Query Query
1. Query N
O
Results
Date
5 substances in Reaxys
2018-02-14 06h:58m:30s (EST)
1 substances in Reaxys
2018-02-14 07h:00m:33s (EST)
Search as: As drawn 2. Query
(1. Query) AND itemno in (1)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Reaxys ID 9348161 View in Reaxys
N
1/1 Chemical Name: 1-pentyl-3-(1-naphthoyl)indole; naphthalen‐1‐ yl‐(1‐pentylindol‐3‐yl)methanone; (1-naphthalenyl)-(1-pentyl-1Hindol-3-yl)methanone; (1-pentyl-1H-indol-3-yl)-1-naphthalenylmethanone; (1-pentyl-1H-indole-3-yl)-1-naphthalenylmethanone; (1-pentyl-1H-indol-3-yl)-1-naphthalenylmethanone; naphthalen-1-yl(1-pentyl-1H-indol-3-yl)methanone Linear Structure Formula: C24H23NO Molecular Formula: C24H23NO Molecular Weight: 341.453 Type of Substance: heterocyclic InChI Key: JDNLPKCAXICMBW-UHFFFAOYSA-N Note:
O
Substance Label (8) Label References JWH-018
Patent; Randox Laboratories Ltd.; EP2487155; (2012); (A1) English, View in Reaxys; Wohlfarth, Ariane; Scheidweiler, Karl B; Chen, Xiaohong; Liu, Hua-Fen; Huestis, Marilyn A.; Analytical Chemistry; vol. 85; nb. 7; (2013); p. 3730 - 3738, View in Reaxys; Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS; THE UNIVERSITY OF KANSAS; PRATHER, Paul, L.; PRISINZANO, Thomas, E.; FANTEGROSSI, William, E.; BRENTS, Lisa, K.; MORAN, Jeffery; RADOMINSKA-PANDYA, Anna; VASILJEVIK, Tamara; WO2013/106349; (2013); (A1) English, View in Reaxys; Cannaert, Annelies; Storme, Jolien; Franz, Florian; Auwärter, Volker; Stove, Christophe P.; Analytical Chemistry; vol. 88; nb. 23; (2016), View in Reaxys; Hruba, Lenka; McMahon, Lance R.; Journal of Pharmacology and Experimental Therapeutics; vol. 362; nb. 2; (2017); p. 278 - 286, View in Reaxys
JWH‐018
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys
1-4p
Seltzman, Herbert H.; Shiner, Craig; Hirt, Erin E.; Gilliam, Anne F.; Thomas, Brian F.; Maitra, Rangan; Snyder, Rod; Black, Sherry L.; Patel, Purvi R.; Mulpuri, Yatendra; Spigelman, Igor; Journal of Medicinal Chemistry; vol. 59; nb. 16; (2016); p. 7525 - 7543, View in Reaxys
C
Canazza, Isabella; Ossato, Andrea; Trapella, Claudio; Fantinati, Anna; De Luca, Maria Antonietta; Margiani, Giulia; Vincenzi, Fabrizio; Rimondo, Claudia; Di Rosa, Fabiana; Gregori, Adolfo; Varani, Katia; Borea, Pier Andrea; Serpelloni, Giovanni; Marti, Matteo; Psychopharmacology; vol. 233; nb. 21-22; (2016); p. 3685 - 3709, View in Reaxys
25
Rusch, Fabian; Schober, Jan-Christian; Brasholz, Malte; ChemCatChem; vol. 8; nb. 18; (2016); p. 2881 2884, View in Reaxys
1
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; RESEARCH TRIANGLE INSTITUTE; SPIGELMAN, Igor; SELTZMAN, Herbert, H.; SHINER, Craig; WO2014/15298; (2014); (A1) English, View in Reaxys; Thaxton, Amber; Belal, Tarek S.; Smith, Forrest; DeRuiter, Jack; Abdel-Hay, Karim M.; Clark, C. Randall; Rapid Communications in Mass Spectrometry; vol. 29; nb. 9; (2015); p. 871 - 877, View in Reaxys
4; JWH-018
Banister, Samuel D.; Wilkinson, Shane M.; Longworth, Mitchell; Stuart, Jordyn; Apetz, Nadine; English, Katrina; Brooker, Lance; Goebel, Catrin; Hibbs, David E.; Glass, Michelle; Connor, Mark; McGregor, Iain S.; Kassiou, Michael; ACS Chemical Neuroscience; vol. 4; nb. 7; (2013); p. 1081 - 1092, View in Reaxys
5
