constants
Comment (NMR Spectroscopy)
1H-1H. Solvent(s): further solvent(s)
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys 5 of 7
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
D2O
Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys; Oster, Timothy A.; Harris, Thomas M.; Journal of Organic Chemistry; vol. 48; nb. 23; (1983); p. 4307 - 4311, View in Reaxys 6 of 7
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
D2O
Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys; Oster, Timothy A.; Harris, Thomas M.; Journal of Organic Chemistry; vol. 48; nb. 23; (1983); p. 4307 - 4311, View in Reaxys 7 of 7
Description (NMR Spectroscopy)
NMR
Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys IR Spectroscopy (3) 1 of 3
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
KBr
Comment (IR Spectroscopy)
3116 - 1632 cm**(-1)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
5/181
2018-08-03 18:12:50
Konda; Takahashi; Onda; Chemical and Pharmaceutical Bulletin; vol. 33; nb. 3; (1985); p. 1083 - 1087, View in Reaxys 2 of 3
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
KBr
Comment (IR Spectroscopy)
3200 - 1470 cm**(-1)
Oster, Timothy A.; Harris, Thomas M.; Journal of Organic Chemistry; vol. 48; nb. 23; (1983); p. 4307 - 4311, View in Reaxys 3 of 3
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
nujol
Comment (IR Spectroscopy)
3445 - 1475 cm**(-1)
Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys Mass Spectrometry (1) Description (Mass References Spectrometry) spectrum
Oster, Timothy A.; Harris, Thomas M.; Journal of Organic Chemistry; vol. 48; nb. 23; (1983); p. 4307 - 4311, View in Reaxys
UV/VIS Spectroscopy (1) 1 of 1
Description (UV/VIS Spectroscopy)
Absorption maxima
Eugster; Naturwissenschaften; vol. 55; (1968); p. 305,310, View in Reaxys Use (187) Use Pattern
References
GABAA-ergic neu- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; rotransmission en- (2007); (A1) English, View in Reaxys hancer Inflammatory diseases
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Inflammation
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Immune response
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Resistance to bacte- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; rial infection (2007); (A1) English, View in Reaxys Resistance to viral infection
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Immunosuppressed patients
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
wound healing delayed wound healing
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Recovery from surgery acceleration
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Burn patients recovery acceleration
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Acute inflammatory condition
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Chronic inflammatory condition
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
meningitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
6/181
2018-08-03 18:12:50
encephalitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
uveitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
colitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
tuberculosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
dermatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
adult respiratory distress syndrome
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
trauma
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Burns
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cuts
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
contusions
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
crush injuries
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
autoimmune diseases
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
organ rejection episodes
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
atherosclerosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
arteriosclerosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
autoimmune conditions
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
multiple sclerosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
systemic lupus erythematosus
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
polymyalgia rheumatica (PMR)
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
gouty arthritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
degenerative arthritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
tendonitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
bursitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
psoriasis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
fibrosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
arthrosteitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
7/181
2018-08-03 18:12:50
rheumatoid arthritis Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys other forms of inPatent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; flammatory arthritis (2007); (A1) English, View in Reaxys Sjogren's Syndrome Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys progressive system- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; ic sclerosis (2007); (A1) English, View in Reaxys scleroderma
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
ankylosing spondylitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
polymyositis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
dermatomyositis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pemphigus
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pemphigoid
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Type I diabetes mellitus
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
myasthenia gravis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Hashimoto's thyroditis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Graves' disease
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Goodpasture's disease
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
mixed connective tissue disease
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
sclerosing cholangitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
inflammatory bowel disease
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Crohn's Disease
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
regional enteritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
ulcerative colitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pernicious anemia
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
inflammatory dermatoses
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
usual interstitial pneumonitis (UIP)
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
asbestosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
silicosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
8/181
2018-08-03 18:12:50
bronchiectasis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
berylliosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
talcosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
all forms of pneumoconiosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
sarcoidosis in the lung
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Sarcoidosis in any organ
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
desquamative inter- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; stitial pneumonia (2007); (A1) English, View in Reaxys lymphoid interstitial pneumonia
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
giant cell interstitial Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; pneumonia (2007); (A1) English, View in Reaxys cellular interstitial pneumonia
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
extrinsic allergic al- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; veolitis (2007); (A1) English, View in Reaxys Wegener's granulomatosis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
related forms of an- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; giitis (2007); (A1) English, View in Reaxys temporal arteritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
polyarteritis nodosa Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys inflammatory dermatoses not presumed to be autoimmune
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
chronic active hepatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
delayed-type hyper- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; sensitivity reactions (2007); (A1) English, View in Reaxys poison ivy dermatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pneumonia
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
other respiratory tract inflammation due to any cause
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Adult Respiratory Distress Syndrome (ARDS)
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
encephalitis with inflammatory edema
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
immediate hyperPatent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; sensitivity reactions (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
9/181
2018-08-03 18:12:50
asthma
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
hayfever
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cutaneous allergies
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
acute anaphylaxis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
diseases involving acute deposition of immune complexes
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
rheumatic fever
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
acute glomerulonephritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
chronic glomerulo- Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; nephritis due to any (2007); (A1) English, View in Reaxys etiology post-infectious glomerulonephritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
post-Streptococcal glomerulonephritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
acute exacerbations of Systemic Lupus Erythematosus
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pyelonephritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cellulitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cystitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
acute cholecytitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
chronic cholecystitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
conditions producing transient ischemia anywhere along the gastrointestinal tract
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Conditions producing transient ischemia anywhere along the bladder
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Conditions producing transient ischemia anywhere along the heart
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Conditions producing transient ischemia anywhere along the other organ
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
sequelae of organ transplantation
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
10/181
2018-08-03 18:12:50
Tissue allograft
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
allograft rejection
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
appendicitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
arteritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
blepharitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
bronchiolitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
bronchitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cervicitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
cholangitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
chorioamnionitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
conjunctivitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
dacryoadenitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
endocarditis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
endometritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
enteritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
enterocolitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
epicondylitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
epididymitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
fasciitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
fibrositis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
gastritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
gastroenteritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
gingivitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
ileitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
iritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
laryngitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
11/181
2018-08-03 18:12:50
myelitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
myocarditis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
nephritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
omphalitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
oophoritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
orchitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
osteitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
otitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pancreatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
parotitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pericarditis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pharyngitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pleuritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
phlebitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
pneumonitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
proctitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
prostatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
rhinitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
salpingitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
sinusitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
stomatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
synovitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
tonsillitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
vaginitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
vasculitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
vulvitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
12/181
2018-08-03 18:12:50
vulvovaginitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
angitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
chronic bronchitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
osteomylitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
optic neuritis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
transverse myelitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
necrotizing fascilitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
hepatitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
necrotizing enterocolitis
Patent; Ebert, Bjarke; Bonnert, Timothy P.; Hutson, Peter Haynes; Rutter, Richard Anthony; US2007/203216; (2007); (A1) English, View in Reaxys
GABAA agonist
Patent; TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK; WO2007/143038; (2007); (A1) English, View in Reaxys
neural activity blocker
Patent; Fenton, Andre A.; US2007/274920; (2007); (A1) English, View in Reaxys
Anti-psychotic
Patent; Fenton, Andre A.; US2007/274920; (2007); (A1) English, View in Reaxys
Psychotic disorders
Patent; Fenton, Andre A.; US2007/274920; (2007); (A1) English, View in Reaxys
Psychosis
Patent; Fenton, Andre A.; US2007/274920; (2007); (A1) English, View in Reaxys
Psychotic symptoms
Patent; Fenton, Andre A.; US2007/274920; (2007); (A1) English, View in Reaxys
psychiatric disorPatent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; WO2006/12563; (2006); (A2) English, ders associated with View in Reaxys the menstrual cycle PMS/PMDD
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; WO2006/12563; (2006); (A2) English, View in Reaxys
catamenial epilepsy Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; WO2006/12563; (2006); (A2) English, View in Reaxys GABA analog
Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, View in Reaxys
plant breeding tech- Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, niques View in Reaxys assays for the screening of candidate modulators of GABA metabolism or GABA analogs
Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, View in Reaxys
method of modulat- Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, ing the fertility of a View in Reaxys plant creating a male sterile plant
Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, View in Reaxys
prevention of selffertilization
Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, View in Reaxys
nuclear or cytoplas- Patent; Palaivelu, Ravishankar; Brass, Laura; Preuss, Daphne; US2004/177398; (2004); (A1) English, mic genetic male View in Reaxys sterility factors Isolation from Natural Product (1)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
13/181
2018-08-03 18:12:50
Isolation from Natural Product
References
Aus Amanita muscaria
Bowden,K.; Drysdale,A.C.; Tetrahedron Letters; (1965); p. 727 - 728, View in Reaxys
Quantum Chemical Calculations (1) Calculated Proper- Method (Quantum ties Chemical Calculations) Transition energies
Ab initio calcns. (LCAO, GO SCF, DIM, SAMO, X-à, Hartree-Fock)
Location
References
supporting informa- Abdul Manan, Mohd Abdul Fatah; Cordes, David B.; Slawin, Alexantion dra M. Z.; Bühl, Michael; Liao, Vivian W. Y.; Chua, Han. C.; Chebib, Mary; O'Hagan, David; Chemistry - A European Journal; vol. 23; nb. 45; (2017); p. 10848 - 10852, View in Reaxys
Medchem (403) 1 of 403
2 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
forebrain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
1.5
Measurement pX
5.82
Concomitants: Compound RN
8141905; 702691
Concomitants: Compound name
[35S]-TBPS; [3H]-Flunitrazepam
Concomitants: Compound role
RAD; RAD
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
NMRI mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
0.300000 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
inhibition rate
Unit
%
Measurement Object
Convulsions
Quantitative value
40
Concomitants: Compound RN
1724431
Concomitants: Compound name
NMDA
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
14/181
2018-08-03 18:12:50
Concomitants: Compound role
IAV
Patent; Schwab; Wilfried; Anagnostopulos; Hiristo; Porsche-Wiebking; Elena; Grome; John; (31 pag.); US5273989; (1993), View in Reaxys 3 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
NMRI mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
0.300000 mg/kg
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
inhibition rate
Unit
%
Measurement Object
Mortality
Quantitative value
60
Concomitants: Compound RN
1724431
Concomitants: Compound name
NMDA
Concomitants: Compound role
IAV
Patent; Schwab; Wilfried; Anagnostopulos; Hiristo; Porsche-Wiebking; Elena; Grome; John; (31 pag.); US5273989; (1993), View in Reaxys 4 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
NMRI mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intravenous administration
Substance Dosing Regimen
Single
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
3 - 10
Patent; Schwab; Wilfried; Anagnostopulos; Hiristo; Porsche-Wiebking; Elena; Grome; John; (31 pag.); US5273989; (1993), View in Reaxys 5 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Brain : histology
Biological Species/NCBI ID
Meriones unguiculatus
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
5 mg/kg
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
15/181
2018-08-03 18:12:50
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
inhibition rate
Unit
%
Measurement Object
% reduction cell necrosis
Quantitative value
74
Patent; Schwab; Wilfried; Anagnostopulos; Hiristo; Porsche-Wiebking; Elena; Grome; John; (31 pag.); US5273989; (1993), View in Reaxys 6 of 403
7 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
heart
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
25
Measurement pX
7.6
Concomitants: Compound RN
4264456; 4264456
Concomitants: Compound name
PK 11195; [3H]-PK 11195
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
16/181
2018-08-03 18:12:50
8 of 403
9 of 403
Organs/Tissues
heart
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
0.9
Concomitants: Compound RN
4264456; 4264456
Concomitants: Compound name
PK 11195; [3H]-PK 11195
Concomitants: Compound role
NSB; RAD
Target Name
OATP [rat]
Target Synonyms
oatp
Target, Subunit, Species
OATP [rat]
Target Mutant/Chimera Details
OATP [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
Metabolism/Transport
Bioassay Name
Flux uptake
Biological Species/NCBI ID
rat
Organs/Tissues
liver
Cells/Cell Lines
liver cell
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
47
Deviation
26
Measurement pX
4.65
Concomitants: Compound RN
64569
Concomitants: Compound name
[3H]-Estradiol-17beta-glucuronide
Concomitants: Compound role
SUB
Target Name
Solute carrier family 22 member 1 [rat]
Target Synonyms
oct1; organic cation transporter 1; roct1; slc22a1; solute carrier family 22 member 1
Target Uniprot ID
q63089
Target, Subunit, Species
Solute carrier family 22 member 1 [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
17/181
2018-08-03 18:12:50
10 of 403
Target Mutant/Chimera Details
Solute carrier family 22 member 1 [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
Metabolism/Transport
Bioassay Name
Flux uptake
Biological Species/NCBI ID
rat
Organs/Tissues
liver
Cells/Cell Lines
liver cell
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
35
Deviation
15
Measurement pX
4.43
Concomitants: Compound RN
1618932
Concomitants: Compound name
[3H]-1-Methyl-4-phenylpyridinium
Concomitants: Compound role
SUB
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : locomotor activityTarget : miceBioassay : mice bred for high and low magnitudes of locomotor activation in response to 2 g/kg EtOH (36 generations, FAST and SLOW mice); injection of title compd.; immediate testing (fluorescent lights)
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
dose-dependent locomotor activity (traveled distance in 15 min) evaluated (diagram); inbred strain sensitivity differences in locomotor response tabulated
Measurement Parameter
qualitative
Shen, Elaine H.; Dorow, Janet; Harland, Richard; Burkhart-Kasch, Sue; Phillips, Tamara J.; Journal of Pharmacology and Experimental Therapeutics; vol. 287; nb. 2; (1998); p. 606 - 615, View in Reaxys 11 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
effect on cerebral glucose consumption
Measurement Parameter
qualitative
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
18/181
2018-08-03 18:12:50
Cinotti; Le Bars; Garcia-Larrea; Peyron; Gregoire; Lavenne; Krogsgaard-Larsen; Comar; Mauguiere; Journal de Chimie Physique et de Physico-Chimie Biologique; vol. 93; nb. 1; (1996); p. 48 - 52, View in Reaxys 12 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |agonist Bioassay : involvement of GABAA receptor in acetylcholine release neocortical slices prelabelled with <3H>choline, superfused (hemicholinium-3) and depolarized electrically (2 min, 3 Hz, 2 ms, 24 mA) 15 min after addition title comp., acetylcholine (ACh) release measd. by liquid scintillation
Biological Species/NCBI ID
human
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Feuerstein; Gleichauf; Peckys; Landwehrmeyer; Scheremet; Jackisch; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 354; nb. 5; (1996); p. 586 - 592, View in Reaxys 13 of 403
Substance Effect
Neuroregulatoric
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : Albino guinea pig medial nucleus tractus solitariusBioassay : mnTS = medial nucleus tractus solitarius; effect of 7-day morphine pretreatment (2 pellets per animal implanted containing 75 mg of morphine each pellet) pigs (200-300 g) decapitated, brainstems removed, slices containing mnTS prepared; neuronal action potentials recorded using glass electrode, spontaneous firing rate calculated
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.300000 µM
Qualitative Results
in neurons treated with title comp. a mean inhibition of neuronal firing of ca. 50 percent occurred; in morphine treated neurons inhibitory effect was significantly less, indicating subsensitivity
Measurement Parameter
qualitative
Malanga; Meng, Jianzhong; Fleming, William W.; Taylor, David A.; Journal of Pharmacology and Experimental Therapeutics; vol. 280; nb. 1; (1997); p. 16 - 23, View in Reaxys 14 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain cortex
Cell Fraction
Synaptosome: membrane (P2 fraction)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
19/181
2018-08-03 18:12:50
15 of 403
16 of 403
Substance RN
606417View in Reaxys
Substance Name
muscinol
Measurement Parameter
IC50
Unit
ÂľM
Quantitative value
0.01
Measurement pX
8
Concomitants: Compound RN
606417; 906818
Concomitants: Compound name
Muscimol; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
Sigma receptor [guinea pig]
Target Synonyms
sigma receptor
Target, Subunit, Species
Sigma receptor [guinea pig]
Target Mutant/Chimera Details
Sigma receptor [guinea pig]:Wild
Target Species (Bioactivity)
guinea pig
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Dunkin Hartley guinea pig
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Musicmol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
>
Quantitative value
100000
Measurement pX
1
Concomitants: Compound RN
5480843; 5480843
Concomitants: Compound name
[3H]-(+)-N-Allylnormetazocine; dl-N-Allylnormetazocine
Concomitants: Compound role
RAD; NSB
Target Name
Sigma receptor [guinea pig]
Target Synonyms
sigma receptor
Target, Subunit, Species
Sigma receptor [guinea pig]
Target Mutant/Chimera Details
Sigma receptor [guinea pig]:Wild
Target Species (Bioactivity)
guinea pig
Target Transfection
Non Transfected
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
20/181
2018-08-03 18:12:50
17 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Dunkin Hartley guinea pig
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Musicmol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
>
Quantitative value
100000
Measurement pX
1
Concomitants: Compound RN
1544735; 9349758
Concomitants: Compound name
Ethylketazocine; [3H]-(+)-EKC
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
cerebellum
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
1.8
Measurement pX
8.74
Concomitants: Compound RN
2114647; 606417; 906818
Concomitants: Compound name
Triton X100; Muscimol; [3H]-GABA
Concomitants: Compound role
COM; NSB; RAD
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
21/181
2018-08-03 18:12:50
18 of 403
19 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
cerebellum
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
39
Measurement pX
7.41
Concomitants: Compound RN
8365396; 8365396; 2114647
Concomitants: Compound name
Gabazine; [3H]-Gabazine; Triton X100
Concomitants: Compound role
NSB; RAD; COM
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
cerebellum
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
22/181
2018-08-03 18:12:50
20 of 403
Quantitative value
135
Measurement pX
6.87
Concomitants: Compound RN
8365396; 8365396
Concomitants: Compound name
Gabazine; [3H]-Gabazine
Concomitants: Compound role
NSB; RAD
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Cavia porcellus, pigmented guinea pigBioassay : VNC: vestibular nuclear complex; SN: spontaneous nystagmus; YHT: yaw head tilt; RHT: roll head tilt; control: vehicle title comp. infused into VNC of 4 animals using osmotic mini-pump for 30 h, then pump disconnected; SN, YHT, RHT obtained using videorecording within 30 h, at 31, 33, 50 h after onset of infusion
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. increased mean YHT at 1 - 20 h but not at 25, 30 h after infusion onset; induced RHT but increase was not significant; SN exhibited by one animal at 10 h after infusion onset without affecting SN frequency; no effect after pump disconnection
Measurement Parameter
qualitative
Gliddon, Catherine M.; Darlington, Cynthia L.; Smith, Paul F.; Journal of Pharmacology and Experimental Therapeutics; vol. 313; nb. 3; (2005); p. 1126 - 1135, View in Reaxys 21 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Cavia porcellus, pigmented guinea pigBioassay : VNC: vestibular nuclear complex; UVD: unilateral vestibular deafferentation; SN: spontaneous nystagmus; YHT: yaw head tilt; RHT: roll head tilt; control: vehicle title comp. infused into contralateral VNC using osmotic mini-pump for 30 h post-UVD induced by aspiration of semicircular canals ampullae, utricle and saccule maculae; SN, YHT, RHT obtained using videorecording during infusion, at 31, 33, 50 h post-UVD
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. dose-dependently decreased SN frequency, mean THT and RHT with more pronounced effect on RHT; after infusion values of SN frequency, mean RHT and THT returned to control by 30, 50, 33 h, resp.; only SN rate of compensation affected
Measurement Parameter
qualitative
Gliddon, Catherine M.; Darlington, Cynthia L.; Smith, Paul F.; Journal of Pharmacology and Experimental Therapeutics; vol. 313; nb. 3; (2005); p. 1126 - 1135, View in Reaxys 22 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Cavia porcellus, pigmented guinea pigBioassay : VNC: vestibular nuclear complex; UVD: unilateral vestibular deafferentation; SN: spontaneous nystagmus; YHT: yaw head tilt; RHT: roll head tilt; control: vehicle title comp. infused into ipsilateral VNC using osmotic mini-pump for 30 h after UVD induced by aspiration of semicircular canals ampullae, utricle and saccule maculae; SN, YHT, RHT obtained using videorecording during infusion, at 31, 33, 50 h post-UVD
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
23/181
2018-08-03 18:12:50
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. dose-dependently increased YHT but not its rate of compensation only during infusion at 20, 30 h post-UVD, no effect observed by 33 h post-UVD; no effect on SN and RHT
Measurement Parameter
qualitative
Gliddon, Catherine M.; Darlington, Cynthia L.; Smith, Paul F.; Journal of Pharmacology and Experimental Therapeutics; vol. 313; nb. 3; (2005); p. 1126 - 1135, View in Reaxys 23 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Cavia porcellus, pigmented guinea pigBioassay : VNC: vestibular nuclear complex; UVD: unilateral vestibular deafferentation title comp. infused into ipsilateral VNC using osmotic minipump for 30 h after UVD induced by aspiration of semicircular canals ampullae, utricle and saccule maculae; distress inspected
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. induced distress of animals
Measurement Parameter
qualitative
Gliddon, Catherine M.; Darlington, Cynthia L.; Smith, Paul F.; Journal of Pharmacology and Experimental Therapeutics; vol. 313; nb. 3; (2005); p. 1126 - 1135, View in Reaxys 24 of 403
25 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
14
Measurement pX
7.85
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
24/181
2018-08-03 18:12:50
26 of 403
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
0.7
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
20
Measurement pX
7.7
Concomitants: Compound RN
774694
Concomitants: Compound name
[3H]-Muscimol
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
25/181
2018-08-03 18:12:50
27 of 403
Concomitants: Compound role
RAD
Substance Effect
Neuroregulatoric
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : further invest. with N-methyl-D-aspartate and AMPA/kainate receptor antagonists (2amino-7-phosphonoheptanoate and glutamic acid diethyl ester (GDEE), resp.); control: vehicle rats administered with title comp. 30 min before electric stimulation of inferior colliculus by bipolar brain electrode (60 Hz, 15 sec, 2 min intervals); alertness, freezing, escape (ALT, FRZ, ESC) thresholds defined; behaviour recorded by videocamera
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.100000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
0.5 mg/kg title comp. sign. decreased intensity of electric current needed to produce ALT, FRZ and ESC responses and increased duration of FRZ from ca. 18 to ca. 55 s; effects blocked by GDEE (figures)
Measurement Parameter
qualitative
Nobre, Manoel Jorge; Borelli, Karina Genaro; Brandao, Marcus L.; Life Sciences; vol. 71; nb. 25; (2002); p. 2961 - 2972, View in Reaxys 28 of 403
Substance Effect
Anticonvulsant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : DBA/2J miceBioassay : visual observation of behaviour mice weight 16-24 g, age 42-48 d; treatment with title compound, then with pefloxacin mesylate (i.p., approximately 95 percent convulsant dose of 0.78 mg/g)
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebroventricular administration
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
0.19 - 0.25
De Sarro; Nava; Calapai; Antimicrobial Agents and Chemotherapy; vol. 41; nb. 2; (1997); p. 427 - 434, View in Reaxys 29 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : motor function evaluated; only doses without motor deficit used; title comp. effect on P1R and P2R, with perF or postF administration, studied 300-325 g rats (12 h light:dark cycle); 50 Îźl 5 percent s.c. formalin inj. (FI) into the dorsal surface of right hind paw; response to FI (flinches) counted for 1 min at 1-2, 5-6 min after FI (phase 1 resp., P1R), /5 min 10-60 min after FI (phase 2 resp.,P2R)
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intrathecal administration
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
26/181
2018-08-03 18:12:50
Qualitative Results
preF: dose-dependent decrease of flinch response (ED50, μg: 1.19 <P1R>; 0.40 <P2R>); postF (0.3 μg): significant suppression of P2R; P1R unaffected (graph); at doses >=1.0 μg: motor depression caused
Measurement Parameter
qualitative
Dirig; Yaksh; Journal of Pharmacology and Experimental Therapeutics; vol. 275; nb. 1; (1995); p. 219 - 227, View in Reaxys 30 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |agonist Target : ICR miceBioassay : antinociception detn. by tail-flick response tested 30, 30 and 20 min after i.c.v. injection of β-endorphin, or DPDPE or U50,488H; hot-plate response tested 15, 15, 10 and 10 min after i.c.v. injection of β-endorphin or DPDPE or U50,488H mice pretreated with tile comp. (GABAA receptor agonist) 10 min before i.c.v. administration of 1 μg of β-endorphine or 10 μg of DPDPE or 60 μg of U50,488H
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebroventricular administration
Qualitative Results
title comp. dose-dependently attenuated the inhibition of the tail-flick and hot-plate responses induced by β-endorphine (β-receptor agonist) or by DPDPE (β-receptor agonist) or by U50,488H (β-receptor agonist)
Measurement Parameter
qualitative
Suh; Song; Kim; Choi; Yoo; Tseng; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 352; nb. 6; (1995); p. 614 - 619, View in Reaxys 31 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |agonist Target : ICR miceBioassay : antinociception detn. by tail-flick response tested 30, 30 and 20 min after i.c.v. injection with saline or morphine; hot-plate response tested 15, 15, 10 and 10 min after i.c.v. injection of morphin; Graphical representation mice pretreated with tile comp. (GABAA receptor agonist) 10 min before i.c.v. administration of saline or 2 μg morphine
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebroventricular administration
Qualitative Results
title comp. alone did not affect any significant effet on the latencies of the tail-flick and hot-plate responses, but dose-dependently attenuated inhibition of the tail-flick and hot-plate resopnses induced by morphine (μ-receptor agonist)
Measurement Parameter
qualitative
Suh; Song; Kim; Choi; Yoo; Tseng; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 352; nb. 6; (1995); p. 614 - 619, View in Reaxys 32 of 403
Bioassay Category
Metabolism/Transport
Bioassay Name
Flux uptake
Bioassay Details
Effect : 36Cl- uptake |transport Target : ddY mouse cortical synaptoneurosomesBioassay : synaptoneurosomal fraction was isolated from cerebral cortices of male ddY mice (7 weeks old, 30-32 g) synaptoneurosomes were preincub. in buffer A at 30 deg C for 3 min, title comp. was added and 36Cl- (NaCl; 3 mCi/g) uptake was determined after a 3-s incubation period; filtration through Whatman GF/C filters; radioactivity measuring
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
25 µM
Qualitative Results
title comp. significantly increased 36Cl- uptake into mouse cortical synaptoneurosomes
Measurement Parameter
qualitative
Maruyama, Yuji; Kuribara, Hisashi; Kishi, Eiko; Weintraub, Susan T.; Ito, Yoshihisa; Journal of Pharmacy and Pharmacology; vol. 53; nb. 5; (2001); p. 721 - 725, View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
27/181
2018-08-03 18:12:50
33 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Bioassay : effect of title comp. on morphine-induced allodynia; effect at the maximal score of allodynia obtained 15 min after i.t. injection of morphine assessed in vivo; test mice (ca. 22 g) divided into groups (6 mice/gr.), title comp. and 0.5 mg/kg morphine i.t. admin. simultaneously; control group received morphine alone; after admin., mice placed individual and observed
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
8 ng/kg
Substance Route of Adm.
intrathecal administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Hara, Naoki; Minami, Toshiaki; Okuda-Ashitaka, Emiko; Sugimoto, Tetsuo; Sakai, Masato; Onaka, Masahiko; Mori, Hidemaro; Imanishi, Toshihiro; Shingu, Koh; Ito, Seiji; British Journal of Pharmacology; vol. 121; nb. 3; (1997); p. 401 408, View in Reaxys 34 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Bioassay : effect of title comp. on nociceptin-induced allodynia; effect at the maximal score of allodynia obtained 10 min after i.t. injection of nociceptin assessed in vivo; test mice (ca. 22 g) divided into groups (6 mice/gr.), title comp. and 2.5 ng/kg nociceptin i.t. admin. simultaneously; control group received nociceptin alone; after admin., mice placed individual and observed
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
5 µg/kg
Substance Route of Adm.
intrathecal administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Hara, Naoki; Minami, Toshiaki; Okuda-Ashitaka, Emiko; Sugimoto, Tetsuo; Sakai, Masato; Onaka, Masahiko; Mori, Hidemaro; Imanishi, Toshihiro; Shingu, Koh; Ito, Seiji; British Journal of Pharmacology; vol. 121; nb. 3; (1997); p. 401 408, View in Reaxys 35 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : inhibition of neurotransmissionBioassay : MBP = mean blood pressure; HR = heart rate; RNA = renal nerve activity; PHE = l-phenylephrine; 8-OH-DPAT = 8-hydroxy-2-(di-n-propylamino)tetralin weight 2.8-3.6 kg; anaesthetized; 3 bilateral microinjections of title comp. administrated into the lateral tegmental field; baroreceptor reflex activation caused by PHE (5 μg/kg, i.v.); then 8OH-DPAT administration (1-30 μg/kg, i.v.)
Biological Species/NCBI ID
cat
Substance RN
606417View in Reaxys
Substance Name
31872
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
28/181
2018-08-03 18:12:50
Qualitative Results
decreased MBP, HR, RNA (by -35 mmHg, -30 beats/min and -53 percent, resp.); greatly reduced effects of subsequent administration of 8-OH-DPAt, values of MBP, HR and RNA after 30 μg/kg were 94 mmHg, 148 beats/min and 48 percent, resp.
Measurement Parameter
qualitative
Vayssettes-Courchay; Bouysset; Verbeuren; Laubie; European Journal of Pharmacology; vol. 285; nb. 3; (1995); p. 299 304, View in Reaxys 36 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : inhibition of neurotransmissionBioassay : MBP = mean blood pressure; HR = heart rate; RNA = renal nerve activity; PHE = l-phenylephrine; 8-OH-DPAT = 8-hydroxy-2-(di-n-propylamino)tetralin weight 2.8-3.6 kg; anaesthetized; 3 bilateral microinjections of title comp. into the nucleus tractus solitarii; baroreceptor reflex activation caused by PHE (5 μg/kg, i.v.); then 8-OHDPAT administration (1-30 μg/kg, i.v.)
Biological Species/NCBI ID
cat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
no significant change in MBP, HR, RNA; suppressed baroreceptor reflex; did not alter 8-OH-DPATinduced dose-related hypotension, bradycardia, sympatho-inhibition: MBP decreased by -35 mmHg, HR reduced by -42 beats/min, RNA by -79 percent (at 30 μg/kg)
Measurement Parameter
qualitative
Vayssettes-Courchay; Bouysset; Verbeuren; Laubie; European Journal of Pharmacology; vol. 285; nb. 3; (1995); p. 299 304, View in Reaxys 37 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : 1.0 mg/kg dose of diazepam occasioned 93.0 percent of drug-associated lever responding substitutional assay; rats trained to discriminate diazepam vs saline and to press appropriate lever; the level of pressing on drug-associated lever determined 15 min after administration of title comp. during a 15-min test session
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.100000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
title comp. occasioned 0.7 percent of diazepam-appropriate responding maximum
Measurement Parameter
qualitative
Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 2; (2004); p. 540 - 547, View in Reaxys 38 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : 3.2 mg/kg dose of baclofen occasioned 81.2 percent of drug-associated lever responding substitutional assay; rats trained to discriminate baclofen vs saline and to press appropriate lever; the level of pressing on drug-associated lever determined 15 min after administration of title comp. during a 15-min test session
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
29/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
0.100000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
title comp. occasioned 9.7 percent of responding on drug-associated lever maximum
Measurement Parameter
qualitative
Carter; Unzeitig; Wu; Chen; Coop; Koek; France, Charles P.; Journal of Pharmacology and Experimental Therapeutics; vol. 309; nb. 2; (2004); p. 540 - 547, View in Reaxys 39 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : exogeneous tachykinin (substance P)-induced contractions; effect onTarget : tracheal rings of guinea pigBioassay : Example 8 - An Agonist At The GABAA Receptor, Muscimol, Dose-Dependently Mimics Propofol's Relaxation Of A Tachykinin-Induced Contraction InGuinea Pig And Human Tracheal Rings And An Antagonist At The GABAA Receptor Attenuates Propofol-Induced Relaxation[0078] Propofol's effect
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title compound at 0-1000&micro;M dose-dependently relaxed exogeneous tachykinin (substance P)-induced contraction; figure is given
Measurement Parameter
qualitative
Patent; EMALA, Charles, W.; (68 pag.); WO2007/143038; (A1); (2007), View in Reaxys 40 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : exogeneous tachykinin (substance P)-induced contractions; effect onTarget : tracheal rings of humanBioassay : Example 8 - An Agonist At The GABAA Receptor, Muscimol, Dose-Dependently Mimics Propofol's Relaxation Of A Tachykinin-Induced Contraction InGuinea Pig And Human Tracheal Rings And An Antagonist At The GABAA Receptor Attenuates Propofol-Induced Relaxation[0078] Propofol's effect
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title compound dose-dependently relaxed exogeneous tachykinin (substance P)-induced contraction; figure is given
Measurement Parameter
qualitative
Patent; EMALA, Charles, W.; (68 pag.); WO2007/143038; (A1); (2007), View in Reaxys 41 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Bioassay Details
Effect : electrophysiologicalTarget : spinal cord membranes of Sprague-Dawley ratBioassay : whole-cell patch clamp recordings; Student's 2-tailed t test spinal cord removed from 7-16 d old rats; effect on electrophysiological properties of sympathetic preganglionic neurones (SPNs) in rat slices
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 ÂľM
Qualitative Results
spontaneous action potential firing, spontaneous membrane potential oscillations were abolished; input resistance reduced; when applied at resting potential, either depolarization, hyperpolarization or no change in membrane potential observed
Measurement Parameter
qualitative
Nolan; Gibson; Logan; British Journal of Pharmacology; vol. 121; nb. 2; (1997); p. 324 - 330, View in Reaxys 42 of 403
Substance Effect
Sympathomimetic
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
30/181
2018-08-03 18:12:50
Bioassay Name
In Vitro (others)
Bioassay Details
Target : New Zealand White rabbitBioassay : MAP, mean arterial pressure; RSNA, renal sympathetic nerve activity; CVLM, caudal ventrolateral medulla anesthetized rabbits (2.4-4.3 kg); microinjections of title comp. in the caudal medullary raphe oder in CVLM
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
no effect of title comp. on MAP or RSNA when injected into the caudal medullary raphe but evoked a pressor and sympathoexcitatory response when injected into the CVLM
Measurement Parameter
qualitative
Coleman; Dampney; American Journal of Physiology - Regulatory Integrative and Comparative Physiology; vol. 268; nb. 5 37-5; (1995); p. R1295-R1302, View in Reaxys 43 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
inhibitory activities in GABAA receptor assay, IC 50 (μM/ml) = 2.9 x 10-3
Measurement Parameter
qualitative
Tatsuta; Yasuda; Journal of Antibiotics; vol. 49; nb. 7; (1996); p. 713 - 715, View in Reaxys 44 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : 300-g rats; food and water ad libitum; ingestive behavior tested
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
significant increase of food and water intake
Measurement Parameter
qualitative
Klitenick; Wirtshafter; Journal of Pharmacology and Experimental Therapeutics; vol. 273; nb. 1; (1995); p. 327 - 336, View in Reaxys 45 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : norepinephrine-stimulated secretion of protein Target : ;des-acyl ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 30 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 46 of 403
Bioassay Category
In Vitro (Efficacy)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
31/181
2018-08-03 18:12:50
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : norepinephrine-stimulated secretion of protein Target : ;ghrelinSpecies : TgGhrelin-SV40T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 30 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 47 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein cellular content Target : ;des-acyl ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 10 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 48 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein cellular content Target : ;ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 10 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 49 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein secretion Target : ;des-acyl ghrelinSpecies : TgGhrelin-SV40-T mouse 1672 Bioassay : stomach ghrelinoma SG-1 cells
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
32/181
2018-08-03 18:12:50
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 50 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein secretion Target : ;des-acyl ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 10 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 51 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein secretion Target : ;ghrelinSpecies : TgGhrelin-SV40-T mouse 1672 Bioassay : stomach ghrelinoma SG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 52 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein secretion Target : ;ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
<= 10 µM
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
33/181
2018-08-03 18:12:50
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 53 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein synthesis Target : ;ghrelinSpecies : TgGhrelin-SV40-T mouse 8175 Bioassay : pancreatic ghrelinoma PG-1 cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Zhao, Tong-Jin; Sakata, Ichiro; Li, Robert Lin; Liang, Guosheng; Richardson, James A.; Brown, Michael S.; Goldstein, Joseph L.; Zigman, Jeffrey M.; Proceedings of the National Academy of Sciences of the United States of America; vol. 107; nb. 36; (2010); p. 15868 - 15873, View in Reaxys 54 of 403
55 of 403
Target Name
GABA-A receptor; Opioid receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor + opioid receptor; opioid receptor activity
Target, Subunit, Species
GABA-A receptor; Opioid receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild; Opioid receptor:Wild
Target Transfection
Non Transfected; Non Transfected
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : behavioural symptomsmonkeys trained to discriminate L-838,417; response: each press of a lever with a minimum downward force of approximately 0.25 N produced an audible click
Biological Species/NCBI ID
Saimiri sciureus
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.300000 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
% L-838,417-appropriate responding 0
Measurement Parameter
qualitative
Target Name
Histamine H1 receptor [rat]
Target Synonyms
h1r; hh1r; histamine h1 receptor; hrh1
Target Uniprot ID
p31390
Target, Subunit, Species
Histamine H1 receptor [rat]
Target Mutant/Chimera Details
Histamine H1 receptor [rat]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
34/181
2018-08-03 18:12:50
56 of 403
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
435610; 87215
Concomitants: Compound name
[3H]-Pyrilamine; Triprolidine
Concomitants: Compound role
RAD; NSB
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : murine homomeric β1 GABAA subunitBioassay : β1 mouse cDNA, injected in Xenopus oocytes; electrophysiological recording tech.; membrane conductance
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
500 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Krishek; Moss; Smart; Molecular Pharmacology; vol. 49; nb. 3; (1996); p. 494 - 504, View in Reaxys 57 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : cerebellar membranes from Sprague-Dawley ratsBioassay : membrane homogenates of cerebellum from rats prepared according to Endo and Olsen (J.Neurochem. 59,1444 (1993)); supernatant or pellet suspension incubated with ligand; radioligand assay
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
binding activities of immunoprecipitates in Fig.
Measurement Parameter
qualitative
Huh, Kyung-Hye; Endo, Shuichi; Olsen, Richard W.; European Journal of Pharmacology; vol. 310; nb. 2-3; (1996); p. 225 233, View in Reaxys 58 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |antagonist Target : rat cerebellar granule cell membranesBioassay : in vitro; radioligand binding assay; 4 nM <3H>GABA (spec. act.: 86 Ci/mmol); cell membranes (25-70 β protein) treated with Triton X-100; Tris-citrate buffer; 0 deg C; incubation time 20 min; scintillation counting
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
35/181
2018-08-03 18:12:50
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1.00000E-11 M
Measurement Parameter
IC50
Unit
nM
Quantitative value
3
Measurement pX
8.52
Vale, Carmen; Pomes, Anna; Rodriguez-Farre, Eduard; Sunol, Cristina; European Journal of Pharmacology; vol. 319; nb. 2-3; (1997); p. 343 - 353, View in Reaxys 59 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : decrease of dopamine releaseBioassay : time - dopamine release curve rat weight 300-350 g; 5-6 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; title comp. local perfusion; perfusate collected every 20 min for 120 min; reverse-phase HPLC-ED
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 µM
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. decreased accumbens dopamine release at 50 μmol/l, but not at 10 μmol/l (diagrams given)
Measurement Parameter
qualitative
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell; European Journal of Pharmacology; vol. 306; nb. 1-3; (1996); p. 33 - 39, View in Reaxys 60 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Bioassay : time - dopamine release curve; rp = reverse-phase rat weight 300-350 g; 5-6 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; 100 mg/kg s.c. modafinil injection; title comp. local perfusion; perfusate collected every 20 min for 120 min; rp HPLC-ED
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 µM
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. fully antagonized modafinil-induced increase of accumbens dopamine release (diagram given)
Measurement Parameter
qualitative
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell; European Journal of Pharmacology; vol. 306; nb. 1-3; (1996); p. 33 - 39, View in Reaxys 61 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |antagonist Bioassay : microdialysis; effect on nomifensine-induced (50μM) changes in extracellular dopamine (DO) levels; title compound is a GABAA receptor agonist rats (250-350 g) housed 3 or 4 per cage at 22 degC, food and water ad libitum; rats anesthetized, concentric dialysis probe implanted into left medial prefrontal cortex
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
36/181
2018-08-03 18:12:50
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
50 µM
Qualitative Results
ca. DO percent of basal level at 0, 30, 60 and 90 min (PCP/PCP+title compound): 100, 3100/800, 2300/500, 500/200; MK/MK+title compound: 100, 350/120, 275/90, 150/80
Measurement Parameter
qualitative
Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki; European Journal of Pharmacology; vol. 341; nb. 1; (1998); p. 45 - 56, View in Reaxys 62 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |antagonist Bioassay : microdialysis; effect on phencyclidine- (PCP, 500μM) or MK-801induced (MK, 50μM) changes in extracellular dopamine (DO) levels; title compound is a GABAA receptor agonist rats (250-350 g) housed 3 or 4 per cage at 22 degC, food and water ad libitum; rats anesthetized, concentric dialysis probe implanted into left medial prefrontal cortex
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
50 µM
Qualitative Results
ca. DO percent of basal level at 0, 30, 60 and 90 min (PCP/PCP+title compound): 100, 3100/800, 2300/500, 500/200; MK/MK+title compound: 100, 350/120, 275/90, 150/80
Measurement Parameter
qualitative
Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki; European Journal of Pharmacology; vol. 341; nb. 1; (1998); p. 45 - 56, View in Reaxys 63 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |secretion stimulant Bioassay : microdialysis; extracellular dopamine (DO) levels; title compound is a GABAA receptor agonist rats (250-350 g) housed 3 or 4 per cage at 22 degC, food and water ad libitum; rats anesthetized, concentric dialysis probe implanted into left medial prefrontal cortex
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
50 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Yonezawa, Yuji; Kuroki, Toshihide; Kawahara, Takeshi; Tashiro, Nobutada; Uchimura, Hideyuki; European Journal of Pharmacology; vol. 341; nb. 1; (1998); p. 45 - 56, View in Reaxys 64 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |transport Target : NMRI albino mouse brain homogenatesBioassay : in vitro; effect on 36Cl- uptake into brain microsacs assayed; brain homogenates from naive or small platform stressed mice; title comp. and 50 nCi of 36Cl- added; scintillation counting
Substance RN
606417View in Reaxys
Substance Name
31872
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
37/181
2018-08-03 18:12:50
Substance Dose
0.300000 µM
Qualitative Results
title comp. stimulated 36Cl- uptake by cortical as well as cerebellar microsacs from naive and stressed mice
Measurement Parameter
qualitative
Pokk; Liljequist; Zharkovsky; European Journal of Pharmacology; vol. 317; nb. 1; (1996); p. 15 - 20, View in Reaxys 65 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Bioassay : cGMP : cyclic guanosine 3',5'-monophosphate; TRH : thyrotropinreleasing hormone rats (250-300 g) given s.c. injection of TRH tartrate (25 mg/kg to increase cGMP level)) after injection of title comp.; 10 min later animals killed; brain dissected; cGMP levels in various cerebellar areas determined by RIA method
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
pretreatment with title comp. suppressed TRH-induced increase in cGMP level in cerebellum
Measurement Parameter
qualitative
Nakayama, Takahiro; Hashimoto, Tadatoshi; Nagai, Yasuo; European Journal of Pharmacology; vol. 316; nb. 2-3; (1996); p. 157 - 164, View in Reaxys 66 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : SKF 82958 - quinpirole mixture injected to nucleus accumbens shell cannula inserted to brain of rats (260-330 g) for application of title comp., bicuculline (150 ng) SKF 82958 (5 μg) quinpirole (10 μg) mixture; jaw movements and electromyographic activity recorded from digastric and masseter muscles
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. (50 ng) completely abolished electromyographic activity induced by bicuculline; dosedependent inhibition of SKF 82958 - quinpirole induced effect; title comp. itself ineffective
Measurement Parameter
qualitative
Uchida, Takuya; Adachi, Kazunori; Fujita, Satoshi; Lee, Jun; Gionhaku, Nobuhito; Cools, Alexander R.; Koshikawa, Noriaki; European Journal of Pharmacology; vol. 510; nb. 1-2; (2005); p. 39 - 47, View in Reaxys 67 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : receptor expression; induction ofBioassay : GABA: β-aminobutyric acid; nonspecific binding determined in the presence of 100 μmol/l diazepam; Scatchard analysis used cells expressing β1β2β2s GABAA receptors were treated with title comp. for 96 h; cell membranes were incubated with <3H>flunitrazepam (0.2 - 16 nmol/l); the effect of title comp. on Bmax and Kd of <3H>flunitrazepam binding was determined
Biological Species/NCBI ID
human
Cells/Cell Lines
HEK293 cell line
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
38/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
100 µM
Qualitative Results
title comp. increased the maximum number of <3H>flunitrazepam binding sites by 96.1 percent; Kd of these sites was unchanged
Measurement Parameter
qualitative
Pericic, Danka; Strac, Dubravka Svob; Jembrek, Maja Jazvinscak; Rajcan, Ivana; European Journal of Pharmacology; vol. 482; nb. 1-3; (2003); p. 117 - 125, View in Reaxys 68 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Target : human embryonic kidney HEK 293 cell membranesBioassay : nonspecific binding determined in presence of clonazepam or β-aminobutyric acid; β1Y159S: GABAA receptor β1 subunit in which tyrosine at position 159 mutated to serine membranes of cells expressing rat β1Y159S and wild-type β2 and β2 GABAA receptor subunits incubated with <3H>-labeled title comp. for 60 min; 4 deg C; pH 7.2; samples filtered; filters washed; radioactivity on filter determined
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1.50000 nM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
19.04
Measurement pX
7.72
Amin, Jahanshah; Brooks-Kayal, Amy; Weiss, David S.; Molecular Pharmacology; vol. 51; nb. 5; (1997); p. 833 - 841, View in Reaxys 69 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Target : human embryonic kidney HEK 293 cell membranesBioassay : nonspecific binding determined in presence of clonazepam or β-aminobutyric acid; β1Y209F: GABAA receptor β1 subunit in which tyrosine at position 209 mutated to phenylalanine membranes of cells expressing rat β1Y209F and wild-type β2 and β2 GABAA receptor subunits incubated with <3H>-labeled title comp. for 60 min; 4 deg C; pH 7.2; samples filtered; filters washed; radioactivity on filter determined
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1.50000 nM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
14.1
Measurement pX
7.85
Amin, Jahanshah; Brooks-Kayal, Amy; Weiss, David S.; Molecular Pharmacology; vol. 51; nb. 5; (1997); p. 833 - 841, View in Reaxys 70 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Target : human embryonic kidney HEK 293 cell membranesBioassay : nonspecific binding determined in presence of clonazepam or β-aminobutyric acid; β1Y209S: GABAA receptor β1 subunit in which tyrosine at position 209 mutated to serine membranes of cells expressing rat β1Y209S and wild-type β2 and β2 GABAA receptor subunits incubated with <3H>-labeled title comp. for 60 min; 4 deg C; pH 7.2; samples filtered; filters washed; radioactivity on filter determined
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
39/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
1.50000 nM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
16.57
Measurement pX
7.78
Amin, Jahanshah; Brooks-Kayal, Amy; Weiss, David S.; Molecular Pharmacology; vol. 51; nb. 5; (1997); p. 833 - 841, View in Reaxys 71 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Target : human embryonic kidney HEK 293 cell membranesBioassay : nonspecific binding determined in presence of clonazepam or β-aminobutyric acid membranes of cells expressing rat wild-type β1, β2 and β2 GABAA receptor subunits incubated with <3H>labeled title comp. for 60 min; 4 deg C; pH 7.2; samples filtered; filters washed; radioactivity on filter determined
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1.50000 nM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
13.87
Measurement pX
7.86
Amin, Jahanshah; Brooks-Kayal, Amy; Weiss, David S.; Molecular Pharmacology; vol. 51; nb. 5; (1997); p. 833 - 841, View in Reaxys 72 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
cerebellum
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.004
Measurement pX
8.4
Concomitants: Compound RN
906818; 774694
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
40/181
2018-08-03 18:12:50
73 of 403
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
1
Measurement Parameter
IC50
Unit
nM
Quantitative value
3
Deviation
0.300000
Measurement pX
8.52
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Nordmann; Graff; Maurer; Gahwiler; Journal of Medicinal Chemistry; vol. 28; nb. 8; (1985); p. 1109 - 1111, View in Reaxys 74 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Oncins France 1 mouse
Substance RN
606417View in Reaxys
Substance Name
1
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
ID150
Unit
mg/kg
Quantitative value
0.76
Concomitants: Compound name
Bicuculline
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
41/181
2018-08-03 18:12:50
Concomitants: Compound role
IAV
Nordmann; Graff; Maurer; Gahwiler; Journal of Medicinal Chemistry; vol. 28; nb. 8; (1985); p. 1109 - 1111, View in Reaxys 75 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
CD-1 mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
17
Deviation
3
Kaplan; Raizon; Desarmenien; Feltz; Headley; Worms; Lloyd; Bartholini; Journal of Medicinal Chemistry; vol. 23; nb. 6; (1980); p. 702 - 704, View in Reaxys 76 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Lethality
Qualitative value
>
Quantitative value
2
Concomitants: Compound name
Bicuculline
Concomitants: Compound role
IAV
Kaplan; Raizon; Desarmenien; Feltz; Headley; Worms; Lloyd; Bartholini; Journal of Medicinal Chemistry; vol. 23; nb. 6; (1980); p. 702 - 704, View in Reaxys 77 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
42/181
2018-08-03 18:12:50
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Convulsions
Quantitative value
0.25
Deviation
0.100000
Concomitants: Compound name
Bicuculline
Concomitants: Compound role
IAV
Kaplan; Raizon; Desarmenien; Feltz; Headley; Worms; Lloyd; Bartholini; Journal of Medicinal Chemistry; vol. 23; nb. 6; (1980); p. 702 - 704, View in Reaxys 78 of 403
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
5.00000E-09 M
Measurement Parameter
Ki (inhibition constant)
Unit
ÂľM
Quantitative value
0.004
Deviation
0.00100000
Measurement pX
8.4
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
RAD
Kaplan; Raizon; Desarmenien; Feltz; Headley; Worms; Lloyd; Bartholini; Journal of Medicinal Chemistry; vol. 23; nb. 6; (1980); p. 702 - 704, View in Reaxys 79 of 403
Target Name
GABA receptor [human]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [human]
Target Mutant/Chimera Details
GABA receptor [human]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
43/181
2018-08-03 18:12:50
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
human
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
5.00000E-09 M
Measurement Parameter
Ki (inhibition constant)
Unit
ÂľM
Quantitative value
0.011
Deviation
0.00200000
Measurement pX
7.96
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
RAD
Kaplan; Raizon; Desarmenien; Feltz; Headley; Worms; Lloyd; Bartholini; Journal of Medicinal Chemistry; vol. 23; nb. 6; (1980); p. 702 - 704, View in Reaxys 80 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
mouse Swiss CD-1
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Convulsions
Quantitative value
0.7
Concomitants: Compound RN
773807
Concomitants: Compound name
3-Mercaptopropionic acid
Concomitants: Compound role
IAV
Sarges; Howard; Koe; Weissman; Journal of Medicinal Chemistry; vol. 32; nb. 2; (1989); p. 437 - 444, View in Reaxys 81 of 403
Bioassay Category
In Vivo (Animal models)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
44/181
2018-08-03 18:12:50
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
CD rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
cGMP level
Quantitative value
1.5
Concomitants: Compound RN
119374
Concomitants: Compound name
Isoniazid
Concomitants: Compound role
IAV
Sarges; Howard; Koe; Weissman; Journal of Medicinal Chemistry; vol. 32; nb. 2; (1989); p. 437 - 444, View in Reaxys 82 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
4.2
Sarges; Howard; Koe; Weissman; Journal of Medicinal Chemistry; vol. 32; nb. 2; (1989); p. 437 - 444, View in Reaxys 83 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
3.2 - 10
Sarges; Howard; Koe; Weissman; Journal of Medicinal Chemistry; vol. 32; nb. 2; (1989); p. 437 - 444, View in Reaxys 84 of 403
Bioassay Category
In Vivo (Animal models)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
45/181
2018-08-03 18:12:50
Bioassay Name
In Vivo: Binding
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
32 µmol/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
stimulation percentage
Unit
%
Measurement Object
stimulation of [3H]-Flunitrazepam binding
Quantitative value
124
Concomitants: Compound RN
702691
Concomitants: Compound name
[3H]-Flunitrazepam
Concomitants: Compound role
OCV
Sarges; Howard; Koe; Weissman; Journal of Medicinal Chemistry; vol. 32; nb. 2; (1989); p. 437 - 444, View in Reaxys 85 of 403
Substance Effect
Antiproliferative
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : control: flies not administered with title comp. in eggs from female flies collected in Tokyo, central Japan; reared by using vials with test medium containing title comp. solution; pupae formed in the vials counted daily to determine pupation time (days from egg to pupation) and measured for size
Biological Species/NCBI ID
Drosophila
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
25 mg/L
Qualitative Results
increase in title comp. conc. significantly prolonged pupation time at 250 μg/ml; no significant effect in pupal size; table
Measurement Parameter
qualitative
Tuno, Nobuko; Takahashi, Kazuo H.; Yamashita, Hiroshi; Osawa, Naoya; Tanaka, Chihiro; Journal of Chemical Ecology; vol. 33; nb. 2; (2007); p. 311 - 317, View in Reaxys 86 of 403
Substance Effect
Toxic
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : control: flies not administered with title comp. in eggs from female flies collected in Tokyo, central Japan; reared by using vials with test medium containing title comp. solution; eggto-pupa survival determined by counting pupae formed in the vials daily
Biological Species/NCBI ID
Drosophila
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
25 mg/L
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
46/181
2018-08-03 18:12:50
Qualitative Results
increase in title comp. conc. significantly decreased egg-to-pupa survival at 125 Îźg/ml; table
Measurement Parameter
qualitative
Tuno, Nobuko; Takahashi, Kazuo H.; Yamashita, Hiroshi; Osawa, Naoya; Tanaka, Chihiro; Journal of Chemical Ecology; vol. 33; nb. 2; (2007); p. 311 - 317, View in Reaxys 87 of 403
Substance Effect
Neuroregulatoric
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : English short hair albino guinea pig brain slicesBioassay : LC: locus ceruleus; rats implanted subcutaneously with morphine pellet (75 mg) for 7 days before experiment slices containing LC voltage clamped at -60 mV under whole-cell patch clamp configuration; rate of action potential firing recorded