Huffman, John W.; Mabon, Ross; Wu, Ming-Jung; Lu, Jianzhong; Hart, Richard; Hurst, Dow P.; Reggio, Patricia H.; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 11; nb. 4; (2003); p. 539 - 549, View in Reaxys
Patent-Specific Data (1) References Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; RESEARCH TRIANGLE INSTITUTE; SPIGELMAN, Igor; SELTZMAN, Herbert, H.; SHINER, Craig; WO2014/15298; (2014); (A1) English, View in Reaxys Druglikeness (1) 1 of 1
LogP
7.136
H Bond Donors
0
H Bond Acceptors
2
Rotatable Bonds
6
TPSA
22
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Lipinski Number
3
Veber Number
2
Highest Clinical Phase (1) Highest Clinical Phase Preclinical Melting Point (1) 1 of 1
Melting Point [°C]
65 - 67
Denton, Justin R.; Synthesis; nb. 5; (2010); p. 775 - 782; Art.No: M05709SS, View in Reaxys Chromatographic Data (2) Chromatographic References data SFC (Supercritical fluid chromatography)
Toyo'Oka, Toshimasa; Kikura-Hanajiri, Ruri; Chemical and Pharmaceutical Bulletin; vol. 63; nb. 10; (2015); p. 762 - 769, View in Reaxys
HPLC (High performance liquid chromatography)
Wohlfarth, Ariane; Scheidweiler, Karl B; Chen, Xiaohong; Liu, Hua-Fen; Huestis, Marilyn A.; Analytical Chemistry; vol. 85; nb. 7; (2013); p. 3730 - 3738, View in Reaxys
Crystal Property Description (3) Colour & Other Location Properties colourless
Page/Page column 1
References Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS; THE UNIVERSITY OF KANSAS; PRATHER, Paul, L.; PRISINZANO, Thomas, E.; FANTEGROSSI, William, E.; BRENTS, Lisa, K.; MORAN, Jeffery; RADOMINSKA-PANDYA, Anna; VASILJEVIK, Tamara; WO2013/106349; (2013); (A1) English, View in Reaxys
brown
Lai, Qiu Yu; Liao, Rong Su; Wu, Shao Yong; Zhang, Jia Xin; Duan, Xin Hong; New Journal of Chemistry; vol. 37; nb. 12; (2013); p. 4069 - 4076, View in Reaxys
white
Denton, Justin R.; Synthesis; nb. 5; (2010); p. 775 - 782; Art.No: M05709SS, View in Reaxys
NMR Spectroscopy (1) 1 of 1
Description (NMR Spec- Chemical shifts troscopy) Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectro- chloroform-d1 scopy) Frequency (NMR Spectroscopy) [MHz]
400
Denton, Justin R.; Synthesis; nb. 5; (2010); p. 775 - 782; Art.No: M05709SS, View in Reaxys Mass Spectrometry (9) Description (Mass References Spectrometry) electrospray ioni- Thaxton, Amber; Belal, Tarek S.; Smith, Forrest; DeRuiter, Jack; Abdel-Hay, Karim M.; Clark, C. Ransation (ESI); frag- dall; Rapid Communications in Mass Spectrometry; vol. 29; nb. 9; (2015); p. 871 - 877, View in Reaxys mentation pattern; spectrum tandem mass spectrometry; electrospray ionisation (ESI); spectrum
Toyo'Oka, Toshimasa; Kikura-Hanajiri, Ruri; Chemical and Pharmaceutical Bulletin; vol. 63; nb. 10; (2015); p. 762 - 769, View in Reaxys
electrospray ionisation (ESI); tandem mass spectrometry; liquid chromatography mass spectrome-
Wohlfarth, Ariane; Scheidweiler, Karl B; Chen, Xiaohong; Liu, Hua-Fen; Huestis, Marilyn A.; Analytical Chemistry; vol. 85; nb. 7; (2013); p. 3730 - 3738, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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try (LCMS); spectrum HRMS (High resolution mass spectrometry); Spectrum
Gottardo, Rossella; Chiarini, Anna; Dal Pra, Ilaria; Seri, Catia; Rimondo, Claudia; Serpelloni, Giovanni; Armato, Ubaldo; Tagliaro, Franco; Journal of Mass Spectrometry; vol. 47; nb. 1; (2012); p. 141 - 146, View in Reaxys