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 nM
Qualitative Results
title comp. dose-dependently inhibited spontaneous firing, after morphine pretreatment significant subsensitivity observed compared to lactose-pretreated control, at 1000 nmol/l curves intersected
Measurement Parameter
qualitative
Kong; Meng; Biser; Fleming; Taylor; Journal of Pharmacology and Experimental Therapeutics; vol. 298; nb. 3; (2001); p. 909 - 916, View in Reaxys 88 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Long-Evans rat pupBioassay : BT also measured; in presence of bicuculline (BC), title comp. showed no effect on BT (body temp.); BC antagonized title comp. effect on LMA 7-d old pups separated from mother; BT was 33 deg C; title comp. admin. alone (30 min before the test) or along with AL (10 min before the test) or BC (35 min before the test); placed on 20 deg C grid surface, 2-min; locomotor activity (LMA) recorded
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.00300000 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. alone dose-dependently decreased LMA (0.3-0.6 mg/kg), no effect on BT; in presence of AL, title comp. showed no effect on LMA and BT; tables
Measurement Parameter
qualitative
Vivian, Jeffrey A.; Barros, Helena M. T.; Manitiu, Andre; Miczek, Klaus A.; Journal of Pharmacology and Experimental Therapeutics; vol. 282; nb. 1; (1997); p. 318 - 325, View in Reaxys 89 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Long-Evans rat pupBioassay : AL: allopregnanolone (3 mg/kg); BC: bicuculline; dose at which USV (ultrasonic vocalization) suppressed to 50 percent of vehicle control (ED50) 7-d old pups separated from mother; BT was 33 deg C; title comp. admin. alone (30 min before the test) or along with AL (10 min before test) or BC (35 min before the test); placed on 20 deg C grid surface for 2-min; USV recorded
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.00300000 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
ED50
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
47/181
2018-08-03 18:12:50
Unit
mg/kg
Quantitative value
0.08
Vivian, Jeffrey A.; Barros, Helena M. T.; Manitiu, Andre; Miczek, Klaus A.; Journal of Pharmacology and Experimental Therapeutics; vol. 282; nb. 1; (1997); p. 318 - 325, View in Reaxys 90 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : GABAA receptors, recombinant, on HEK 293 cellsBioassay : HEK: human embryonic kidney cells transfected with cDNAs for β1-, β3-, β2 subunits of GABAA receptors and their combinations; incubated in Tris-citrate buffer, 90 min, 4 deg C, with <3H>-labeled title comp.; non-specific binding in pres. GABA; scintillation count
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
20 nM
Qualitative Results
high affinity binding only to membranes from cells transfected with β1β3- and β1β3β2-subunits; diagram
Measurement Parameter
qualitative
Zezula; Slany; Sieghart; European Journal of Pharmacology; vol. 301; nb. 1-3; (1996); p. 207 - 214, View in Reaxys 91 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Bioassay : filtered, filters were subjected to scintillation counting cells were cultured and transfected with cDNAs encoding for β1, β3 or β2 subunits of GABAA receptors, membranes extracted, frozen membranes thawed, centrifuged, incubated in buffer with 3H-radiolabeled title comp. at 4 degC for 90 min
Biological Species/NCBI ID
human
Cells/Cell Lines
HEK293-EBNA cell line
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
high affinity binding sites observed in membranes from cells cotransfected with β1, β3, and β2 subunits while no binding sites were formed from cells transfected with these subunits
Measurement Parameter
qualitative
Slany; Zezula; Tretter; Sieghart; Molecular Pharmacology; vol. 48; nb. 3; (1995); p. 385 - 391, View in Reaxys 92 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionTarget : ICR miceBioassay : mouse weight 35-40 g
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
1-amino-5-bromouracil-induced anesthesia was potentiated by title compound
Measurement Parameter
qualitative
Miyazaki; Imaizumi; Machida; European Journal of Pharmacology; vol. 271; nb. 1; (1994); p. 179 - 184, View in Reaxys 93 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : radioligand bindingTarget : rat brains synaptosomal membraneBioassay : 300-350 g Wistar rats; 3H-muscimol radioligand used
Substance RN
606417View in Reaxys
Substance Name
31872
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
48/181
2018-08-03 18:12:50
Substance Dose
5 nM
Qualitative Results
Bmax2 3.5 pmol/mg protein
Measurement Parameter
qualitative
Miyazaki; Imaizumi; Machida; European Journal of Pharmacology; vol. 271; nb. 1; (1994); p. 179 - 184, View in Reaxys 94 of 403
Substance Effect
Myorelaxant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : measuring before (control, 100 percent) and 20 min after i.p. injection urethane-β-chloralose anesthetised rats (250-280 g); recording flexor reflex from tibial muscle evoked by 5 electrical shocks applied to the hindpaw and Hoffmann reflex from plantar foot muscles evoked by electrical stimulation of the tibial nerve
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
21 µmol/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
Hoffmann reflex: 49 percent; flexor reflex: 53 percent
Measurement Parameter
qualitative
Schwarz; Schmitt; Pergande; Block; European Journal of Pharmacology; vol. 276; nb. 3; (1995); p. 247 - 255, View in Reaxys 95 of 403
Substance Effect
Myorelaxant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : measuring before (control, 100 percent) and 10 min after i.t. injection; influence of coadministration of the specific GABAA receptor antagonist bicuculline methiodide (1 nmol) urethane-β-chloralose anesthetised rats (250-280 g); recording flexor reflex from tibial muscle evoked by 5 electrical shocks applied to the hindpaw and Hoffmann reflex from plantar foot muscles evoked by electrical stimulation of the tibial nerve
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intrathecal administration
Qualitative Results
Hoffmann reflex: 29 percent; flexor reflex:19 percent; abolishment of the effect of title comp. by coadmin. bicuculline methiodide
Measurement Parameter
qualitative
Schwarz; Schmitt; Pergande; Block; European Journal of Pharmacology; vol. 276; nb. 3; (1995); p. 247 - 255, View in Reaxys 96 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |secretion stimulant Bioassay : gastric acid secretion of perfused stomach in intact and vagotomized rats 12 rats (220-270 g) anesthetized with urethane; intact rat: vagus nerve separated from carotid arteries and cut at cervical level; vagotomized rat: distal end of left vagus nerve stimulated 120 min with Pt electrodes
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebroventricular administration
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
49/181
2018-08-03 18:12:50
Qualitative Results
title comp. evoked acid secretion in intact but not in vagotomized rats
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys 97 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionBioassay : gastric acid secretion of perfused stomach rat (220-270 g) anesthetized with urethane; title comp. administ. 30 min after bethanechol (BeCh, 1 mg/kg s.c.) or pentagastrin (Penta, 2 mg/kg s.c.), histamine (His, 10 mg/kg s.c.) or vagal stimulation
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.250000 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
title comp. dose dependently potentiated acid secretion induced by BeCh, Penta and direct vagal stimulation but not His
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys 98 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionBioassay : gastric acid secretion of perfused stomach rat (220-270 g) anesthetized with urethane; title comp. administ. 30 min after electrical vagal stimulation and proglumide (P, 800 mg/kg i.p.) injected stimultaneously with vagal stimulation
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
effect of title comp. potentiating acid secretion induced by direct vagal stimulation prevented by P
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys 99 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionBioassay : gastric acid secretion of perfused stomach rat (220-270 g) anesthetized with urethane; title comp. administ. 30 min after pentagastrin (Penta, 2 mg/kg) and atropine (A, 0.5 mg/kg s.c.) injected stimultaneously with Penta
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
effect of title comp. potentiating acid secretion induced by Penta not influenced by A
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
50/181
2018-08-03 18:12:50
100 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionnBioassay : gastric acid secretion of perfused stomach rat (220-270 g) anesthetized with urethane; title comp. administ. 30 min after bethanechol (BeCh, 1 mg/kg s.c.) and cimetidine (C, 2.5 mg/kg s.c.) or bicuculline methiodide (BCM, 1-10 mg/kg s.c.) injected stimultaneously with BeCh
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
effect of title comp. potentiating acid secretion induced by BeCh not influenced by C and dose dependently prevented by BCM
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys 101 of 403
Substance Effect
Mortality
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : mortalityBioassay : gastric acid secretion of perfused stomach in intact and vagotomized rats 36 rats (220-270 g) anesthetized with urethane; intact rat: vagus nerve separated from carotid arteries and cut at cervical level; vagotomized rat: distal end of left vagus nerve stimulated 120 min with Pt electrodes
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
title comp. did not stimulate acid secretion; 3/6 intact rats and 2/6 vagotomized rats died at 4 mg/kg
Measurement Parameter
qualitative
Lin; European Journal of Pharmacology; vol. 279; nb. 1; (1995); p. 43 - 50, View in Reaxys 102 of 403
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
51/181
2018-08-03 18:12:50
103 of 403
104 of 403
Substance Name
Muscimol
Substance Dose
1 nM
Measurement Parameter
IC50
Unit
M
Quantitative value
3.2E-09
Deviation
1.20000E-10
Measurement pX
8.49
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
P2 fraction: membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0 nM
Measurement Parameter
IC50
Unit
nM
Qualitative value
#
Quantitative value
90
Measurement pX
7.05
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
52/181
2018-08-03 18:12:50
105 of 403
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Mitochondria (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
10 µM
Measurement Parameter
inhibition rate
Unit
%
Measurement Object
of radioligand binding
Quantitative value
81
Measurement pX
5.63
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol; Lubrol-Wx
Concomitants: Compound role
NSB; RAD; VPR
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Mitochondria (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
10 µM
Measurement Parameter
stimulation percentage
Unit
%
Measurement Object
of radioligand binding
Quantitative value
222
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
53/181
2018-08-03 18:12:50
106 of 403
107 of 403
Measurement pX
6.28
Concomitants: Compound RN
754371; 1718733; 767925
Concomitants: Compound name
[3H]-Diazepam; Ethanol; Flurazepam; Lubrol-Wx
Concomitants: Compound role
RAD; AGO; NSB; VPR
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Mitochondria (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
10 ÂľM
Measurement Parameter
inhibition rate
Measurement Object
of radioligand binding
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
93499; 93499
Concomitants: Compound name
[3H]-alpha-dihydropicrotoxinin; alpha-Dihydropicrotoxinin; Lubrol-Wx
Concomitants: Compound role
RAD; NSB; VPR
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
54/181
2018-08-03 18:12:50
108 of 403
109 of 403
Cell Fraction
P2 fraction
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
100 ÂľM
Measurement Parameter
inhibition rate
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
93499
Concomitants: Compound name
[3H]-alpha-dihydropicrotoxinin
Concomitants: Compound role
RAD
Target Name
Ionotropic gamma aminobutyric acid receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid receptor
Target, Subunit, Species
Ionotropic gamma aminobutyric acid receptor [rat]
Target Mutant/Chimera Details
Ionotropic gamma aminobutyric acid receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Cell Fraction
Synaptosome: membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
6
Deviation
0.200000
Measurement pX
8.22
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
Ionotropic gamma aminobutyric acid receptor [mouse]
Target Synonyms
ionotropic gamma aminobutyric acid receptor
Target, Subunit, Species
Ionotropic gamma aminobutyric acid receptor [mouse]
Target Mutant/Chimera Details
Ionotropic gamma aminobutyric acid receptor [mouse]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
55/181
2018-08-03 18:12:50
110 of 403
Target Species (Bioactivity)
mouse
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
C57BL 6 mouse
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
IC50
Unit
ÂľM
Measurement Object
assay in cell in culture
Quantitative value
0.005
Measurement pX
8.3
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p63138 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
EC50
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
56/181
2018-08-03 18:12:50
111 of 403
112 of 403
Unit
ÂľM
Quantitative value
7.1
Deviation
1
Measurement pX
5.15
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p63138 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.32
Deviation
0.220000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,86,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
57/181
2018-08-03 18:12:50
113 of 403
114 of 403
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
19.9
Deviation
3.80000
Statistical sgnificance (pvalue)
0.01
Measurement pX
4.7
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,86,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.21
Deviation
0.0600000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,86,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
58/181
2018-08-03 18:12:50
115 of 403
116 of 403
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
48.9
Deviation
0.600000
Statistical sgnificance (pvalue)
0.01
Measurement pX
4.31
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,86,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.2
Deviation
0.400000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
59/181
2018-08-03 18:12:50
117 of 403
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
4.7
Deviation
0.300000
Measurement pX
5.33
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
60/181
2018-08-03 18:12:50
118 of 403
119 of 403
Substance Dose
0.000100000 mM
Measurement Parameter
nH (Hill coefficient)
Quantitative value
0.91
Deviation
0.160000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
5.7
Deviation
1.80000
Measurement pX
5.24
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
61/181
2018-08-03 18:12:50
120 of 403
121 of 403
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 mM
Measurement Parameter
nH (Hill coefficient)
Quantitative value
0.92
Deviation
0.0200000
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric-acid A receptor, alpha subunit [rat]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gamma-aminobutyric-acid a receptor, alpha subunit
Target Uniprot ID
p18508 + p63138
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]; Gamma-aminobutyric-acid A receptor, alpha subunit [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric-acid A receptor, alpha subunit [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
tsA201 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 ÂľM
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
16.7
Deviation
1.20000
Measurement pX
7.78
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
62/181
2018-08-03 18:12:50
122 of 403
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,86,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
tsA201 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 ÂľM
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
47.1
Deviation
14.8000
Statistical sgnificance (pvalue)
0.05
Measurement pX
7.33
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
tsA201 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
63/181
2018-08-03 18:12:50
123 of 403
124 of 403
Substance Dose
0.000100000 µM
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
7.8
Deviation
1.30000
Measurement pX
8.11
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,98,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
tsA201 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.000100000 µM
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
20.2
Deviation
2.40000
Measurement pX
7.69
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
64/181
2018-08-03 18:12:50
125 of 403
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
9.6
Deviation
1.50000
Measurement pX
8.02
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
65/181
2018-08-03 18:12:50
126 of 403
127 of 403
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
8.2
Deviation
1.70000
Measurement pX
8.09
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.17
Deviation
0.150000
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
66/181
2018-08-03 18:12:50
128 of 403
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.12
Deviation
0.330000
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2
Target Uniprot ID
p28472 + p18507 + p47869
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
15
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
67/181
2018-08-03 18:12:50
129 of 403
130 of 403
Deviation
1.50000
Measurement pX
7.82
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2
Target Uniprot ID
p28472 + p18507 + p47869
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
2.2
Deviation
1.70000
Measurement pX
8.66
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho (rho 3)
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
68/181
2018-08-03 18:12:50
131 of 403
132 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
1.9
Deviation
0.100000
Measurement pX
5.72
Target Name
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho (rho 3)
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.5
Deviation
0.100000
Target Name
Gamma-aminobutyric acid receptor subunit rho-1 [human]
Target Synonyms
gaba(a) receptor subunit rho-1; gaba(c) receptor; gabrr1; gamma-aminobutyric acid receptor subunit rho-1
Target Uniprot ID
p24046
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit rho-1 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit rho-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
HEK293 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
69/181
2018-08-03 18:12:50
133 of 403
134 of 403
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Qualitative value
>
Quantitative value
10000
Measurement pX
1
Concomitants: Compound RN
3619281; 8327357
Concomitants: Compound name
[3H]-EBOB; 4'-Cyano-4-sec-butyl-bicycloorthobenzoate
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho (rho 3)
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho (Rho 3) [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IA (intrinsic activity)
Unit
%
Quantitative value
88
Target Name
Gamma-aminobutyric acid receptor subunit beta-1 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-1; gabrb1; gamma-aminobutyric acid receptor subunit beta-1 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18505 + p18507 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-1 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
70/181
2018-08-03 18:12:50
135 of 403
136 of 403
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.17
Deviation
0.160000
Measurement pX
8.17
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18507 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.08
Deviation
0.0790000
Measurement pX
8.08
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
71/181
2018-08-03 18:12:50
137 of 403
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.34
Deviation
0.0590000
Measurement pX
8.34
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2
Target Uniprot ID
p28472 + p18507 + p47869
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
72/181
2018-08-03 18:12:50
138 of 403
139 of 403
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.05
Deviation
0.140000
Measurement pX
8.05
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-3 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-3; gabra3; gamma-aminobutyric acid receptor subunit alpha-3
Target Uniprot ID
p28472 + p18507 + p34903
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-3 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.24
Deviation
0.140000
Measurement pX
8.24
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-5 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
73/181
2018-08-03 18:12:50
140 of 403
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-5; gabra5; gamma-aminobutyric acid receptor subunit alpha-5 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + p31644 + p18507
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-5 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.54
Deviation
0.0870000
Measurement pX
8.54
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-6 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-6; gabra6; gamma-aminobutyric acid receptor subunit alpha-6 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + q16445 + p18507
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-6 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
LTK- cell line
Cell Fraction
Membrane
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
74/181
2018-08-03 18:12:50
141 of 403
142 of 403
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pKi
Quantitative value
8.27
Deviation
0.150000
Measurement pX
8.27
Concomitants: Compound RN
906818; 774694
Concomitants: Compound name
GABA; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
Gamma-aminobutyric acid receptor subunit beta-1 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-1; gabrb1; gamma-aminobutyric acid receptor subunit beta-1 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18505 + p18507 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-1 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
5.15
Deviation
0.120000
Measurement pX
5.15
Target Name
Gamma-aminobutyric acid receptor subunit beta-1 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-1; gabrb1; gamma-aminobutyric acid receptor subunit beta-1 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18505 + p18507 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-1 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
75/181
2018-08-03 18:12:50
143 of 403
144 of 403
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
99
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18507 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
5.3
Deviation
0.130000
Measurement pX
5.3
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
76/181
2018-08-03 18:12:50
145 of 403
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18507 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
97
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
77/181
2018-08-03 18:12:50
146 of 403
147 of 403
Quantitative value
5.4
Deviation
0.0730000
Measurement pX
5.4
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p28472 + p18507 + p14867
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
97
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2
Target Uniprot ID
p28472 + p18507 + p47869
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
78/181
2018-08-03 18:12:50
148 of 403
149 of 403
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
6.04
Deviation
0.0560000
Measurement pX
6.04
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2
Target Uniprot ID
p28472 + p18507 + p47869
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
96
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-3 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-3; gabra3; gamma-aminobutyric acid receptor subunit alpha-3
Target Uniprot ID
p28472 + p18507 + p34903
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-3 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
Target Species (Bioactivity)
human
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
79/181
2018-08-03 18:12:50
150 of 403
151 of 403
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
5.05
Deviation
0.0970000
Measurement pX
5.05
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-3 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-3; gabra3; gamma-aminobutyric acid receptor subunit alpha-3
Target Uniprot ID
p28472 + p18507 + p34903
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-3 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
98
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-5 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-5; gabra5; gamma-aminobutyric acid receptor subunit alpha-5 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + p31644 + p18507
Target PDB ID
4cof
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
80/181
2018-08-03 18:12:50
152 of 403
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-5 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
5.7
Deviation
0.0480000
Measurement pX
5.7
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-5 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-5; gabra5; gamma-aminobutyric acid receptor subunit alpha-5 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + p31644 + p18507
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-5 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
98
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
81/181
2018-08-03 18:12:50
153 of 403
154 of 403
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-6 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-6; gabra6; gamma-aminobutyric acid receptor subunit alpha-6 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + q16445 + p18507
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-6 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
pEC50
Quantitative value
5.79
Deviation
0.0480000
Measurement pX
5.79
Target Name
Gamma-aminobutyric acid receptor subunit beta-3 [human];+Gamma-aminobutyric acid receptor subunit alpha-6 [human];+Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit alpha-6; gabra6; gamma-aminobutyric acid receptor subunit alpha-6 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target Uniprot ID
p28472 + q16445 + p18507
Target PDB ID
4cof
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-6 [human]; Gamma-aminobutyric acid receptor subunit beta-3 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
82/181
2018-08-03 18:12:50
155 of 403
156 of 403
Substance Name
Muscimol
Substance Dose
1.00000E-10 M
Measurement Parameter
Emax
Unit
%
Quantitative value
101
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
forebrain
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1.00000E-07 M
Measurement Parameter
Slope
Quantitative value
0.92
Concomitants: Compound RN
754371; 754371
Concomitants: Compound name
Diazepam; [3H]-Diazepam
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
forebrain
Cells/Cell Lines
cells
Cell Fraction
Membrane
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
83/181
2018-08-03 18:12:50
157 of 403
158 of 403
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1.00000E-07 M
Measurement Parameter
EC50
Unit
ÂľM
Measurement Object
enhancement of radioligand binding
Quantitative value
0.6
Measurement pX
6.22
Concomitants: Compound RN
754371; 754371
Concomitants: Compound name
Diazepam; [3H]-Diazepam
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
28
Measurement pX
7.55
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
84/181
2018-08-03 18:12:50
159 of 403
160 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.3
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
16
Measurement pX
7.8
Concomitants: Compound RN
606417; 774694
Concomitants: Compound name
Muscimol; [3H]-Muscimol
Concomitants: Compound role
NSB; RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : spatial working memory Species : Wistar ratdelayed spatial-win shift (SWSh) task performance in eight-arm radial arm maze; running time per choice determined; control value: 9.8
Biological Species/NCBI ID
rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
85/181
2018-08-03 18:12:50
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Saito, Shunsuke; Okada, Akiko; Ouwa, Takako; Kato, Akane; Akagi, Masaaki; Kamei, Chiaki; Biological and Pharmaceutical Bulletin; vol. 33; nb. 3; (2010); p. 439 - 443, View in Reaxys 161 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : spatial working memory Target : rat β-aminobutyric acidA receptor Species : Wistar ratdelayed spatial-win shift (SWSh) task performance in eight-arm radial arm maze; no effect at 0.3 and 1 nmol/side doses; control value: number of correct choices = 3.7, across-phase errors = 0.5, within-phase errors = 0
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
number of across-phase errors 1.5
Measurement Parameter
qualitative
Saito, Shunsuke; Okada, Akiko; Ouwa, Takako; Kato, Akane; Akagi, Masaaki; Kamei, Chiaki; Biological and Pharmaceutical Bulletin; vol. 33; nb. 3; (2010); p. 439 - 443, View in Reaxys 162 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : Drosophila simulansBioassay : mutant strain, containing Gly instead of Ala302 in the Rdl unit of the GABA receptor subunit, mortality detd. in 5 percent sucrose water
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1000 ppm
Qualitative Results
percentage mortality 39 percent
Measurement Parameter
qualitative
Quantitative value
39
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 163 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : Drosophila simulansBioassay : mutant strain, containing Ser instead of Ala302 in the Rdl unit of the GABA receptor subunit, mortality detd. in 5 percent sucrose water
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1000 ppm
Qualitative Results
percentage mortality 39 percent
Measurement Parameter
qualitative
Quantitative value
39
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 164 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : Drosophila simulansBioassay : normal strain, mortality detd. in 5 percent sucrose water
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
86/181
2018-08-03 18:12:50
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1000 ppm
Qualitative Results
percentage mortality 34 percent
Measurement Parameter
qualitative
Quantitative value
34
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 165 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor blocking agent Bioassay : normal and mutant strains, the mutants contain in the Rdl GABA subunit Ser instead of Ala302, flies frozen, heads recovered, homogenized in buffer, centrifuged, membrane prepared, treated with <3H>EBOB and title comp., binding detd.
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title comp. at 30 μM inhibited the specific binding in the normal strain, the mutants were significantly less sensitive
Measurement Parameter
qualitative
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 166 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor blocking agent Target : Drosophila simulansBioassay : normal and mutant strains, the mutants contain in the Rdl GABA subunit Ser or Gly instead of Ala302, flies frozen, heads recovered, homogenized in buffer, centrifuged, membrane prepared, treated with <3H>EBOB and title comp., binding detd.
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title comp. at 30 μM inhibited the specific binding in the normal strain, the Ser-mutants were significantly less sensitive
Measurement Parameter
qualitative
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 167 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : mutant strain, containing Ser instead of Ala302 in the Rdl unit of the GABA receptor subunit, mortality detd. in 5 percent sucrose water
Biological Species/NCBI ID
Drosophila
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1000 ppm
Qualitative Results
percentage mortality 27 percent
Measurement Parameter
qualitative
Quantitative value
27
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 168 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : normal strain, mortality detd. in 5 percent sucrose water
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
87/181
2018-08-03 18:12:50
Biological Species/NCBI ID
Drosophila
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1000 ppm
Qualitative Results
percentage mortality 22 percent
Measurement Parameter
qualitative
Quantitative value
22
Cole, Loretta M.; Roush, Richard T.; Casida, John E.; Life Sciences; vol. 56; nb. 10; (1995); p. 757 - 765, View in Reaxys 169 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |agonist Target : rat hippocampal CA1 neuronsBioassay : Wistar rats, 100-200 g b. wt.; brain removed, placed in cold artificial cerebrospinal fluid, hippocampus dissected, slices incubated 90 min, stimulus 0.1 Hz; paired-pulse facilitation (PPF) of field population spikes (PS) measurement
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2.00000E-05 M
Qualitative Results
test comp. decreased PS amplitude, increased PPF
Measurement Parameter
qualitative
Hirota; Roth; Fujimura; Masuda; Ito; Toxicology Letters; vol. 100-101; (1998); p. 203 - 207, View in Reaxys 170 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |releasing hormones Target : synaptosomes of human neocortexBioassay : synaptosomes freshly isolated by ultracentrifugation from various brain cortex samples of patients undergoing neurosurgery; title compound is a GABAA-receptor agonist synaptosomal suspensions in superfusion chambers; depolarized by 15 mM KCl in physiological solution for 90 s at 37 deg C, then exposed to title comp.; collecting fractions, radioimmunoassay of somatostatin-like immunoreactivity (<125I>-tracer)
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
100 µM
Qualitative Results
no inhibition of hormone release evoked by KCl
Measurement Parameter
qualitative
Bonanno, Giambattista; Gemignani, Anita; Schmid, Giovanna; Severi, Paolo; Cavazzani, Paolo; Raiteri, Maurizio; British Journal of Pharmacology; vol. 118; nb. 6; (1996); p. 1441 - 1446, View in Reaxys 171 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |releasing hormones Target : synaptosomes of human neocortexBioassay : synaptosomes freshly isolated by ultracentrifugation from various brain cortex samples of patients undergoing neurosurgery; title compound is a GABAA-receptor agonist synaptosomal suspensions superfused by physiological solution at 37 deg C in presence of title comp.; radioimmunoassay of somatostatin-like immunoreactivity in fractions of superfusate
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
100 µM
Qualitative Results
no effect on basal release of somatostatin
Measurement Parameter
qualitative
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
88/181
2018-08-03 18:12:50
Bonanno, Giambattista; Gemignani, Anita; Schmid, Giovanna; Severi, Paolo; Cavazzani, Paolo; Raiteri, Maurizio; British Journal of Pharmacology; vol. 118; nb. 6; (1996); p. 1441 - 1446, View in Reaxys 172 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : tolerance to hypothermia; influence onTarget : Sprague-Dawley ALAB/S-D ratBioassay : control - saline; area under curve (AUC 0-120 min) calculated; 8-OH-DPAT - 8-hydroxy-2-(di-npropylamino)tetralin hydrobromide rats 220-300 g weight housed 5 per cage; 12 h light/dark cycle, 20 deg C; free access to food and water; rectal temperature det. before and 30, 60, 90, 120 min after last 8-OH-DPAT treatment
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
3 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. couteracted tolerance to hypothermic effect: AUC was 154 deg C for title comp. + 8OH-DPAT vs. 53 deg C for saline control
Measurement Parameter
qualitative
Kelder, Diana; Ross, Svante B.; Pharmacology and Toxicology; vol. 90; nb. 1; (2002); p. 14 - 19, View in Reaxys 173 of 403
Substance Effect
Myocontractant
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : stimulation: 1 Hz, 1 ms, 300 mA for 10 s at 10 min interval; isometric force measurements; PSS: physiological salt solution, gassed with 95 percent O2/5 percent CO2; further investigations using tetrodotoxin or bicuculline longitudinal muscle strips; intact myenteric plexus; PSS at 37 deg C; histamine (1 μmol/l) induced preconstriction; electric field stimulation; 20-min addition of title comp.; effect of title comp. on stimulation-evoked relaxation
Biological Species/NCBI ID
guinea pig
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 µM
Qualitative Results
title comp. inhibited stimulation-evoked relaxation to 67 percent; tetrodotoxin enhanced and bicuculline suppressed effect of title comp. (figure)
Measurement Parameter
qualitative
Kilbinger; Ginap; Erbelding; Naunyn-Schmiedeberg's Archives of Pharmacology; vol. 359; nb. 6; (1999); p. 500 - 504, View in Reaxys 174 of 403
Substance Effect
Neuroregulatoric
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : cat isolated superior sagittal sinusBioassay : L-glutamate given via microiontophoresis primary trigeminal afferents supramaximally stimulated with stimulus-isolated square wave pulses (20-28 V, 250 μs, 0.1-10 Hz) after neuromuscular blockade; extracellular recordings made using microiontopheric combination electrode
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title comp. reversibly inhibited cell firing evoked by L-glutamate
Measurement Parameter
qualitative
Storer; Akerman; Goadsby; British Journal of Pharmacology; vol. 134; nb. 4; (2001); p. 896 - 904, View in Reaxys 175 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
89/181
2018-08-03 18:12:50
Bioassay Details
Effect : inward current agonistTarget : RDL receptor RDL subunit cDNA subcloned into pRmHa3RDL into oocyte expression vector pGEMHE ;RDL receptorRDL: resistance to dieldrin
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
nH Hill coefficient 2.2
Measurement Parameter
qualitative
McGonigle, Ian; Lummis, Sarah C. R.; Biochemistry; vol. 49; nb. 13; (2010); p. 2897 - 2902, View in Reaxys 176 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Bioassay Details
Effect : inward current agonistTarget : RDL receptor RDL subunit cDNA subcloned into pRmHa3RDL into oocyte expression vector pGEMHE ;RDL receptorRDL: resistance to dieldrin
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
EC50
Unit
µM
Quantitative value
9.04
Measurement pX
5.04
McGonigle, Ian; Lummis, Sarah C. R.; Biochemistry; vol. 49; nb. 13; (2010); p. 2897 - 2902, View in Reaxys 177 of 403
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound RN
906818; 906818
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
90/181
2018-08-03 18:12:50
178 of 403
179 of 403
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
0.0100000 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
86
Deviation
3
Measurement pX
8.79
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cell Fraction
Synaptosome: membrane (P2 fraction)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
91/181
2018-08-03 18:12:50
180 of 403
181 of 403
Substance RN
606417View in Reaxys
Substance Name
muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.005
Measurement pX
8.3
Concomitants: Compound RN
9997090
Concomitants: Compound name
[3H]-THIP
Concomitants: Compound role
RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
92/181
2018-08-03 18:12:50
182 of 403
183 of 403
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound RN
8138400
Concomitants: Compound name
[3H]-P4S
Concomitants: Compound role
RAD
Target Name
GAT [rat]
Target Synonyms
gat
Target, Subunit, Species
GAT [rat]
Target Mutant/Chimera Details
GAT [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
320
Measurement pX
3.49
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
SUB
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
93/181
2018-08-03 18:12:50
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
4
Measurement Parameter
IC50
Unit
nM
Quantitative value
2
Measurement pX
8.7
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Melikian; Schlewer; Chambon; Wermuth; Journal of Medicinal Chemistry; vol. 35; nb. 22; (1992); p. 4092 - 4097, View in Reaxys 184 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cells/Cell Lines
nerve cell
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
4
Measurement Parameter
IC50
Unit
nM
Quantitative value
135
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
94/181
2018-08-03 18:12:50
Measurement pX
6.87
Concomitants: Compound RN
8365396; 8365396
Concomitants: Compound name
Gabazine; [3H]-Gabazine
Concomitants: Compound role
NSB; RAD
Melikian; Schlewer; Chambon; Wermuth; Journal of Medicinal Chemistry; vol. 35; nb. 22; (1992); p. 4092 - 4097, View in Reaxys 185 of 403
186 of 403
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18507 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
Sf9 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
11
Deviation
4.50000
Measurement pX
7.96
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18507 + p47870
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit gamma-2 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated:Substitution,1,Isoleucine,121,Valine
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
95/181
2018-08-03 18:12:50
187 of 403
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
Sf9 cell line
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
340
Deviation
47
Measurement pX
6.47
Concomitants: Compound RN
8365396; 906818
Concomitants: Compound name
[3H]-Gabazine; GABA
Concomitants: Compound role
RAD; NSB
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
0.5
Haefliger; Revesz; Maurer; et al.; European Journal of Medicinal Chemistry; vol. 19; nb. 2; (1984); p. 149 - 156, View in Reaxys 188 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Lethality
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
Protection against arthritis
Quantitative value
4.8
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
96/181
2018-08-03 18:12:50
Haefliger; Revesz; Maurer; et al.; European Journal of Medicinal Chemistry; vol. 19; nb. 2; (1984); p. 149 - 156, View in Reaxys 189 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Oncins France 1 mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intracerebroventricular administration
Substance Dosing Regimen
Single
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Dose which prolonged the time to the occurence of clonic convulsions by 50%
Quantitative value
0.29
Concomitants: Compound RN
773807
Concomitants: Compound name
3-Mercaptopropionic acid
Concomitants: Compound role
IAV
Haefliger; Revesz; Maurer; et al.; European Journal of Medicinal Chemistry; vol. 19; nb. 2; (1984); p. 149 - 156, View in Reaxys 190 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Oncins France 1 mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Dose which prolonged the time to the occurence of clonic convulsions by 50%
Quantitative value
0.75
Concomitants: Compound name
Bicuculline
Concomitants: Compound role
IAV
Haefliger; Revesz; Maurer; et al.; European Journal of Medicinal Chemistry; vol. 19; nb. 2; (1984); p. 149 - 156, View in Reaxys 191 of 403
Target Name
GABA receptor [human]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [human]
Target Mutant/Chimera Details
GABA receptor [human]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
97/181
2018-08-03 18:12:50
192 of 403
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
human
Organs/Tissues
cerebellum cortex
Cells/Cell Lines
nerve cell
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
2
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.02
Measurement pX
7.7
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain cortex
Cells/Cell Lines
nerve cell
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.024
Deviation
0.00300000
Measurement pX
7.62
Concomitants: Compound RN
906818; 906818
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
98/181
2018-08-03 18:12:50
193 of 403
194 of 403
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain cortex
Cells/Cell Lines
nerve cell
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
100 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
103
Deviation
4
Measurement pX
5.28
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
GAT [rat]
Target Synonyms
gat
Target, Subunit, Species
GAT [rat]
Target Mutant/Chimera Details
GAT [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
Wistar rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
99/181
2018-08-03 18:12:50
195 of 403
196 of 403
Organs/Tissues
brain cortex
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
0.500000 mM
Measurement Parameter
inhibition rate
Unit
%
Qualitative value
<
Quantitative value
5
Measurement pX
1
Concomitants: Compound RN
8319427
Concomitants: Compound name
[3H]-L-glutamate
Concomitants: Compound role
SUB
Target Name
ionotropic gamma aminobutyric acid a receptor [guinea pig]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [guinea pig]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [guinea pig]:Wild
Target Species (Bioactivity)
guinea pig
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Organ contraction
Biological Species/NCBI ID
guinea pig
Organs/Tissues
ileum
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
0.99
Measurement pX
6
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
100/181
2018-08-03 18:12:50
197 of 403
198 of 403
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
14.3
Deviation
3.20000
Measurement pX
4.84
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.42
Deviation
0.0900000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,181,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
101/181
2018-08-03 18:12:50
Biological Species/NCBI ID
199 of 403
200 of 403
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
2570
Deviation
467
Measurement pX
2.59
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Tyrosine,181,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.25
Deviation
0.0900000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Threonine,184,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
102/181
2018-08-03 18:12:50
201 of 403
202 of 403
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
145.7
Deviation
33.1000
Measurement pX
3.84
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,1,Threonine,184,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.59
Deviation
0.0200000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
103/181
2018-08-03 18:12:50
203 of 403
204 of 403
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,2,Threonine,226,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
536.3
Deviation
169
Measurement pX
3.27
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,2,Threonine,226,Serine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.21
Deviation
0.170000
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
104/181
2018-08-03 18:12:50
+ gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
205 of 403
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,2,Tyrosine,229,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
ÂľM
Quantitative value
296.6
Deviation
78.9000
Measurement pX
3.53
Target Name
Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit gamma-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18508 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit gamma-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Mutated:Substitution,2,Tyrosine,229,Phenylalanine + Gamma-aminobutyric acid receptor subunit gamma-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.37
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
105/181
2018-08-03 18:12:50
206 of 403
207 of 403
Deviation
0.350000
Target Name
Ionotropic gamma aminobutyric acid receptor [cat]
Target Synonyms
ionotropic gamma aminobutyric acid receptor
Target, Subunit, Species
Ionotropic gamma aminobutyric acid receptor [cat]
Target Mutant/Chimera Details
Ionotropic gamma aminobutyric acid receptor [cat]:Wild
Target Species (Bioactivity)
cat
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
cat
Organs/Tissues
spinal ganglion
Cells/Cell Lines
nerve cell
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1 mM
Measurement Parameter
Emax
Unit
%
Quantitative value
141
Deviation
9
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
26
Measurement pX
7.59
Concomitants: Compound RN
774694
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
106/181
2018-08-03 18:12:50
208 of 403
209 of 403
Concomitants: Compound name
[3H]-Muscimol
Concomitants: Compound role
RAD
Target Name
GABA-A receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor
Target, Subunit, Species
GABA-A receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
nM
Quantitative value
28
Measurement pX
7.55
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : Nrf2 activity; inhibition ofTarget : lung adenocarcinoma cells transfected with ARE-luciferase reporter vectorBioassay : Example 2 A Novel Assay for Nrf2 Inhibitors A high throughput approach to screen compounds was developed. A cell based reporter assay was used to identify agents that can inhibit Nrf2 mediated transcription. Lung adenocarcinoma cells that are stably transfected with ARE-luciferase reporter vector were
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title compound treatment showed inhibited luciferase activity of 50%
Measurement Parameter
qualitative
Patent; BISWAL, Shyam; SINGH, Anju; MALHOTRA, Deepti; WO2008/124660; (A2); (2008), View in Reaxys 210 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |antagonist Bioassay : recording of orthodromic extracellular field potentials were made from CA1 pyramidal cell layer following stimulation of Schaffer collateral fibres in stratum radiatum; size of population spikes by title comp. applied for 10 minutes were measured rat (170-200 g) anaesthetised and decapitated, brains were taken out, put in ice-gold artifical cerebrospinal fluid; hippocampi were cut transversely into 450 μm thick slices, kept in incubation chamber; long-term depression (LTD)
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 µM
Qualitative Results
title comp. induced a time and concentration-dependent LTD at a frequency of stimulation of 0.01 Hz or in the absence of stimulation; max. effect of title comp. was at 10 μM produces LTD no reversed by washing, but LTD reversed by stimulation at
Measurement Parameter
qualitative
Akhondzadeh; Stone; Life Sciences; vol. 58; nb. 13; (1996); p. 1023 - 1030, View in Reaxys 211 of 403
Target Name
Gamma-aminobutyric acid receptor subunit beta-1
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
107/181
2018-08-03 18:12:50
212 of 403
Target Synonyms
gaba(a) receptor subunit beta-1; gabrb-1; gabrb1; gamma-aminobutyric acid receptor subunit beta-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit beta-1
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-1:Wild
Target Transfection
Non Transfected
Substance Effect
Anti-Prion
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : PrPres formationTarget : RML prion strain PrPres: partially protease-resistant abnormal isoform of prion protein
Biological Species/NCBI ID
mouse
Cells/Cell Lines
Neuro-2a cell line
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Substance Effect
Anticonvulsant
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : AT: area tempestas; controls received bilateral microinfusions of 0.9 percent saline into AT; anticonvulsant effects determined as prolonged latency from injection of soman to onset of seizures/convulsions or prevention of seizures rats implanted sterotaxically with guide cannulas aimed at AT in both hemispheres; title comp. infused bilaterally into AT 20 min before soman exposure (100 μg/kg, s.c.); rats observed for first 1-2 h and 10 min at 24 h thereafter; EEG
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
infusion of title comp. appeared to yeild anticonvulsant impact; median latency to seizure/non seizure: 33 min (AT); control values: 5 min (AT); table
Measurement Parameter
qualitative
Myhrer, Trond; Nguyen, Nga H. T.; Enger, Siri; Aas, Pal; Archives of Toxicology; vol. 80; nb. 8; (2006); p. 502 - 507, View in Reaxys 213 of 403
Substance Effect
Anticonvulsant
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : SN: substantia nigra; controls received bilateral microinfusions of 0.9 percent saline into SN; anticonvulsant effects determined as prolonged latency from injection of soman to onset of seizures/convulsions or prevention of seizures rats implanted sterotaxically with guide cannulas aimed at SN in both hemispheres; title comp. infused bilaterally into SN 20 min before soman exposure (100 μg/kg, s.c.); rats observed for first 1-2 h and 10 min at 24 h thereafter; EEG
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
infusion of title comp. appeared to yeild anticonvulsant impact; median latency to seizure/non seizure: 6 min; control values: 4.6 min; table
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
108/181
2018-08-03 18:12:50
Measurement Parameter
qualitative
Myhrer, Trond; Nguyen, Nga H. T.; Enger, Siri; Aas, Pal; Archives of Toxicology; vol. 80; nb. 8; (2006); p. 502 - 507, View in Reaxys 214 of 403
215 of 403
Target Name
Gamma hydroxybutyric acid receptor [rat]
Target Synonyms
gamma hydroxybutyric acid receptor
Target, Subunit, Species
Gamma hydroxybutyric acid receptor [rat]
Target Mutant/Chimera Details
Gamma hydroxybutyric acid receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain cortex
Cells/Cell Lines
cells
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
10 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
4.1
Deviation
1.50000
Measurement pX
1
Concomitants: Compound RN
24175947; 24175947
Concomitants: Compound name
NCS-382; [3H]-NCS-382
Concomitants: Compound role
NSB; RAD
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
109/181
2018-08-03 18:12:50
216 of 403
217 of 403
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
µM
Quantitative value
27
Deviation
8
Measurement pX
4.57
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
nH (Hill coefficient)
Quantitative value
1.1
Target Name
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho [bovine]:Wild
Target Species (Bioactivity)
bovine
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
EC50
Unit
µM
Quantitative value
2.3
Deviation
0.300000
Measurement pX
5.64
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
110/181
2018-08-03 18:12:50
218 of 403
219 of 403
Concomitants: Compound name
Bicuculline
Concomitants: Compound role
COM
Target Name
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho [bovine]:Wild
Target Species (Bioactivity)
bovine
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Emax
Unit
%
Quantitative value
73
Deviation
4
Concomitants: Compound name
Bicuculline
Concomitants: Compound role
COM
Target Name
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Synonyms
gamma-aminobutyric-acid a receptor, rho
Target, Subunit, Species
Gamma-aminobutyric-acid A receptor, Rho [bovine]
Target Mutant/Chimera Details
Gamma-aminobutyric-acid A receptor, Rho [bovine]:Wild
Target Species (Bioactivity)
bovine
Substance Action on Target
Antagonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Biological Species/NCBI ID
Xenopus laevis
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
100 ÂľM
Measurement Parameter
inhibition rate
Unit
%
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
111/181
2018-08-03 18:12:50
220 of 403
Quantitative value
20 - 25
Measurement pX
1
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; GABA; Bicuculline
Concomitants: Compound role
AGO; AGO; COM
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
7
Measurement Parameter
IC50
Unit
ÂľM
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Falch; Hedegaard; Nielsen; Jensen; Hjeds; Krogsgaard-Larsen; Journal of Neurochemistry; vol. 47; nb. 3; (1986); p. 898 903, View in Reaxys 221 of 403
Target Name
Gamma aminobutyric acid B receptor [rat]
Target Synonyms
gamma aminobutyric acid b receptor
Target, Subunit, Species
Gamma aminobutyric acid B receptor [rat]
Target Mutant/Chimera Details
Gamma aminobutyric acid B receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
112/181
2018-08-03 18:12:50
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
7
Measurement Parameter
IC50
Unit
µM
Quantitative value
2.4
Measurement pX
5.62
Concomitants: Compound RN
386127; 2104494; 906818
Concomitants: Compound name
Isoguvacine; Baclofen; [3H]-GABA
Concomitants: Compound role
COM; NSB; RAD
Falch; Hedegaard; Nielsen; Jensen; Hjeds; Krogsgaard-Larsen; Journal of Neurochemistry; vol. 47; nb. 3; (1986); p. 898 903, View in Reaxys 222 of 403
Bioassay Category
Metabolism/Transport
Bioassay Name
Flux uptake
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
7
Measurement Parameter
IC50
Unit
µM
Quantitative value
240
Measurement pX
3.62
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
SUB
Falch; Hedegaard; Nielsen; Jensen; Hjeds; Krogsgaard-Larsen; Journal of Neurochemistry; vol. 47; nb. 3; (1986); p. 898 903, View in Reaxys 223 of 403
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
113/181
2018-08-03 18:12:50
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.01
Measurement pX
8
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 224 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Swiss Webster mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
0.7
Concomitants: Compound RN
773807
Concomitants: Compound name
3-Mercaptopropionic acid
Concomitants: Compound role
IAV
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 225 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Brain biochemistry : Others
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
> 5 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
concentration (parameters)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
114/181
2018-08-03 18:12:50
Measurement Object
cGMP
Qualitative value
NA
Measurement pX
1
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 226 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
2 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
percentage
Unit
%
Measurement Object
cGMP level
Quantitative value
30
Statistical sgnificance (pvalue)
0.05
Concomitants: Compound RN
119374; 29319
Concomitants: Compound name
Isoniazid; (-)-Apomorphine
Concomitants: Compound role
IAV; IAV
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 227 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
> 5 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
percentage
Measurement Object
cGMP level
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
119374; 29319
Concomitants: Compound name
Isoniazid; (-)-Apomorphine
Concomitants: Compound role
IAV; IAV
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
115/181
2018-08-03 18:12:50
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 228 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.50000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
percentage
Unit
%
Measurement Object
cGMP level
Quantitative value
50
Statistical sgnificance (pvalue)
0.05
Concomitants: Compound RN
119374
Concomitants: Compound name
Isoniazid
Concomitants: Compound role
IAV
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 229 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.50000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
percentage
Unit
%
Measurement Object
cGMP level
Quantitative value
100
Concomitants: Compound RN
29319
Concomitants: Compound name
(-)-Apomorphine
Concomitants: Compound role
IAV
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 230 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Brain biochemistry : Others
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
116/181
2018-08-03 18:12:50
Biological Species/NCBI ID
Sprague Dawley rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
1.50000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
percentage
Unit
%
Measurement Object
cGMP level
Quantitative value
85
Leader; Koe; Weissman; Journal of clinical pharmacology; vol. 21; nb. 8-9 Suppl; (1981); p. 262S-270S, View in Reaxys 231 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : cocaine self-administration; effect onBioassay : The effect of muscimol and CP-154,526 on intravenous self-administration of cocaine: These experiments were designed to determine the effects of a combination of CP-154,526 and muscimol on intravenous cocaine self-administration in rats responding under a multiple, alternating schedule of food reinforcement
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
title compound had no significant effect at low doses (0.5-2.0 mg/kg) but reduced cocaine self-administration at high doses (1-4 mg/kg) produced ~18-35% cocaine infusions (% baseline); figures are given
Measurement Parameter
qualitative
Patent; BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY and AGRICULTURAL and MECHANICAL COLLEGE; WO2007/56618; (2007); (A1) English, View in Reaxys 232 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : Nrf2 activity; inhibition of Bioassay : lung adenocarcinoma cells transfected with AREluciferase reporter vectorExample 2 A Novel Assay for Nrf2 Inhibitors A high throughput approach to screen compounds was developed. A cell based reporter assay was used to identify agents that can inhibit Nrf2 mediated transcription. Lung adenocarcinoma cells that are stably transfected with ARE-luciferase reporter vector were
Cells/Cell Lines
cells
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title compound treatment showed inhibited luciferase activity of 50%
Measurement Parameter
qualitative
Patent; THE UNIVERSITY OF MONTANA; WO2008/24660; (2008); (A2) English, View in Reaxys 233 of 403
Substance Effect
Toxic
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Name
Cell/tumor cell: proliferation/viability/growth
Bioassay Details
Effect : cell viability; effect onBioassay : neuronal PC12 cells transfected with Htt-exon-1 constructs containing Q103 polyglutamine repeats treated with tebufenozideExample 4Defining the
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
117/181
2018-08-03 18:12:50
Structure-Activity Relationship for SUP-2[0163] One of the four hit compounds, SUP-2, was particularly attractive as a probe reagent because it has a chloromethylcarbonyl functionality. Chloromethylcarbonyls are frequently used as moieties for covalently inhibiting enzymes: a nucleophilic Biological Species/NCBI ID
rat
Cells/Cell Lines
PC12 cell line
Substance RN
606417View in Reaxys
Substance Name
SUP-1A
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Patent; STOCKWELL, Brent, R.; HOFFSTROM, Benjamin, G.; (151 pag.); WO2008/143876; (A2); (2008), View in Reaxys 234 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Enzymology inhibition
Bioassay Details
Effect : protein disulfide isomerase (PDI) activity; inhibition of Bioassay : protein disulfide isomerase (PDI)Example 5Protein disulfide isomerases as novel regulators of neuronal apoptosis[0170] We sequenced the target proteins using mass spectrometry and discovered that they were two related protein disulfide isomerases (Figure 6): PDIA1 (SEQ ID NO:1) and PDIA3 (SEQ ID NO:2), which is also known as ERp57
Biological Species/NCBI ID
bovine
Substance RN
606417View in Reaxys
Substance Name
SUP-1A
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Patent; STOCKWELL, Brent, R.; HOFFSTROM, Benjamin, G.; (151 pag.); WO2008/143876; (A2); (2008), View in Reaxys 235 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
reduces the number of avoidance responses of male Wistar rats subjected to a conditioned avoidance situation (0.4 - 0.8 mg/kg i.p.)
Measurement Parameter
qualitative
Cuomo; Cortese; Siro-Brigiani; Arzneimittel-Forschung/Drug Research; vol. 31; nb. 10; (1981); p. 1724 - 1726, View in Reaxys 236 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
strong inhibition of LON-954 induced tremor, and weak inhibition of oxotremorine induced tremor; mice
Measurement Parameter
qualitative
Brand; Menge; Arzneimittel-Forschung/Drug Research; vol. 30; nb. 8; (1980); p. 1242 - 1243, View in Reaxys 237 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
118/181
2018-08-03 18:12:50
Bioassay Details
Effect : |delivery system, controlled release Bioassay : CCK-LI release investigated in synaptosomal suspensions made from cerebral cortex after homogenation and centrifugation by superfusion at 37 deg C; CCK-LI determined by radioligand assay
Biological Species/NCBI ID
human
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.300000 ÂľM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Raiteri; Bonanno; Paudice; Cavazzani; Schmid; Journal of Pharmacology and Experimental Therapeutics; vol. 278; nb. 2; (1996); p. 747 - 751, View in Reaxys 238 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : transport; effect onBioassay : control: vehicle
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
.
Measurement Parameter
qualitative
Aono, Yuri; Saigusa, Tadashi; Mizoguchi, Naoko; Iwakami, Tomoyo; Takada, Koji; Gionhaku, Nobuhito; Oi, Yoshiyuki; Ueda, Koichiro; Koshikawa, Noriaki; Cools, Alexander R.; European Journal of Pharmacology; vol. 580; nb. 1-2; (2008); p. 87 - 94, View in Reaxys 239 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : transport; effect onBioassay : control: vehicle rats implanted with guide cannula for nucleus accumbens; dialysis experiments performed after 7-10 days of surgery; title comp. administered; infused with endomorphin-1 or -2 for 25 min; extracellular levels of dopamine determined
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. increased endomorphin-1-induced enhancement of accumbal extracellular dopamine efflux by over a period of 100 min; title comp. did not affect endomorphin-2-mediated dopamine efflux; fig.
Measurement Parameter
qualitative
Aono, Yuri; Saigusa, Tadashi; Mizoguchi, Naoko; Iwakami, Tomoyo; Takada, Koji; Gionhaku, Nobuhito; Oi, Yoshiyuki; Ueda, Koichiro; Koshikawa, Noriaki; Cools, Alexander R.; European Journal of Pharmacology; vol. 580; nb. 1-2; (2008); p. 87 - 94, View in Reaxys 240 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |transmitter releasing Bioassay : control: vehicle rats implanted with guide cannula for nucleus accumbens; dialysis experiments performed after 7-10 days of surgery; pre-treated with or without bicuculline; 25 min later, title comp. administered; extracellular levels of dopamine determined
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
119/181
2018-08-03 18:12:50
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp. alone increased accumbal extracellular dopamine efflux over a period of 150 min; title comp.-increased dopamine efflux was counteracted by bicuculline pre-treatment; fig.
Measurement Parameter
qualitative
Aono, Yuri; Saigusa, Tadashi; Mizoguchi, Naoko; Iwakami, Tomoyo; Takada, Koji; Gionhaku, Nobuhito; Oi, Yoshiyuki; Ueda, Koichiro; Koshikawa, Noriaki; Cools, Alexander R.; European Journal of Pharmacology; vol. 580; nb. 1-2; (2008); p. 87 - 94, View in Reaxys 241 of 403
242 of 403
Target Name
Neuronal acetylcholine receptor subunit alpha-7 [rat]
Target Synonyms
acra7; chrna7; neuronal acetylcholine receptor subunit alpha-7
Target Uniprot ID
q05941
Target, Subunit, Species
Neuronal acetylcholine receptor subunit alpha-7 [rat]
Target Mutant/Chimera Details
Neuronal acetylcholine receptor subunit alpha-7 [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
P2 fraction: membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
>
Quantitative value
40000
Measurement pX
1
Concomitants: Compound RN
24141394; 24141394
Concomitants: Compound name
Methyllycaconitine; [3H]-Methyllycaconitine
Concomitants: Compound role
NSB; RAD
Target Name
Neuronal acetylcholine receptor subunit alpha-7 [rat]
Target Synonyms
acra7; chrna7; neuronal acetylcholine receptor subunit alpha-7
Target Uniprot ID
q05941
Target, Subunit, Species
Neuronal acetylcholine receptor subunit alpha-7 [rat]
Target Mutant/Chimera Details
Neuronal acetylcholine receptor subunit alpha-7 [rat]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
120/181
2018-08-03 18:12:50
243 of 403
244 of 403
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain
Cells/Cell Lines
nerve cell
Cell Fraction
P2 fraction: membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Qualitative value
ND
Target Name
Ionotropic gamma aminobutyric acid receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid receptor
Target, Subunit, Species
Ionotropic gamma aminobutyric acid receptor [rat]
Target Mutant/Chimera Details
Ionotropic gamma aminobutyric acid receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain
Cells/Cell Lines
cells
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
2
Measurement Parameter
IC50
Unit
nM
Measurement Object
Membrane preparation 1
Quantitative value
6
Deviation
0.200000
Measurement pX
8.22
Concomitants: Compound RN
906818; 906818
Concomitants: Compound name
GABA; [3H]-GABA
Concomitants: Compound role
NSB; RAD
Target Name
4-aminobutanoate: 2-oxoglutarate aminotransferase [rat]
Target Synonyms
4-aminobutanoate: 2-oxoglutarate aminotransferase
Target, Subunit, Species
4-aminobutanoate: 2-oxoglutarate aminotransferase [rat]
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
121/181
2018-08-03 18:12:50
245 of 403
Target Mutant/Chimera Details
4-aminobutanoate: 2-oxoglutarate aminotransferase [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain
Cells/Cell Lines
nerve cell
Cell Fraction
Mitochondria: membrane
Substance RN
606417View in Reaxys
Substance Name
2
Substance Dose
1 mM
Measurement Parameter
inhibition rate
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
234749; 906818
Concomitants: Compound name
Pyridoxal-5-phosphate; [3H]-GABA
Concomitants: Compound role
COM; SUB
Target Name
Glutamine synthetase [rat]
Target Synonyms
glns; glul; glutamate decarboxylase; glutamate-ammonia ligase; glutamine synthetase; gs
Target Uniprot ID
p09606
Target, Subunit, Species
Glutamine synthetase [rat]
Target Mutant/Chimera Details
Glutamine synthetase [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
brain
Cells/Cell Lines
nerve cell
Cell Fraction
Mitochondria: membrane
Substance RN
606417View in Reaxys
Substance Name
2
Substance Dose
1 mM
Measurement Parameter
inhibition rate
Qualitative value
NA
Measurement pX
1
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
122/181
2018-08-03 18:12:50
246 of 403
247 of 403
Concomitants: Compound RN
234749; 1723801
Concomitants: Compound name
Pyridoxal-5-phosphate; [3H]-L-Glutamic acid
Concomitants: Compound role
COM; SUB
Target Name
Nicotinic acetylcholine receptor [rat]
Target Synonyms
nicotinic acetylcholine receptor
Target, Subunit, Species
Nicotinic acetylcholine receptor [rat]
Target Mutant/Chimera Details
Nicotinic acetylcholine receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
>
Quantitative value
10000
Measurement pX
1
Concomitants: Compound RN
82109; 8619061
Concomitants: Compound name
Nicotine; [3H]-ABT 418
Concomitants: Compound role
NSB; RAD
Target Name
Nicotinic acetylcholine receptor [rat]
Target Synonyms
nicotinic acetylcholine receptor
Target, Subunit, Species
Nicotinic acetylcholine receptor [rat]
Target Mutant/Chimera Details
Nicotinic acetylcholine receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Membrane
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
123/181
2018-08-03 18:12:50
248 of 403
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Qualitative value
>
Quantitative value
10000
Measurement pX
1
Concomitants: Compound RN
82109; 83882
Concomitants: Compound name
Nicotine; [3H]-Cytisine
Concomitants: Compound role
NSB; RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : Xenopus laevis oocyte, expressing human β1 GABAC receptorBioassay : OR2: oocyte Ringers-2 incubation solution; Ki: apparent dissociation constant single oocyte binding technique; oocyte incubated with 1 μmol/l <3H>GABA and title comp. in OR2, pH 7.5, for 30 s at room temp.; then rinsed, placed to OR2 for 60 s to let <3H>GABA to dissociate; scintillation fluid added, radioactivity measured
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.0900000 µM
Measurement Parameter
IC50
Unit
µM
Quantitative value
1.17
Measurement pX
5.93
Chang, Yong; Covey, Douglas F.; Weiss, David S.; Molecular Pharmacology; vol. 58; nb. 6; (2000); p. 1375 - 1380, View in Reaxys 249 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |agonist Target : Xenopus laevis oocyte, expressing human β1 GABAC receptorBioassay : oocyte voltage-clamped at -70 mV; current induced by title comp. measured
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.100000 µM
Measurement Parameter
EC50
Unit
µM
Quantitative value
1.48
Measurement pX
5.83
Chang, Yong; Covey, Douglas F.; Weiss, David S.; Molecular Pharmacology; vol. 58; nb. 6; (2000); p. 1375 - 1380, View in Reaxys 250 of 403
Target Name
GABA-A receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor
Target, Subunit, Species
GABA-A receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
124/181
2018-08-03 18:12:50
251 of 403
252 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
inhibition rate
Unit
nM
Quantitative value
16
Target Name
GABA-A receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor
Target, Subunit, Species
GABA-A receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
inhibition rate
Unit
nM
Quantitative value
16
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
time course changes concentrations in plasma and brain of rats after intravenous injection of 1 mg/kg <(3)H>-labelled drug
Measurement Parameter
qualitative
Moroni; Forchetti; Krogsgaard-Larsen; Guidotti; Journal of Pharmacy and Pharmacology; vol. 34; nb. 10; (1982); p. 676 678, View in Reaxys 253 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : chlorid currentTarget : rat cerebral cortex neuroneBioassay : determination of chloride current in vitro; neurons from embryonic rats; whole-cell patch-clamp measurements; add. of (1S,5S)-2-oxabicyclo<3.3.o>octan-3-one ((-)-SBL, 1-10mM), pentylenetetrazol (PTZ, 1-10mM) or picrotoxinin (5 μM)
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 µM
Qualitative Results
title comp. elicited chloride currents; (-)-SBL, PTZ, or picrotoxinin inhibited this effect
Measurement Parameter
qualitative
Maksay; Molnar; Gruber; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 288; nb. 1; (1994); p. 61 - 68, View in Reaxys 254 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : protein disulfide isomerase (PDI) activity; inhibition ofBioassay : Example 5Protein disulfide isomerases as novel regulators of neuronal apoptosis[0170] We sequenced the target proteins
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
125/181
2018-08-03 18:12:50
using mass spectrometry and discovered that they were two related protein disulfide isomerases (Figure 6): PDIA1 (SEQ ID NO:1) and PDIA3 (SEQ ID NO:2), which is also known as ERp57 Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Patent; STOCKWELL, Brent, R.; HOFFSTROM, Benjamin, G.; WO2008/143876; (A2); (2008), View in Reaxys 255 of 403
Substance Effect
Toxic
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : neuronal PC12 cells transfected with Htt-exon-1 constructs containing Q103 polyglutamine repeats treated with tebufenozide of ratBioassay : Example 4Defining the Structure-Activity Relationship for SUP-2[0163] One of the four hit compounds, SUP-2, was particularly attractive as a probe reagent because it has a chloromethylcarbonyl functionality. Chloromethylcarbonyls are frequently used as moieties for covalently inhibiting enzymes: a nucleophilic
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Patent; STOCKWELL, Brent, R.; HOFFSTROM, Benjamin, G.; WO2008/143876; (A2); (2008), View in Reaxys 256 of 403
Substance Effect
Myorelaxant
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Bioassay : uterine-relaxant effect on KCl-induced contraction uteri removed of i) non-pregnant, ii) pregnant (5-20 d), iii) ovariectomized rats; placed into Krebs-Hanseleit solution, 40 mM KCl, 100-500 μM title comp.; contraction of uterine rings recorded by isometric method
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Perusquia, Mercedes; Villalon, Carlos M.; Life Sciences; vol. 58; nb. 11; (1996); p. 913 - 926, View in Reaxys 257 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : PA3 cellsBioassay : effect on (GABA)A receptor function; Kd, Bmax, GABA shift cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 100 μM title comp. and 50 μM GABA
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
Kd = 3.39 nM, Bmax = 101 percent of control, GABA shift: 1.54
Measurement Parameter
qualitative
Klein; Mascia; Harkness; Hadingham; Whiting; Harris; Journal of Pharmacology and Experimental Therapeutics; vol. 274; nb. 3; (1995); p. 1484 - 1492, View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
126/181
2018-08-03 18:12:50
258 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : PA3 cellsBioassay : effect on (GABA)A receptor subunit β1, β1 protein cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 100 μM title comp. and 50 μM GABA; Western blot analysis
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Klein; Mascia; Harkness; Hadingham; Whiting; Harris; Journal of Pharmacology and Experimental Therapeutics; vol. 274; nb. 3; (1995); p. 1484 - 1492, View in Reaxys 259 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : PA3 cellsBioassay : effect on (GABA)A receptor subunit mRNAs: β1, β1, β2L cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 100 μM title comp. and 50 μM GABA; Northern blot analysis
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Klein; Mascia; Harkness; Hadingham; Whiting; Harris; Journal of Pharmacology and Experimental Therapeutics; vol. 274; nb. 3; (1995); p. 1484 - 1492, View in Reaxys 260 of 403
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : ICR mouseBioassay : further invest. with 5-aminovaleric acid or SR 95531 mice pretreated with title comp. for 10 min, then 0.2 μg morphine or 0.1 μg β-endorphin i.t. injected; 15-60 min later, antinociception assessed by measurement of tail-flick response latency after radiant heat stimulation
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intrathecal administration
Qualitative Results
title comp. alone had no effect but significantly potentiated β-endorphin- but not morphine-induced antinociception, maximally at 15 min after administration; effect was antagonized by SR 95531 (figures)
Measurement Parameter
qualitative
Kim, Kee-Won; Woo, Ran-Sook; Kim, Chul-Jin; Cheong, Young-Pyo; Kim, Jong-Keun; Kwun, Jin; Cho, Kyu-Park; Life Sciences; vol. 67; nb. 1; (2000); p. 61 - 71, View in Reaxys 261 of 403
Substance Effect
Nociceptive
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : NMRI albino miceBioassay : pain sensitivity assessed by the hot-plate test at 55 deg C; failure to respond by 45 sec. resulted test; antinociception quantified as the percentage of maximum possible effect; saline as control 20-25 g weight; 10 per cage; light 12 hr per day; 23 deg C; food and water available except experimental sessions; animal's right sciatic nerve exposed, and a 2-3 mm long nerve segment dissected; ligature made around the dissected nerve
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
127/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
0.500000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
antinociceptive effects of different doses of title comp. (figure)
Measurement Parameter
qualitative
Zarrindast, Mohammad-Reza; Pharmacology and Toxicology; vol. 89; nb. 2; (2001); p. 79 - 84, View in Reaxys 262 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : oral dyskinesia; effect onTarget : CR albino ratBioassay : oral activity represents spontaneous chewing (vacuous chewing), which is not directed onto any physical material; HAL = haloperidol; 6-OHDA = 6-hydroxydopamine; title comp. is a GABAA receptor agonist effect of title comp. on oral activity (number of oral movements counted) in intact and 6-OHDA-lesioned rats after HAL or tap water administration for 43 weeks and after HAL withdrawal for 12 weeks
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
no effect on spontaneous oral activity of intact and 6-OHDA-lesioned rats maintained on tap water; no effect on intact rats, but significantly reduced spontaneous oral activity of 6-OHDA-lesioned rats receiving HAL, effect persisted after HAL withdrawal
Measurement Parameter
qualitative
Huang, Nuo-Yu; Kostrzewa, Richard M.; Li, Chuanfu; Perry, Kenneth W.; Fuller, Ray W.; Journal of Pharmacology and Experimental Therapeutics; vol. 280; nb. 1; (1997); p. 268 - 276, View in Reaxys 263 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |secretion stimulant Bioassay : vehicle control; SSTR2: somatostatin type 2 receptor; reference comp.: pentagastrin and 2-deoxy-D-glucose SSTR2 knockout mice; urethane anesthesia; continuous intragastric perfusion with saline; cumulative bolus injections of title comp.; acid secretion measurements during experiment; backtitration
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.100000 mg/kg
Substance Route of Adm.
intravenous administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Piqueras, Laura; Martinez, Vicente; British Journal of Pharmacology; vol. 142; nb. 6; (2004); p. 1038 - 1048, View in Reaxys 264 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |secretion stimulant Target : wild-type mouseBioassay : vehicle control; reference comp.: pentagastrin and 2-deoxy-D-glucose urethane-anesthetized mice; continuous intragastric perfusion with saline; cumulative bolus injections of title comp.; acid secretion measurements during experiment; backtitration
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.100000 mg/kg
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
128/181
2018-08-03 18:12:50
Substance Route of Adm.
intravenous administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Piqueras, Laura; Martinez, Vicente; British Journal of Pharmacology; vol. 142; nb. 6; (2004); p. 1038 - 1048, View in Reaxys 265 of 403
Substance Effect
Toxic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : wild-type mouseBioassay : vehicle control urethane-anesthetized mice; continuous intragastric perfusion with saline; cumulative bolus injections of title comp.; adverse events monitored
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 mg/kg
Substance Route of Adm.
intravenous administration
Qualitative Results
title comp. at 1.0 mg/kg caused signs of dyspnea in some of animals, which increased at 3 mg/kg
Measurement Parameter
qualitative
Piqueras, Laura; Martinez, Vicente; British Journal of Pharmacology; vol. 142; nb. 6; (2004); p. 1038 - 1048, View in Reaxys 266 of 403
267 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
human
Organs/Tissues
brain cortex
Cell Fraction
Cytoplasmic membrane
Substance RN
606417View in Reaxys
Substance Name
musimol
Substance Dose
100 ÂľM
Measurement Parameter
Ki (inhibition constant)
Qualitative value
NA
Measurement pX
1
Concomitants: Compound RN
702691; 702691
Concomitants: Compound name
Flunitrazepam; [3H]-Flunitrazepam
Concomitants: Compound role
NSB; RAD
Target Name
Ionotropic glutamate NMDA receptor [rat]
Target Synonyms
ionotropic glutamate nmda receptor
Target, Subunit, Species
Ionotropic glutamate NMDA receptor [rat]
Target Mutant/Chimera Details
Ionotropic glutamate NMDA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
129/181
2018-08-03 18:12:50
268 of 403
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Dose
100 µM
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
13
Deviation
15
Measurement pX
1
Concomitants: Compound RN
4132986; 4234994
Concomitants: Compound name
L-Glutamate; [3H]-CPP
Concomitants: Compound role
NSB; RAD
Substance Effect
Hypothermic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)+/+ mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; changes in body temperature recorded using subcutaneous temperature-sensitive chip
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 269 of 403
Substance Effect
Hypothermic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)+/- mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; changes in body temperature recorded using subcutaneous temperature-sensitive chip
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
qualitative
Qualitative value
NA
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
130/181
2018-08-03 18:12:50
Measurement pX
1
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 270 of 403
Substance Effect
Hypothermic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)-/- mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; changes in body temperature recorded using subcutaneous temperature-sensitive chip
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. induced pronounced hypothermia with maximal effect at 60 - 80 min after administration (figure)
Measurement Parameter
qualitative
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 271 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)+/+ mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; behavioral changes were scored according to semiquantitative scale
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. induced sedation and reduced locomotor activity (table)
Measurement Parameter
qualitative
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 272 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)+/- mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; behavioral changes were scored according to semiquantitative scale
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. induced sedation and reduced locomotor activity (table)
Measurement Parameter
qualitative
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
131/181
2018-08-03 18:12:50
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 273 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : C57B16/129Sv F1 hybrid GABAB(1)-/- mouseBioassay : GABAB: β-aminobutyric acid B receptor animals placed in individual cages; title comp. injected; behavioral changes were scored according to semiquantitative scale
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 mg/kg
Substance Route of Adm.
subcutaneous administration
Qualitative Results
title comp. induced completely different pattern of behaviour; it triggered periods of intense jumping and wild running (table)
Measurement Parameter
qualitative
Queva, Christophe; Bremner-Danielsen, Marianne; Edlund, Anders; Ekstrand, A. Jonas; Elg, Susanne; Erickson, Sven; Johansson, Thore; Lehmann, Anders; Mattsson, Jan P.; British Journal of Pharmacology; vol. 140; nb. 2; (2003); p. 315 322, View in Reaxys 274 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |antagonist Bioassay : max. height of vertical jump (MHVJ) measured (using Watanabe's method) for 24 h; title comp. effect on TA- or TRH-induced increase of MHVJ studied (diagram) 164-210 g rats (T=25 deg C; R.H.=55 percent; 12 h light/dark cycle); ataxia induced by 75 mg/kg i.p. 3-acetylpyridine; 4 h later 300 mg/kg i.p. niacinamid; 15 min after title comp. 1 mg/kg TA-0910 (TA) or 10 mg/kg thyrotropin-releasing hormone (TRH) inj. i.p.
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.300000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Kinoshita, Kiyoshi; Watanabe, Yumi; Yamamura, Michio; Matsuoka, Yuzo; European Journal of Pharmacology; vol. 343; nb. 2-3; (1998); p. 129 - 133, View in Reaxys 275 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : parakeratosis; inhibition ofTarget : hairless mouseBioassay : Test on parakeratosis inhibitory action] A 3% or 30% oleic acid solution (100 &micro;L, solvent: ethanol) was applied on the back of a hairless mouse. Thereafter, 100 &micro;L of sample solution or reference solution was applied. This procedure was repeated for 3 days, and the keratin layer on
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
cutaneous administration
Qualitative Results
title comp. improved parakeratosis caused by oleic acid
Measurement Parameter
qualitative
Patent; SHISEIDO COMPANY, LTD.; WO2003/99327; (2003); (A1) japanese, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
132/181
2018-08-03 18:12:50
276 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
0.25
Concomitants: Compound name
PBQ
Concomitants: Compound role
IAV
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 277 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
which prolonge the reaction time by more than 75%
Quantitative value
0.36
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 278 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
oral administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
which prolonge the reaction time by more than 75%
Quantitative value
0.5
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 279 of 403
Bioassay Category
In Vivo (Animal models)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
133/181
2018-08-03 18:12:50
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
which prolonge the reaction time by more than 75%
Qualitative value
>
Quantitative value
0.56
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 280 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
4.8
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 281 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
rhesus monkey
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
MED (minimum effective drug dose)
Unit
mg/kg
Quantitative value
1
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 282 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
134/181
2018-08-03 18:12:50
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
3.8
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 283 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
5
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 284 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Substance Route of Adm.
subcutaneous administration
Substance Dosing Regimen
Single
Measurement Parameter
ED50
Unit
mg/kg
Quantitative value
0.29
Concomitants: Compound name
Yeast solution
Concomitants: Compound role
IAV
Hill; Maurer; Buescher; Roemer; European Journal of Pharmacology; vol. 69; nb. 2; (1981); p. 221 - 224, View in Reaxys 285 of 403
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
135/181
2018-08-03 18:12:50
286 of 403
287 of 403
288 of 403
Bioassay Name
Binding
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
98.81
Measurement pX
6.28
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
98.81
Measurement pX
6.28
Target Name
ionotropic gamma aminobutyric acid a receptor [rat]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [rat]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [rat]:Wild
Target Species (Bioactivity)
rat
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cell Fraction
Membrane
Substance RN
606417View in Reaxys
Substance Name
Muscimol
Measurement Parameter
inhibition rate
Unit
%
Quantitative value
98.81
Measurement pX
6.28
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
136/181
2018-08-03 18:12:50
Qualitative Results
inhibitor of GABAA receptor inhibitor in rat brain synaptic membranes (IC50=0.006 μM)
Measurement Parameter
qualitative
Hjeds, Hans; Christensen, Inge T.; Cornett, Claus; Frolund, Bente; Falch, Erik; et al.; Acta Chemica Scandinavica; vol. 46; nb. 8; (1992); p. 772 - 777, View in Reaxys 289 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Bioassay : Wistar rats, membranes prepared from the whole brain, enriched with cholesterol, incubated with phosphatidylcholine liposomes, experiments were performed to determine the binding effects of flunitrazepam
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title comp. resulted in an increase in its potency as a potentiator of flunitrazepam binding, following cholesterol enrichment
Measurement Parameter
qualitative
Bennett; Simmonds; British Journal of Pharmacology; vol. 117; nb. 1; (1996); p. 87 - 92, View in Reaxys 290 of 403
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : ECT: stimulated by constant current pulses, electrodes at base of the neck, 1 cm apart, and at base of the tail, electrodes 4 cm apart, result expressed as times of control (predrug) value rats 160-200 g with lumbar subarachnoid catheters (adjacent to lower lumbar and sacral segments); analgesic effect by electrical current threshold (ECT) test at neck and at tail, min. current causing vocalization
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intrathecal administration
Qualitative Results
increased simultaneously, dose-dependently ECT (at tail, but not at neck) (analgesic effect spinally mediated); dose-effect, time-effect diagrams, numerical tables
Measurement Parameter
qualitative
Nadeson; Guo; Porter; Gent; Goodchild; Journal of Pharmacology and Experimental Therapeutics; vol. 278; nb. 2; (1996); p. 620 - 626, View in Reaxys 291 of 403
Substance Effect
Anticonvulsant
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Target : hippocampus of Wistar ratBioassay : MEM: minimal essential medium organotypic hippocampal slice cultures pre-incubated with title comp. for 30-60 min; continuously superfused with prewarmed MEM contg. low magnesium ion and KCl; neuronal interactions recorded tungsten-inglass microelectrode
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 µM
Qualitative Results
title comp. reversible blocked the seizure-like events; fig.
Measurement Parameter
qualitative
Albus; Wahab; Heinemann; British Journal of Pharmacology; vol. 154; nb. 3; (2008); p. 709 - 724, View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
137/181
2018-08-03 18:12:50
292 of 403
293 of 403
Target Name
Gamma aminobutyric acid B receptor [rat]
Target Synonyms
gamma aminobutyric acid b receptor
Target, Subunit, Species
Gamma aminobutyric acid B receptor [rat]
Target Mutant/Chimera Details
Gamma aminobutyric acid B receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
Sprague Dawley rat
Organs/Tissues
brain
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
muscinol
Measurement Parameter
IC50
Unit
µM
Quantitative value
0.01
Measurement pX
8
Concomitants: Compound RN
774694
Concomitants: Compound name
[3H]-Muscimol
Concomitants: Compound role
RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : attraction of dendrites to axon terminals of GABAergic interneurons Bioassay : cerebellar cortex Purkinje cells
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
30 µM
Qualitative Results
number of interneurons neighboring dendrites per primary dendrite ~ 0.7
Measurement Parameter
qualitative
Qualitative value
#
Kawaguchi, Koji; Habara, Tomomi; Terashima, Toshio; Kikkawa, Satoshi; Journal of Neurochemistry; vol. 114; nb. 2; (2010); p. 627 - 638, View in Reaxys 294 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : cell dendrites morphology Bioassay : cerebellar cortex Purkinje cellsparameters for control untreated cells: length of the longest dendrite: 80 μm, number of branching points: 4
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
138/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
30 µM
Qualitative Results
length of the longest dendrite at 1-7 days ~ 95 μm
Measurement Parameter
qualitative
Qualitative value
#
Kawaguchi, Koji; Habara, Tomomi; Terashima, Toshio; Kikkawa, Satoshi; Journal of Neurochemistry; vol. 114; nb. 2; (2010); p. 627 - 638, View in Reaxys 295 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : cell dendrites morphology Bioassay : cerebellar cortex Purkinje cellsparameters for control untreated cells: length of the longest dendrite: 85.7 μm, number of branching points: 25.8, and dendritic area: ~ 3000 μm2
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 µM
Qualitative Results
length of the longest dendrite ~ 110 - ~ 140 μm
Measurement Parameter
qualitative
Qualitative value
#
Kawaguchi, Koji; Habara, Tomomi; Terashima, Toshio; Kikkawa, Satoshi; Journal of Neurochemistry; vol. 114; nb. 2; (2010); p. 627 - 638, View in Reaxys 296 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
anticonvulsant activity in epileptic fowl at the dose of 0.75 mg/kg
Measurement Parameter
qualitative
Johnson; Davis; Arzneimittel-Forschung/Drug Research; vol. 34; nb. 12; (1984); p. 1753 - 1757, View in Reaxys 297 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |agonist Bioassay : olfactory bulb granule cell layers from rats (200-350g); adenylyl cyclase activity stimulated by title comp. determined by monitoring the conversion of (β-32P)-ATP into <32P>-cyclic AMP; comparison with the effect of (-)-baclofen
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1.00000E-06 M
Qualitative Results
(diagram) No effect
Measurement Parameter
qualitative
Olianas, Maria C.; Onali, Pierluigi; British Journal of Pharmacology; vol. 126; nb. 3; (1999); p. 657 - 664, View in Reaxys 298 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : drug interactionTarget : rostral ventrolateral medulla (RVLM) of Sprague-Dawley ratsBioassay : stable RVLM neurons were recorded intra- and extracellular; GABAA selective receptor agonist title comp. (1 μM in aCFS soln.) rats perfused transcardially with modified artificial cerebro-
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
139/181
2018-08-03 18:12:50
spinal (maCSF) fluid; after removal of the brain slices were cut through the RVLM, then incubated first in maCSF then in aCFS with low Ca++/high Mg++, used to block synaptic transmission Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
GABAB receptor antagonists: 2-hydroxysalcofen, CGP-5426A, CGP-55845A have no effect on inhibitory activity of title comp.
Measurement Parameter
qualitative
Li; Guyenet; American Journal of Physiology - Regulatory Integrative and Comparative Physiology; vol. 268; nb. 2 37-2; (1995); p. R428-R437, View in Reaxys 299 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Bioassay : incubation with title comp. at 4 deg C for 1 h; binding assayed with liquid scintillation 10-w-old male rats killed; brain removed, homogenized; membrane separated; protein conc. measured with bicinchoninic acid protein assay
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 µM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
18.5
Measurement pX
7.73
Hauser; Chesnoy-Marchais; Robel; Baulieu; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 289; nb. 2; (1995); p. 249 - 257, View in Reaxys 300 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |receptor; binding activity Target : 293 cell lineBioassay : binding assayed with liquid scintillation; other receptor subtypes also studied cells incubated at 37 deg C, 5 percent CO2; transfected with rat β6, β1, β2, β2 cDNA; membranes from transfected cells separated; incubated with title comp. at 4 deg C for 1 h
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
1 µM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
3.3
Measurement pX
8.48
Hauser; Chesnoy-Marchais; Robel; Baulieu; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 289; nb. 2; (1995); p. 249 - 257, View in Reaxys 301 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : electrophysiologicalTarget : rat hippocampal slicesBioassay : recordings of orthodromic extracellular field potentials made from the CA1 pyramidal cell layer following stimulation of the Schaffer collateral fibres in Stratum radiatum; glass microelectrodes (2 M NaCl); stimulation by bipolar electrodes (0.01 Hz) rats (170-200 g) anaesthetized and decapitated; brains rapidly taken out; hippocampi cut transversely into 450 μm thick slices; submerged in perfusion chamber in the medium (4 ml/min)
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
140/181
2018-08-03 18:12:50
Substance Name
31872
Substance Dose
0.100000 µM
Qualitative Results
induced concentration-dependent inhibition of the evoked population potential; at 0.1 to 5 μM this inhibition was reversible; the response depended also on duration of perfusion; at 10 μM stable long-lasting depression, supressed with 1 Hz stimulation
Measurement Parameter
qualitative
Akhondzadeh; Stone; British Journal of Pharmacology; vol. 115; nb. 3; (1995); p. 527 - 533, View in Reaxys 302 of 403
Substance Effect
Behavioural Symptoms
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Bioassay : adult rats weighing 300-425 g; unilateral injection of title comp. with 2-20 μg Tween 80 into the substantia nigra pars reticulata
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
significant asymmetric circling
Measurement Parameter
qualitative
Wickens; Pertwee; European Journal of Pharmacology; vol. 282; nb. 1-3; (1995); p. 251 - 254, View in Reaxys 303 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : drug interactionBioassay : adult rats weighing 300-425 g; unilateral injection into the substantia nigra pars reticulata of title comp. with 1-10 μg Δ9-tetrahydrocannabinol
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Route of Adm.
intracerebral administration
Qualitative Results
title comp.-induced contralateral circling increased by simultaneous admin. of 1 μg Δ9-tetrahydrocannabinol and abolished by 10 μg Δ9-tetrahydrocannabinol
Measurement Parameter
qualitative
Wickens; Pertwee; European Journal of Pharmacology; vol. 282; nb. 1-3; (1995); p. 251 - 254, View in Reaxys 304 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : baroreflex regulation effectBioassay : measured mean pressure (MAP), heart rate (HR), renal nerve activity; magnitude of the reflex bradycardia and sympathoinhibition caused by phenylephrine; magnitude of reflex tachycardia and sympathoexcitation caused by sodium nitroprusside 3-month-old rats <30 females (ca. 281g) and 33 males (ca.435 g)>; cannulated femoral vein and artery; before of title comp. baroreflex responses induced by phenylephrine (37.5 μg/ml, i.v.) or sodium nitroprusside (50 μg/ml, i.v.), CFS control
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
title comp. increased MAP and HR, but reduced all phenylephrine- and Na-nitroprusside-induced reflex responses
Measurement Parameter
qualitative
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
141/181
2018-08-03 18:12:50
Okada; Bunag; Journal of Cardiovascular Pharmacology; vol. 26; nb. 3; (1995); p. 363 - 371, View in Reaxys 305 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : drug interactionTarget : OVX Sprague-Dawley rat preoptic area neurosomesBioassay : in vitro; 37 deg C; glutamate and 4-aminobutyric acid (GABA) release; OVX female rat=ovariohysterectomized female rat; EB=β-estradiol-3-benzoate; P=progesterone postpubertal rat weight 150-175 g; OVX bilaterally; EB (2x2 μg s.c. inj. 24-48 h presacr.) and/or P (500 μg s.c. inj. 3.5-4 h presacr.) pretreatment; neurosome preparation; <3H>-glutamate pretreat. (37 deg C, 30 min); drug incubation; radioactivity
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2 µM
Qualitative Results
EB+P significantly increased drug-induced GABA and glutamate release; drug promoted glutamate release dose-dependently in EB+P treated neurosomes
Measurement Parameter
qualitative
Fleischmann; Makman; Etgen; Life Sciences; vol. 56; nb. 20; (1995); p. 1665 - 1678, View in Reaxys 306 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |secretion stimulant Target : OVX Sprague-Dawley rat preoptic area neurosomesBioassay : in vitro; 37 deg C; glutamate and 4-aminobutyric acid release; OVX female rat=ovariohysterectomized female rat postpubertal rat weight 150-175 g; OVX bilaterally; sacrifice; neurosome preparation and incubation; <3H>-glutamate pretreatment (37 deg C, 30 min); drug incubation; radioactivity
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
100 µM
Measurement Parameter
qualitative
Qualitative value
NA
Measurement pX
1
Fleischmann; Makman; Etgen; Life Sciences; vol. 56; nb. 20; (1995); p. 1665 - 1678, View in Reaxys 307 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : drug interactionTarget : gonadally intact Sprague-Dawley rat preoptic area neurosomesBioassay : in vitro; 37 deg C; glutamate and 4-aminobutyric acid (GABA) release postpubertal rat weight 150-175 g; sacrifice; neurosome preparation and incubation; <3H>-glutamate pretreatment (37 deg C, 30 min); drug incubation with 25 μM picrotoxin or 10 μM bicuculline; radioactivity
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
100 µM
Qualitative Results
picrotoxin and bicuculline inhibited drug-induced glutamate and GABA release
Measurement Parameter
qualitative
Fleischmann; Makman; Etgen; Life Sciences; vol. 56; nb. 20; (1995); p. 1665 - 1678, View in Reaxys 308 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |secretion stimulant Target : gonadally intact Sprague-Dawley rat preoptic area neurosomesBioassay : in vitro; 37 deg C; glutamate and 4-aminobutyric acid (GABA) release; KRB=Krebs-Ringer buffer postpubertal rat weight 150-175 g; sacrifice; neurosome preparation and incubation in calcium- or high magnesium-containing KRB; <3H>-glutamate pretreatment (37 deg C, 30 min); drug incubation; radioactivity
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
142/181
2018-08-03 18:12:50
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 µM
Qualitative Results
dose-dependently induced significant glutamate and GABA release in calcium-containing, but not in magnesium-containing KRB
Measurement Parameter
qualitative
Fleischmann; Makman; Etgen; Life Sciences; vol. 56; nb. 20; (1995); p. 1665 - 1678, View in Reaxys 309 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |secretion stimulant Target : Sprague-Dawley rat frontal cortical neurosomesBioassay : in vitro; 37 deg C; glutamate release; KRB=Krebs-Ringer buffer gonadally intact, postpubertal rat weight 150-175 g; sacrifice; neurosome preparation and incubation in calcium- or high magnesiumcontaining KRB; <14C>-glutamate pretreatment (37 deg C, 30 min); drug incubation; radioactivity
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
400 µM
Qualitative Results
induced significant glutamate release in calcium-containing KRB, but not in high magnesium-containing KRB
Measurement Parameter
qualitative
Fleischmann; Makman; Etgen; Life Sciences; vol. 56; nb. 20; (1995); p. 1665 - 1678, View in Reaxys 310 of 403
Substance Effect
Dopaminergic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Target : Sprague-Dawley rat striatumBioassay : dopamine (DA) release; GVA=β-guanidinovaleric acid rat weight 250-350 g; surgical preparation; immobilization; dialysis (perfusion rate 2 μl/min with Ringer solution); drug treatment alone or with 10 mM GVA; 20 min dialysate collections; HPLC-ECD; decapitation and cannula location after experiment
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 mM
Substance Route of Adm.
intracerebral administration
Qualitative Results
alone no effect; drug+GVA increased DA release between 20 and 180 min, 220 min, the release smaller than that induced by GVA alone
Measurement Parameter
qualitative
Kabuto; Yokoi; Iwaya; Mori; Life Sciences; vol. 56; nb. 20; (1995); p. 1741 - 1748, View in Reaxys 311 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : |secretion stimulant Target : Sprague-Dawley rat striatumBioassay : serotonin (5-HT) release; GVA=β-guanidinovaleric acid rat weight 250-350 g; surgical preparation; immobilization; dialysis (perfusion rate 2 μl/min with Ringer solution); drug treatment alone or with 10 mM GVA; 20 min dialysate collections; HPLC-ECD; decapitation and cannula location after experiment
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
10 mM
Substance Route of Adm.
intracerebral administration
Qualitative Results
alone increased 5-HT release between 100 and 120 min; drug+GVA increased 5-HT release between 60 and 160 min, the release smaller than that induced by GVA alone
Measurement Parameter
qualitative
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
143/181
2018-08-03 18:12:50
Kabuto; Yokoi; Iwaya; Mori; Life Sciences; vol. 56; nb. 20; (1995); p. 1741 - 1748, View in Reaxys 312 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : rat cerebellar membrane GABAA receptorBioassay : receptors immunoprecipitated by sera specific for β-subunit of GABAA receptor, bound to protein ASepharose; receptor labelled with <3H>-title comp., competition curve with title comp.
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
0.49
Measurement pX
9.31
Quirk; Whiting; Ragan; McKernan; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 290; nb. 3; (1995); p. 175 - 181, View in Reaxys 313 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : rat cerebellar membrane GABAA receptorBioassay : receptors immunoprecipitated by sera specific for β2-subunit of GABAA receptor, bound to protein ASepharose; receptor labelled with <3H>-title comp., competition curve with title comp.
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
Ki (inhibition constant)
Unit
nM
Quantitative value
2.9
Measurement pX
8.54
Quirk; Whiting; Ragan; McKernan; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 290; nb. 3; (1995); p. 175 - 181, View in Reaxys 314 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : rat cerebellar membrane GABAA receptorBioassay : receptors immunoprecipitated by polyclonal antibody (raised against cytoplasmic loop region of βsubunit of GABAA receptor) bound to protein A-Sepharose; <3H>-title comp. binding assay
Substance RN
606417View in Reaxys
Substance Name
31872
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
1.17
Measurement pX
8.93
Quirk; Whiting; Ragan; McKernan; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 290; nb. 3; (1995); p. 175 - 181, View in Reaxys 315 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Target : rat cerebellar membrane GABAA receptorBioassay : receptors immunoprecipitated by sera specific for β2-subunit of GABAA receptor, bound to protein ASepharose; <3H>-title comp. binding assay
Substance RN
606417View in Reaxys
Substance Name
31872
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
144/181
2018-08-03 18:12:50
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
5.9
Measurement pX
8.23
Quirk; Whiting; Ragan; McKernan; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 290; nb. 3; (1995); p. 175 - 181, View in Reaxys 316 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : drug interactionBioassay : membranes, from 3000-4000 starved (24-48 h) hydra, (0.250-0.30 mg protein), incubated 10 min at 0 deg C with 20 nM 3H-labeled β-aminobutyric acid ((3H)GABA) in presence or absence of title comp.
Biological Species/NCBI ID
Hydra vulgaris
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
30 µM
Qualitative Results
title comp. completely inhibited (96.5 percent) GABA binding to crude membrane preparation
Measurement Parameter
qualitative
Pierobon, Paola; Concas, Alessandra; Santoro, Giovanna; Marino, Giuseppe; Minei, Rosario; Pannaccione, Anna; Mostallino, Maria Cristina; Biggio, Giovanni; Life Sciences; vol. 56; nb. 18; (1995); p. 1485 - 1497, View in Reaxys 317 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Bioassay Details
Effect : |agonist Bioassay : 2 ml of Ag+-pretreated membrane suspension, preincubated with 1E-5 M thiomuscimol for 40 min in the dark at 0-4 deg C; UV radiation applied for 40 min at 254 nm; resuspended for (3H)-title comp. binding assay rats decapitated, cerebral cortex removed and homogenized, pellets separated and resuspended in Tris, citrate contg. AgNO3 (5E-4 M) at 0-4 deg C for 10 min; pellets washed, and resuspended in Tris, citrate buffer pH 7.1 at a concn. of 20 mg tissue/ml
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.000100000 M
Qualitative Results
thiomuscimol inhibits (3H)-title comp. binding to Ag+-treated membrane preparation, produced a 20-30 percent irreversible decrease in high-affinity (3H)-title comp. binding sites; Kd 2.8; Bmax 150
Measurement Parameter
qualitative
Nielsen; Witt; Ebert; Krogsgaard-Larsen; European Journal of Pharmacology - Molecular Pharmacology Section; vol. 289; nb. 1; (1995); p. 109 - 112, View in Reaxys 318 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : bindingTarget : brain of Sprague-Dawley ratBioassay : autoradiographic anal. of dried slices; ASO - antisense oligodeoxynuclide rats (250-300 g) cannulated, injection of vehicle or gamma-2 ASO (18 μg, every 12 h 3 days) into right i.c.v. space; 6 h after last i.c.v. injection rats killing, brain slices prepn.; preincubation (15 min); incubation with 3H-labeled title compd.
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
5 nM
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
145/181
2018-08-03 18:12:50
Qualitative Results
specific binding in various brain tissue areas (dependence on gamma-2 ASO pretreatment) evaluated (diagram)
Measurement Parameter
qualitative
Zhao, Tai-Jun; Li, Ming; Chiu, Ted H.; Rosenberg, Howard C.; Journal of Pharmacology and Experimental Therapeutics; vol. 287; nb. 2; (1998); p. 752 - 759, View in Reaxys 319 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
606417View in Reaxys
Substance Name
31872
Qualitative Results
binding to membranes from rat forebrain
Measurement Parameter
qualitative
Frolund; Ebert; Lawrence; Hurt; Krogsgaard-Larsen; Journal of Labelled Compounds and Radiopharmaceuticals; vol. 36; nb. 9; (1995); p. 877 - 889, View in Reaxys 320 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : |receptor; binding activity Bioassay : in vitro; saturation binding assay; brain membranes from normal or renal dysfunction rats; <3H>title comp. as radioligand; 50 mmol Tris-HCl buffer, pH 7.4; 100 mmol/l KCl; 4 deg C; incub. 10 min; radioligand binding measured by scintillation counting
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
2.55000 nM
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Quantitative value
51.81 - 58.43
Measurement pX
7.29
Srivastava, Kalpana; Hatanaka, Tomomi; Katayama, Kazunori; Koizumi, Tamotsu; Biological and Pharmaceutical Bulletin; vol. 22; nb. 3; (1999); p. 288 - 294, View in Reaxys 321 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Bioassay Details
Effect : receptor; activation ofTarget : ICR mouseBioassay : morphine administered once in HR and once a day for 6 d in RT and DS experiments title comp. effect on 10 mg/kg s.c. morphine-induced hyperactivity (HR), reverse tolerance (RT) and postsynaptic dopamine receptor supersensitivity (DS) examined using tilting-type ambulometer
Substance RN
606417View in Reaxys
Substance Name
31872
Substance Dose
0.300000 mg/kg
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
inhibition on morphine-induced HR, RT and DS via activation of GABAA receptors (diagrams)
Measurement Parameter
qualitative
Yoon, In-Seup; Kim, Hack-Seang; Hong, Jin-Tae; Lee, Myung-Koo; Oh, Ki-Wan; Pharmacology; vol. 65; nb. 4; (2002); p. 204 - 209, View in Reaxys 322 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Anticonvulsant activity expressed as oral dose required to prevent the induction of tonic extensor seizures in 50 of mice was determined
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
146/181
2018-08-03 18:12:50
Biological Species/NCBI ID
mouse
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
Oral dose required to prevent the induction of tonic extensor seizures in 50% of mice
Qualitative value
=
Quantitative value
1.34
Atkinson; Girard; Rokach; Rooney; McFarlane; Rackham; Share; Journal of Medicinal Chemistry; vol. 22; nb. 1; (1979); p. 99 - 106, View in Reaxys 323 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Skeletal Muscle Relaxant activity expressed as reduction of the flexor reflex response by 70 in cat after a cumulative intravenous dose; IE is Ineffective upto 7.5 mg/Kg
Biological Species/NCBI ID
cat
Substance RN
606417View in Reaxys
Substance Route of Adm.
intravenous administration
Qualitative Results
IE
Measurement Parameter
ED70
Measurement Object
Skeletal Muscle Relaxant activity expressed as reduction of the flexor reflex response by 70% in cat
Atkinson; Girard; Rokach; Rooney; McFarlane; Rackham; Share; Journal of Medicinal Chemistry; vol. 22; nb. 1; (1979); p. 99 - 106, View in Reaxys 324 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Skeletal Muscle Relaxant activity expressed as reduction of the flexor reflex response by 70 in rat after a cumulative intravenous dose
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
ED70
Unit
mg/kg
Measurement Object
Skeletal Muscle Relaxant activity expressed as reduction of the flexor reflex response by 70% in rat
Qualitative value
=
Quantitative value
16
Atkinson; Girard; Rokach; Rooney; McFarlane; Rackham; Share; Journal of Medicinal Chemistry; vol. 22; nb. 1; (1979); p. 99 - 106, View in Reaxys 325 of 403
Target Name
Gamma-aminobutyric acid receptor subunit delta [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18506 + p63138 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit delta [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
147/181
2018-08-03 18:12:50
326 of 403
327 of 403
Target Species (Bioactivity)
rat
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards rat brain synaptic membrane gamma-aminobutyric acid A receptor alpha upon incubation in buffer, pH 7.4 for 45 minutes at 0 degree C using [3H]muscimol as radioligand
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound name
[3H]Muscimol
Concomitants: Compound role
RAD
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonist activity of the compound towards human GABAA receptor expressed in bovine oocytes
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
Kd (dissociation constant)
Unit
µM
Qualitative value
=
Quantitative value
1.4
Measurement pX
5.85
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
148/181
2018-08-03 18:12:50
328 of 403
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonist activity of the compound towards human GABAA receptor expressed in oocytes
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
Kd (dissociation constant)
Unit
µM
Qualitative value
=
Quantitative value
2.3
Measurement pX
5.64
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro inhibitory concentration of the compound against whole-cell patch-clamp using cultured rat cerebral cortical neurons
Biological Species/NCBI ID
rat
Cells/Cell Lines
Brain cerebrocortical neuron cell
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Frolund; Tagmose; Liljefors; Stensbol; Engblom; Kristiansen; Krogsgaard-Larsen; Journal of Medicinal Chemistry; vol. 43; nb. 26; (2000); p. 4930 - 4933, View in Reaxys 329 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Body weight of nephrectomized rats was determined upon oral administration of the compound at a dose of 1 mg/kg body weight on 15 day; n = 8, Control = 264.1+/-10.2
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
body weight
Unit
g
Measurement Object
Body weight
Qualitative value
=
Quantitative value
247.8
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
149/181
2018-08-03 18:12:50
Deviation
6.3
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 330 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on serum urea nitrogen in nephrectomized rats upon oral administration of 1 mg/kg on 0 day; n = 8, Control = 65.2+/-4.2
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
Activity
Unit
mg/dL
Measurement Object
Water Intake
Qualitative value
=
Quantitative value
65
Deviation
3.6
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 331 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on serum creatinine in nephrectomized rats upon oral administration of 1 mg/kg on 0 day; n = 8, Control = 1.03+/-0.07
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
Activity
Unit
mg/dL
Qualitative value
=
Quantitative value
1.03
Deviation
0.06
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 332 of 403
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Body weight of nephrectomized rats was determined upon oral administration of the compound at a dose of 1 mg/kg body weight on 0 day; n = 8, Control = 223.1+/-6.2
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
body weight
Unit
g
Measurement Object
Body weight
Qualitative value
=
Quantitative value
219.9
Deviation
4.2
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
150/181
2018-08-03 18:12:50
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 333 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on urinary protein in nephrectomized rat upon oral administration of 1 mg/kg on 15 day; n = 8, Control = 33.5+/-5.7
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
Activity not calculated
Measurement Parameter
qualitative
Measurement Object
Activity
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 334 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on serum urea nitrogen in nephrectomized rats upon oral administration of 1 mg/kg on 15 day; n = 8, Control = 56.4+/-5.7
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
Activity
Unit
mg/dL
Qualitative value
=
Quantitative value
44.8
Deviation
3.6
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 335 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on water intake in nephrectomized rat upon oral administration of 1 mg/kg on 10 day; n = 8, Control = 54.8+/-2.4
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
Activity
Unit
mL/day
Measurement Object
Water Intake
Qualitative value
=
Quantitative value
56.7
Deviation
4.2
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 336 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effect of the compound on serum creatinine in nephrectomized rats upon oral administration of 1 mg/kg on 15 day; n = 8, Control = 0.92+/-0.09
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
151/181
2018-08-03 18:12:50
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
Activity
Unit
mg/dL
Qualitative value
=
Quantitative value
0.74
Deviation
0.04
Sasaki, Sumiyo; Tohda, Chihiro; Kim, Mujo; Yokozawa, Takako; Biological and Pharmaceutical Bulletin; vol. 30; nb. 4; (2007); p. 687 - 691, View in Reaxys 337 of 403
338 of 403
Target Name
Gamma-aminobutyric acid receptor subunit delta [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18506 + p63138 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit delta [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro inhibitory concentration of the compound against GABA receptor in rat brain membrane
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
ÂľM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Target Name
Proton-coupled amino acid transporter 1 [human]
Target Synonyms
hpat1; pat1; proton-coupled amino acid transporter 1; proton/amino acid transporter 1; slc36a1; solute carrier family 36 member 1
Target Uniprot ID
q7z2h8
Target, Subunit, Species
Proton-coupled amino acid transporter 1 [human]
Target Mutant/Chimera Details
Proton-coupled amino acid transporter 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
152/181
2018-08-03 18:12:50
339 of 403
340 of 403
Bioassay Details
Ability to inhibit proline (12.5 nM) uptake in Caco-2 monolayers mediated by human proton-coupled amino acid transporter
Biological Species/NCBI ID
human
Cells/Cell Lines
Caco-2 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
Ki (inhibition constant)
Unit
mM
Qualitative value
=
Quantitative value
1.7
Deviation
0.1
Measurement pX
2.77
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding constant of the compound towards human GABAC receptor rho2 expressed in xenopus oocytes
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
Kd (dissociation constant)
Unit
ÂľM
Qualitative value
=
Quantitative value
1.4
Measurement pX
5.85
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
153/181
2018-08-03 18:12:50
341 of 403
342 of 403
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Concentration of compound required for 50 inhibition of human gamma-aminobutyric-acid A receptor
Biological Species/NCBI ID
human
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding constant of the compound towards human GABAC receptor rho1 expressed in xenopus oocytes
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
Kd (dissociation constant)
Unit
µM
Qualitative value
=
Quantitative value
2.3
Measurement pX
5.64
Target Name
Gamma-aminobutyric acid receptor subunit rho-2 [rat]
Target Synonyms
gaba(a) receptor subunit rho-2; gaba(c) receptor; gabrr2; gamma-aminobutyric acid receptor subunit rho-2
Target Uniprot ID
p47742
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit rho-2 [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit rho-2 [rat]:Wild
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
154/181
2018-08-03 18:12:50
343 of 403
344 of 403
Target Species (Bioactivity)
rat
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound against rat GABAC receptor rho1 expressed
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µM
Qualitative value
=
Quantitative value
1.9
Measurement pX
5.72
Target Name
Gamma-aminobutyric acid receptor subunit delta;+Gamma-aminobutyric acid receptor subunit beta-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-2; Gamma-aminobutyric acid receptor subunit delta
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory activity against Gamma-aminobutyric-acid A receptor
Substance RN
606417View in Reaxys
Measurement Parameter
qualitative
Qualitative value
Not Published
Target Name
Gamma-aminobutyric acid receptor subunit delta;+Gamma-aminobutyric acid receptor subunit beta-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-2; Gamma-aminobutyric acid receptor subunit delta
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration against GABAA receptor
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
=
Quantitative value
0.006
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
155/181
2018-08-03 18:12:50
345 of 403
346 of 403
347 of 403
Measurement pX
8.22
Target Name
Gamma aminobutyric acid B receptor
Target Synonyms
gamma aminobutyric acid b receptor
Target, Subunit, Species
Gamma aminobutyric acid B receptor
Target Mutant/Chimera Details
Gamma aminobutyric acid B receptor:Wild
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonistic activity towards gamma-aminobutyric acid B receptor
Substance RN
606417View in Reaxys
Measurement Parameter
Activity
Qualitative value
ND
Target Name
Gamma-aminobutyric acid receptor subunit delta;+Gamma-aminobutyric acid receptor subunit beta-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-2; Gamma-aminobutyric acid receptor subunit delta
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonistic activity towards gamma-aminobutyric acid A receptor
Substance RN
606417View in Reaxys
Measurement Parameter
Activity
Qualitative value
ND
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro maximal GABA (100 uM) agonistic response at wild-type human GABA receptor rho1 expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
156/181
2018-08-03 18:12:50
348 of 403
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
Rmax
Unit
%
Qualitative value
=
Quantitative value
104
Deviation
6
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration of the compound against GABA uptake in rat brain slices was determined
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
ÂľM
Measurement Object
GABA uptake
Qualitative value
=
Quantitative value
2500
Measurement pX
2.6
Hog, Signe; Greenwood, Jeremy R.; Madsen, Karsten B.; Larsson, Orla M.; Frolund, Bente; Schousboe, Arne; Krogsgaard-Larsen, Povl; Clausen, Rasmus P.; Current Topics in Medicinal Chemistry; vol. 6; nb. 17; (2006); p. 1861 - 1882, View in Reaxys 349 of 403
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro maximal GABA (100 uM) agonistic response at human GABA receptor rho1 expressed HEK 293 cell line upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
HEK293 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
Rmax
Unit
%
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
157/181
2018-08-03 18:12:50
350 of 403
351 of 403
Qualitative value
=
Quantitative value
101
Deviation
5
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at human GABA receptor rho1 expressed HEK 293 cell line upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
HEK293 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
pEC50
Quantitative value
5.7
Measurement pX
5.7
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration of the compound against GABA uptake in cerebrocortical astrocytes was determined
Cells/Cell Lines
Brain cerebrocortical astrocyte
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
ÂľM
Measurement Object
GABA uptake
Qualitative value
=
Quantitative value
2000
Measurement pX
2.7
Hog, Signe; Greenwood, Jeremy R.; Madsen, Karsten B.; Larsson, Orla M.; Frolund, Bente; Schousboe, Arne; Krogsgaard-Larsen, Povl; Clausen, Rasmus P.; Current Topics in Medicinal Chemistry; vol. 6; nb. 17; (2006); p. 1861 - 1882, View in Reaxys 352 of 403
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
158/181
2018-08-03 18:12:50
353 of 403
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at human GABA receptor rho1 expressed HEK 293 cell line upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
HEK293 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µM
Qualitative value
=
Quantitative value
2.2
Measurement pX
5.66
Target Name
Gamma-aminobutyric acid receptor subunit delta [rat];+Gamma-aminobutyric acid receptor subunit beta-2 [rat];+Gamma-aminobutyric acid receptor subunit alpha-1 [rat]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
p18506 + p63138 + p62813
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [rat]; Gamma-aminobutyric acid receptor subunit beta-2 [rat]; Gamma-aminobutyric acid receptor subunit delta [rat]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [rat]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [rat]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [rat]:Wild
Target Species (Bioactivity)
rat
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards GABAA receptor in rat brain synaptic membranes using [3H]muscimol as radioligand
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
Ki (inhibition constant)
Unit
µM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound name
[3H]Muscimol
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
159/181
2018-08-03 18:12:50
354 of 403
355 of 403
Concomitants: Compound role
RAD
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA agonistic response at human GABAA receptor alpha1beta2gamma2S expressed in Xenopus oocytes using two-electrode voltage-clamp technique
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
ÂľM
Qualitative value
=
Quantitative value
4
Measurement pX
5.4
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at wild-type human GABA receptor rho1 expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
160/181
2018-08-03 18:12:50
356 of 403
357 of 403
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
ÂľM
Qualitative value
=
Quantitative value
0.62
Measurement pX
6.21
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at wild-type human GABA receptor rho1 expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
pEC50
Quantitative value
6.2
Measurement pX
6.2
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target Uniprot ID
o14764 + p47870 + p14867
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
161/181
2018-08-03 18:12:50
358 of 403
359 of 403
Bioassay Details
Percent maximal agonistic response of GABA at human GABAA receptor alpha1beta2gamma2S expressed in Xenopus oocytes using two-electrode voltage-clamp technique
Biological Species/NCBI ID
human
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
Rmax
Unit
%
Qualitative value
=
Quantitative value
100
Concomitants: Compound name
GABA
Concomitants: Compound role
COM
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated:Substitution
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at mutant human GABA receptor rho1 S168T expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
pEC50
Quantitative value
4.6
Measurement pX
4.6
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated:Substitution
Target Species (Bioactivity)
human
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
162/181
2018-08-03 18:12:50
360 of 403
361 of 403
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro effective concentration of the compound required for GABA (100 uM) agonistic response at mutant human GABA receptor rho1 S168T expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µM
Qualitative value
=
Quantitative value
24
Measurement pX
4.62
Target Name
Gamma-aminobutyric acid receptor subunit delta [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human]
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]; Gamma-aminobutyric acid receptor subunit delta [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Mutated:Substitution + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated:Substitution
Target Species (Bioactivity)
human
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro maximal GABA (100 uM) agonistic response at mutant human GABA receptor rho1 S168T expressed tsA-201 cells upon incubation in 20 mM HEPES buffer, pH 7.4 at 37 degree C for 30 min by FMP (FLIPR membrane potential) assay
Biological Species/NCBI ID
human
Cells/Cell Lines
tsA201 cell line
Substance RN
606417View in Reaxys
Measurement Parameter
Rmax
Unit
%
Measurement Object
maximal GABA (100 uM) agonistic response
Qualitative value
=
Quantitative value
96
Deviation
4
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration of the compound against GABA uptake in synaptosomes was determined
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
163/181
2018-08-03 18:12:50
Measurement Object
GABA uptake
Qualitative value
=
Quantitative value
320
Measurement pX
3.49
Hog, Signe; Greenwood, Jeremy R.; Madsen, Karsten B.; Larsson, Orla M.; Frolund, Bente; Schousboe, Arne; Krogsgaard-Larsen, Povl; Clausen, Rasmus P.; Current Topics in Medicinal Chemistry; vol. 6; nb. 17; (2006); p. 1861 - 1882, View in Reaxys 362 of 403
363 of 403
364 of 403
Target Name
Gamma-aminobutyric acid receptor subunit delta;+Gamma-aminobutyric acid receptor subunit beta-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit delta; gabrd; gamma-aminobutyric acid receptor subunit delta + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-2; Gamma-aminobutyric acid receptor subunit delta
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration of compound against GABA A receptor
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
=
Quantitative value
0.006
Measurement pX
8.22
Target Name
D-amino-acid oxidase
Target Synonyms
d-amino-acid oxidase; d-amino-acid oxidase activity; d-amino-acid:oxygen oxidoreductase (deaminating); daao; daao-1; damox; dao; dao1; l-amino acid:o2 oxidoreductase
Target, Subunit, Species
D-amino-acid oxidase
Target Mutant/Chimera Details
D-amino-acid oxidase:Wild
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro inhibitory concentration of the compound against D-amino acid oxidase (0.2 mg/ml) upon incubation with 20 mM Mops buffer (pH 8.1) at 37 degree C for 2 h
Substance RN
606417View in Reaxys
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
100
Measurement pX
1
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Tested for reduction in blood pressure into cats i.c.v.; active
Biological Species/NCBI ID
cat
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
164/181
2018-08-03 18:12:50
Substance Route of Adm.
intracerebroventricular administration
Qualitative Results
Acitve
Measurement Parameter
Activity
Measurement Object
Reduction in blood pressure
Qualitative value
@
P. Krogsgaard-Larsen; A. V. Christensen; Annual reports in medicinal chemistry; vol. 15; (1980); p. 41 - 50, View in Reaxys 365 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was evaluated for hallucinogenic activity; Active
Substance RN
606417View in Reaxys
Qualitative Results
Acitve
Measurement Parameter
Activity
Measurement Object
hallucinogenic activity
Qualitative value
@
M.A. Davis; Annual reports in medicinal chemistry; vol. 4; (1968); p. 13 - 27, View in Reaxys 366 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was tested for its ability to displace GABA receptor ligand; potent
Substance RN
606417View in Reaxys
Measurement Parameter
Activity
Qualitative value
ND
Jeffrey K. Saelens; Fredric J. Vinick; Annual reports in medicinal chemistry; vol. 13; (1978); p. 31 - 40, View in Reaxys 367 of 403
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Tested for agonistic activity towards gamma-amino butyric acid receptor; powerful agonist
Substance RN
606417View in Reaxys
Qualitative Results
Powerful agonist
Measurement Parameter
Activity
Qualitative value
@
P. Krogsgaard-Larsen; A. V. Christensen; Annual reports in medicinal chemistry; vol. 15; (1980); p. 41 - 50, View in Reaxys 368 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ability of compound to protect animals against audiogenic convulsion and those induced by electro-shock; active
Substance RN
606417View in Reaxys
Qualitative Results
Acitve
Measurement Parameter
Activity
Qualitative value
@
P. Krogsgaard-Larsen; A. V. Christensen; Annual reports in medicinal chemistry; vol. 15; (1980); p. 41 - 50, View in Reaxys 369 of 403
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonistic activity of the compound towards gamma-aminobutyric acid receptor; Active
Substance RN
606417View in Reaxys
Qualitative Results
Active
Measurement Parameter
Activity
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
165/181
2018-08-03 18:12:50
Qualitative value
@
S.J. Enna; Annual reports in medicinal chemistry; vol. 14; (1979); p. 41 - 50, View in Reaxys 370 of 403
371 of 403
372 of 403
Target Name
Gamma-aminobutyric acid receptor subunit rho-1 [human]
Target Synonyms
gaba(a) receptor subunit rho-1; gaba(c) receptor; gabrr1; gamma-aminobutyric acid receptor subunit rho-1
Target Uniprot ID
p24046
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit rho-1 [human]
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit rho-1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required to measure electrical currents in XENOPUS OOCYTES expressing human GABA RHO1 RECEPTOR upon incubation in 5 mM HEPES buffer, pH 7.5 determined by two-electrode voltage clamp assay
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µM
Measurement Object
Gaba-Stimulated Currents
Qualitative value
=
Quantitative value
2.3
Measurement pX
5.64
Target Name
ionotropic gamma aminobutyric acid a receptor [human]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [human]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required to measure electrical currents in XENOPUS OOCYTES expressing human GABAA RECEPTOR upon incubation in 5 mM HEPES buffer, pH 7.5 was determined by two-electrode voltage clamp assay
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µM
Measurement Object
Gaba-Stimulated Currents
Qualitative value
=
Quantitative value
27
Measurement pX
4.57
Target Name
ionotropic gamma aminobutyric acid a receptor [mouse]
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
166/181
2018-08-03 18:12:50
373 of 403
374 of 403
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [mouse]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [mouse]:Wild
Target Species (Bioactivity)
mouse
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Dissociation constant of compound towards displacement of 5 nM [3H]muscimol from mouse brain membrane fraction expressing GABAA RECEPTOR upon incubation for 45 min at 4 degree C was determined by liquid scintillation counting assay
Cells/Cell Lines
brain membranes
Substance RN
606417View in Reaxys
Measurement Parameter
Kd (dissociation constant)
Unit
nM
Qualitative value
=
Quantitative value
15.2
Measurement pX
7.82
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI ID
rat
Organs/Tissues
brain cortex
Cell Fraction
Synaptosome: membrane (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Table 2, Entry muscimol; Table 4, Entry Muscimol
Measurement Parameter
Ki (inhibition constant)
Unit
ÂľM
Quantitative value
0.006
Measurement pX
8.22
Concomitants: Compound RN
774694
Concomitants: Compound name
[3H]-Muscimol
Concomitants: Compound role
RAD
Target Name
GABA receptor [rat]
Target Synonyms
gaba receptor
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
167/181
2018-08-03 18:12:50
375 of 403
Target, Subunit, Species
GABA receptor [rat]
Target Mutant/Chimera Details
GABA receptor [rat]:Wild
Target Species (Bioactivity)
rat
Target Transfection
Non Transfected
Substance Action on Target
Antagonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Flux uptake
Biological Species/NCBI ID
rat
Organs/Tissues
brain
Cell Fraction
Synaptosome (P2 fraction)
Substance RN
606417View in Reaxys
Substance Name
Table 2, Entry muscimol; Table 4, Entry Muscimol
Measurement Parameter
EC50
Unit
µM
Measurement Object
uptake
Quantitative value
0.54
Measurement pX
6.27
Concomitants: Compound RN
906818
Concomitants: Compound name
[3H]-GABA
Concomitants: Compound role
SUB
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2;+Gamma-aminobutyric acid receptor subunit beta-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-2; Gamma-aminobutyric acid receptor subunit gamma-2
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
100 μM
Measurement Parameter
% Activation
Qualitative value
Active
Measurement pX
4
Patent; THE JOHNS HOPKINS UNIVERSITY; BOSMANS, Frank; WO2014/120994; (2014); (A1) English, View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
168/181
2018-08-03 18:12:50
376 of 403
377 of 403
Target Name
Gamma-aminobutyric acid receptor subunit beta-3;+Gamma-aminobutyric acid receptor subunit gamma-2;+Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit beta-3; gabrb-3; gabrb3; gamma-aminobutyric acid receptor subunit beta-3 + gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2 + gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1; Gamma-aminobutyric acid receptor subunit beta-3; Gamma-aminobutyric acid receptor subunit gamma-2
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Target Transfection
Transfected
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
Neuro-2a cell line
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
200 μM
Measurement Parameter
inhibition rate
Unit
%
Qualitative value
~
Quantitative value
80
Measurement pX
4.3
Concomitants: Compound RN
28666812; 906818
Concomitants: Compound name
β-cobratoxin Naja kaouthia cobra; β-aminobutyric acid
Concomitants: Compound role
IND; IND
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of plasma protein extravasation following trigeminal electrical stimulation in rats at compound dose of 1 mg/kg to that of unstimulated animals
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
ratio
Qualitative value
=
Quantitative value
1.06
Patent; MOSKOWITZ Michael A.; WO1996/15782; (A1); (1996), View in Reaxys 378 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Reduction in leakage ratio in rat duramater induced by electrical trigeminal stimulation at compound dose of 10 ug/kg, i.v.
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
ratio
Measurement Object
Reduction in leakage ratio
Qualitative value
=
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
169/181
2018-08-03 18:12:50
Quantitative value
1.44
Patent; MOSKOWITZ Michael A.; WO1996/15782; (A1); (1996), View in Reaxys 379 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration required to reduce substance P induced (1 nM/kg, i.v.) plasma protein extravasation in rats
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
µg/kg
Qualitative value
=
Quantitative value
385
Patent; MOSKOWITZ Michael A.; WO1996/15782; (A1); (1996), View in Reaxys 380 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective dose of the compound required to reduce leakage in rat duramater induced by electrical trigeminal stimulation administered by i.v. 30 mins prior to stimulation
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
ED50
Unit
µg/kg
Qualitative value
=
Quantitative value
58
Patent; MOSKOWITZ Michael A.; WO1996/15782; (A1); (1996), View in Reaxys 381 of 403
Target Name
GABA-A receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor
Target, Subunit, Species
GABA-A receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild
Substance Action on Target
Agonist
Substance Effect
agonistic activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Agonistic activity of the compound towards GABAA receptor
Substance RN
606417View in Reaxys
Qualitative Results
Not Published
Measurement Parameter
qualitative
Qualitative value
Not Published
Patent; MOSKOWITZ Michael A.; WO1996/15782; (A1); (1996), View in Reaxys 382 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Extravasation ratio determined as electrical trigeminal stimulated [125I]-BSA within the dura mater in rat to that of unstimulated upon i.v administration at 1 mg/kg compound concentration
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
ratio
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
170/181
2018-08-03 18:12:50
Qualitative value
=
Quantitative value
1.06
Patent; Moskowitz Michael A.; EP1839657; (A2); (2007), View in Reaxys 383 of 403
Target Name
GABA-A receptor
Target Synonyms
gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor
Target, Subunit, Species
GABA-A receptor
Target Mutant/Chimera Details
GABA-A receptor:Wild
Substance Action on Target
Inhibitor
Substance Effect
inhibitory activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory activity against GABAA receptor
Substance RN
606417View in Reaxys
Qualitative Results
Not Published
Measurement Parameter
qualitative
Qualitative value
Not Published
Patent; Moskowitz Michael A.; EP1839657; (A2); (2007), View in Reaxys 384 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective dose of the compound required for decreased plasma protein extravasation in rat
Biological Species/NCBI ID
rat
Substance RN
606417View in Reaxys
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
Decreased plasma protein extravasation in rat
Qualitative value
=
Quantitative value
58
Patent; Moskowitz Michael A.; EP1839657; (A2); (2007), View in Reaxys 385 of 403
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required for reduced the SP-induced rat plasma protein extravasation
Biological Species/NCBI ID
rat
Cells/Cell Lines
plasma cell
Substance RN
606417View in Reaxys
Measurement Parameter
EC50
Unit
Âľg/kg
Measurement Object
SP-induced rat plasma protein extravasation
Qualitative value
=
Quantitative value
385
Patent; Moskowitz Michael A.; EP1839657; (A2); (2007), View in Reaxys 386 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
171/181
2018-08-03 18:12:50
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
50 μM
Measurement Parameter
% Cells
Unit
%
Measurement Object
chromaffin cells with raised [Ca2+]i
Quantitative value
29
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 387 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
50 μM
Measurement Parameter
% Cells
Unit
%
Measurement Object
chromaffin cells with decreased [Ca2+]i
Quantitative value
16
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 388 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
50 μM
Measurement Parameter
% Cells
Unit
%
Measurement Object
chromaffin cells with no change in [Ca2+]i
Quantitative value
7
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 389 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Increase
Measurement Object
resting calcium concentration [Ca2+]i in chromaffin cells
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
172/181
2018-08-03 18:12:50
Qualitative value
Active
Measurement pX
4.7
Concomitants: Compound RN
3587173
Concomitants: Compound name
calcium cation
Concomitants: Compound role
COM
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 390 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Increase
Measurement Object
resting calcium concentration [Ca2+]i in chromaffin cells
Qualitative value
Not active
Measurement pX
1
Concomitants: Compound RN
98786
Concomitants: Compound name
bicuculline
Concomitants: Compound role
ANT
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 391 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Increase
Measurement Object
resting calcium concentration [Ca2+]i in chromaffin cells
Qualitative value
Not active
Measurement pX
1
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 392 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
173/181
2018-08-03 18:12:50
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Increase
Measurement Object
chromaffin cells with spontaneous calcium fluctuations (SCFs)
Qualitative value
Active
Measurement pX
4.7
Concomitants: Compound RN
98786
Concomitants: Compound name
bicuculline
Concomitants: Compound role
ANT
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 393 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Decrease
Measurement Object
chromaffin cells with spontaneous calcium fluctuations (SCFs)
Qualitative value
Active
Measurement pX
4.7
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 394 of 403
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Wistar rat
Organs/Tissues
adrenal gland
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
20 μM
Measurement Parameter
% Increase
Measurement Object
chromaffin cells with spontaneous calcium fluctuations (SCFs)
Qualitative value
Active
Measurement pX
4.7
Concomitants: Compound RN
3587173
Concomitants: Compound name
calcium cation
Concomitants: Compound role
COM
Tzitzitlini, Alejandre-García; Pedro, Segura-Chama; Martha, Pérez-Armendáriz E.; Rodolfo, Delgado-Lezama; Arturo, Hernández-Cruz; Pflugers Archiv European Journal of Physiology; vol. 468; nb. 2; (2016); p. 351 - 365, View in Reaxys 395 of 403
Substance Effect
Memory enhancer
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
174/181
2018-08-03 18:12:50
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
% increase
Measurement Object
preference for novel object in 1st session
Qualitative value
Not active
Measurement pX
1
Kunisawa, Kazuo; Kido, Kiwamu; Nakashima, Natsuki; Matsukura, Takuya; Nabeshima, Toshitaka; Hiramatsu, Masayuki; European Journal of Pharmacology; vol. 796; (2017); p. 122 - 130, View in Reaxys 396 of 403
Substance Effect
Memory enhancer
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
% increase
Measurement Object
preference for novel object in 2nd session
Qualitative value
Active
Statistical sgnificance (Qualitative)
S
Kunisawa, Kazuo; Kido, Kiwamu; Nakashima, Natsuki; Matsukura, Takuya; Nabeshima, Toshitaka; Hiramatsu, Masayuki; European Journal of Pharmacology; vol. 796; (2017); p. 122 - 130, View in Reaxys 397 of 403
Substance Effect
Memory enhancer
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
% increase
Measurement Object
preference for novel object in 3rd session
Qualitative value
Active
Statistical sgnificance (Qualitative)
S
Kunisawa, Kazuo; Kido, Kiwamu; Nakashima, Natsuki; Matsukura, Takuya; Nabeshima, Toshitaka; Hiramatsu, Masayuki; European Journal of Pharmacology; vol. 796; (2017); p. 122 - 130, View in Reaxys 398 of 403
Substance Effect
Memory enhancer
Bioassay Category
In Vivo (Animal models)
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
175/181
2018-08-03 18:12:50
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
% change
Measurement Object
response to electric shock in training trial
Qualitative value
Not active
Measurement pX
1
Kunisawa, Kazuo; Kido, Kiwamu; Nakashima, Natsuki; Matsukura, Takuya; Nabeshima, Toshitaka; Hiramatsu, Masayuki; European Journal of Pharmacology; vol. 796; (2017); p. 122 - 130, View in Reaxys 399 of 403
Substance Effect
Memory enhancer
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
1 mg/kg
Substance Route of Adm.
subcutaneous administration
Measurement Parameter
% decrease
Measurement Object
stepdown latency
Qualitative value
Not active
Measurement pX
1
Kunisawa, Kazuo; Kido, Kiwamu; Nakashima, Natsuki; Matsukura, Takuya; Nabeshima, Toshitaka; Hiramatsu, Masayuki; European Journal of Pharmacology; vol. 796; (2017); p. 122 - 130, View in Reaxys 400 of 403
401 of 403
Target Name
Gamma-aminobutyric acid receptor subunit beta-2
Target Synonyms
gaba(a) receptor subunit beta-2; gabrb-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit beta-2
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit beta-2:Wild
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Xenopus
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Dose
5 ÎźM
Measurement Parameter
stimulation percentage
Qualitative value
Active
Measurement pX
5.3
Target Name
Gamma-aminobutyric acid receptor subunit gamma-2
Target Synonyms
gaba(a) receptor subunit gamma-2; gabrg2; gamma-aminobutyric acid receptor subunit gamma-2
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit gamma-2
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
176/181
2018-08-03 18:12:50
402 of 403
403 of 403
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit gamma-2:Wild
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Xenopus
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Dose
5 μM
Measurement Parameter
stimulation percentage
Qualitative value
Active
Measurement pX
5.3
Target Name
Gamma-aminobutyric acid receptor subunit alpha-1
Target Synonyms
gaba(a) receptor subunit alpha-1; gabra-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1
Target, Subunit, Species
Gamma-aminobutyric acid receptor subunit alpha-1
Target Mutant/Chimera Details
Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Substance Action on Target
Activator
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI ID
Xenopus
Cells/Cell Lines
oocyte
Substance RN
606417View in Reaxys
Substance Dose
5 μM
Measurement Parameter
stimulation percentage
Qualitative value
Active
Measurement pX
5.3
Target Name
ionotropic gamma aminobutyric acid a receptor [mouse]
Target Synonyms
ionotropic gamma aminobutyric acid a receptor
Target, Subunit, Species
ionotropic gamma aminobutyric acid a receptor [mouse]
Target Mutant/Chimera Details
ionotropic gamma aminobutyric acid a receptor [mouse]:Wild
Target Species (Bioactivity)
mouse
Target Transfection
Non Transfected
Substance Effect
Antidepressant-like effect
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI ID
ddY mouse
Substance RN
606417View in Reaxys
Substance Name
muscimol
Substance Dose
0.03 mg/kg
Substance Route of Adm.
intraperitoneal administration
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
177/181
2018-08-03 18:12:50
Substance Dosing Regimen
Single
Measurement Parameter
% Decrease
Measurement Object
immobility time (of control)
Qualitative value
Active
Reaxys ID 9899889 View in Reaxys HO
2/5
N
Linear Structure Formula: C4H5DN2O2 Molecular Formula: C4H6N2O2 Molecular Weight: 115.096 Type of Substance: heterocyclic InChI Key: ZJQHPWUVQPJPQT-VMNATFBRSA-N Note:
O
NH 2 2H
Substance Label (1) Label References 3b
Filer, Crist N.; Lacy, James M.; Peng; Synthetic Communications; vol. 35; nb. 7; (2005); p. 967 - 970, View in Reaxys
Druglikeness (1) 1 of 1
LogP
-0.473
H Bond Donors
2
H Bond Acceptors
1
Rotatable Bonds
1
TPSA
72.28
Lipinski Number
4
Veber Number
2
NMR Spectroscopy (1) 1 of 1
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
dimethylsulfoxide-d6
Frequency (NMR Spectro- 300 scopy) [MHz] Filer, Crist N.; Lacy, James M.; Peng; Synthetic Communications; vol. 35; nb. 7; (2005); p. 967 - 970, View in Reaxys
Reaxys ID 9899888 View in Reaxys HO
3/5 Chemical Name: [methylene-3H1] muscimol Linear Structure Formula: C4H5TN2O2 Molecular Formula: C4H6N2O2 Molecular Weight: 116.096 Type of Substance: heterocyclic InChI Key: ZJQHPWUVQPJPQT-FUPOQFPWSA-N Note:
N O
NH 2 3
H
Substance Label (1) Label References 3a
Filer, Crist N.; Lacy, James M.; Peng; Synthetic Communications; vol. 35; nb. 7; (2005); p. 967 - 970, View in Reaxys
Druglikeness (1)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
178/181
2018-08-03 18:12:50
1 of 1
LogP
-0.473
H Bond Donors
2
H Bond Acceptors
1
Rotatable Bonds
1
TPSA
72.28
Lipinski Number
4
Veber Number
2
NMR Spectroscopy (1) 1 of 1
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
3H
Filer, Crist N.; Lacy, James M.; Peng; Synthetic Communications; vol. 35; nb. 7; (2005); p. 967 - 970, View in Reaxys
Reaxys ID 4547459 View in Reaxys
4/5 Cl
CAS Registry Number: 3579-03-1 Linear Structure Formula: C4H6N2O2*ClH Molecular Formula: C4H6N2O2*ClH Molecular Weight: 150.565 Type of Substance: heterocyclic InChI Key: IIDOLBNZAZXSHC-UHFFFAOYSA-N Note:
H
N
HO
O
NH 2
Substance Label (1) Label References 1*HCl
Jaeger; Frey; Liebigs Annalen der Chemie; vol. No. 4; (1982); p. 817 - 820, View in Reaxys
Druglikeness (1) 1 of 1
LogP
0.039
H Bond Donors
2
H Bond Acceptors
1
Rotatable Bonds
1
TPSA
72.28
Lipinski Number
4
Veber Number
2
Reaxys ID 3998136 View in Reaxys
5/5 CAS Registry Number: 18174-72-6 Chemical Name: muscimol hydrobromide; 5-aminomethyl-isoxazol-3-one; hydrobromide; 5-Aminomethyl-3-isoxaolol-hydrobromid; muscimol; hydrobromide Linear Structure Formula: C4H6N2O2*BrH Molecular Formula: BrH*C4H6N2O2 Molecular Weight: 195.016 Type of Substance: heterocyclic InChI Key: OPZOJWHOZRKYQX-UHFFFAOYSA-N Note:
N HO
O Br
H
NH 2
Substance Label (2) Label References
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
179/181
2018-08-03 18:12:50
5a
Liu, Genyan; Ozoe, Fumiyo; Furuta, Kenjiro; Ozoe, Yoshihisa; Journal of Agricultural and Food Chemistry; vol. 63; nb. 28; (2015); p. 6304 - 6312, View in Reaxys
7
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys
Druglikeness (1) 1 of 1
LogP
0.377
H Bond Donors
2
H Bond Acceptors
1
Rotatable Bonds
1
TPSA
72.28
Lipinski Number
4
Veber Number
2
Melting Point (1) 1 of 1
Melting Point [°C]
179 - 181
Solvent (Melting Point)
diethyl ether; methanol
Comment (Melting Point)
Decomposition
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys Crystal Property Description (1) Colour & Other References Properties brown
Liu, Genyan; Ozoe, Fumiyo; Furuta, Kenjiro; Ozoe, Yoshihisa; Journal of Agricultural and Food Chemistry; vol. 63; nb. 28; (2015); p. 6304 - 6312, View in Reaxys
NMR Spectroscopy (3) 1 of 3
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
dimethylsulfoxide-d6
Frequency (NMR Spectro- 400 scopy) [MHz] Liu, Genyan; Ozoe, Fumiyo; Furuta, Kenjiro; Ozoe, Yoshihisa; Journal of Agricultural and Food Chemistry; vol. 63; nb. 28; (2015); p. 6304 - 6312, View in Reaxys 2 of 3
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
dimethylsulfoxide-d6
Frequency (NMR Spectro- 100 scopy) [MHz] Liu, Genyan; Ozoe, Fumiyo; Furuta, Kenjiro; Ozoe, Yoshihisa; Journal of Agricultural and Food Chemistry; vol. 63; nb. 28; (2015); p. 6304 - 6312, View in Reaxys 3 of 3
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys IR Spectroscopy (1)
Copyright © 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
180/181
2018-08-03 18:12:50
1 of 1
Description (IR Spectroscopy)
Bands
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys Mass Spectrometry (1) Description (Mass References Spectrometry) high resolution mass spectrometry (HRMS); electrospray ionisation (ESI); spectrum
Liu, Genyan; Ozoe, Fumiyo; Furuta, Kenjiro; Ozoe, Yoshihisa; Journal of Agricultural and Food Chemistry; vol. 63; nb. 28; (2015); p. 6304 - 6312, View in Reaxys
UV/VIS Spectroscopy (1) 1 of 1
Description (UV/VIS Spectroscopy)
Absorption maxima
Krogsgaard-Larsen,P.; Christensen,S.B.; Acta Chemica Scandinavica, Series B: Organic Chemistry and Biochemistry; vol. 30; (1976); p. 281-282percent, View in Reaxys
Copyright Š 2018 Elsevier Life Sciences IP Limited except certain content provided by third parties. Reaxys is a trademark of Elsevier Life Sciences IP Limited.
181/181
2018-08-03 18:12:50