MALDI-TOF (Ma- Gottardo, Rossella; Chiarini, Anna; Dal Pra, Ilaria; Seri, Catia; Rimondo, Claudia; Serpelloni, Giovanni; trix assisted laser Armato, Ubaldo; Tagliaro, Franco; Journal of Mass Spectrometry; vol. 47; nb. 1; (2012); p. 141 - 146, desorption ioniza- View in Reaxys tion - time of flight); Spectrum LCMS (Liquid chromatography mass spectrometry); ESI (Electrospray ionisation); IT (ion trap); Tandem mass spectrometry; Spectrum
Hutter; Broecker; Kneisel; Auwaerter; Journal of Mass Spectrometry; vol. 47; nb. 1; (2012); p. 54 - 65, View in Reaxys
LCMS (Liquid chromatography mass spectrometry); TOFMS (Time of flight mass spectrum); HRMS (High resolution mass spectrometry); Spectrum
Grabenauer, Megan; Krol, Wojciech L.; Wiley, Jenny L.; Thomas, Brian F.; Analytical Chemistry; vol. 84; nb. 13; (2012); p. 5574 - 5581, View in Reaxys
LCMS (Liquid chromatography mass spectrometry); Tandem mass spectrometry; QIT (quadrupole ion trap); Spectrum
Dresen, Sebastian; Kneisel, Stefan; Weinmann, Wolfgang; Zimmermann, Ralf; Auwarter, Volker; Journal of Mass Spectrometry; vol. 46; nb. 2; (2011); p. 163 - 171, View in Reaxys
EI (Electron imAuwaerter; Journal of Mass Spectrometry; vol. 44; nb. 5; (2009); p. 832 - 837, View in Reaxys pact); GCMS (Gas chromatography mass spectrometry); Spectrum Medchem (101) 1 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Electrophysiology
Bioassay Details
Effect : excitatory postsynaptic current neurotransmissionTarget : CB1 receptor Bioassay : glutamatergic autaptic neuronsmaximal inhibition 48% at 1μmol/l
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Substance Name
38203
Measurement Parameter
IC50
Unit
nM
Quantitative value
4.8 - 45.9
Measurement pX
8.32
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Atwood, Brady K; Huffman, John; Straiker, Alex; MacKie, Ken; British Journal of Pharmacology; vol. 160; nb. 3; (2010); p. 585 - 593, View in Reaxys 2 of 101
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1 Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : CB1 receptor internalization internalization measured after 3h exposure at 100 nmol/l and after 2h exposure at 1μmol/l
Cells/Cell Lines
HEK 293
Substance RN
9348161View in Reaxys
Substance Name
38203
Substance Dose
100 nM
Qualitative Results
internalization rate 54.7 - 61.9 percent
Measurement Parameter
Qualitative
Atwood, Brady K; Huffman, John; Straiker, Alex; MacKie, Ken; British Journal of Pharmacology; vol. 160; nb. 3; (2010); p. 585 - 593, View in Reaxys 3 of 101
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1 Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : CB1 receptor internalization
Cells/Cell Lines
HEK 293
Substance RN
9348161View in Reaxys
Substance Name
38203
Measurement Parameter
EC50
Unit
nM
Quantitative value
1.6 - 6.3
Measurement pX
8.8
Atwood, Brady K; Huffman, John; Straiker, Alex; MacKie, Ken; British Journal of Pharmacology; vol. 160; nb. 3; (2010); p. 585 - 593, View in Reaxys 4 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : CB1 receptor-mediated enzyme activation Target : CB1 receptor cannabinoid receptor 1HBS: HEPES buffered saline; BSA: bovine serum albumin; MAPK: ERK1/2 mitogen activated protein kinase
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Cells/Cell Lines
HEK 293
Substance RN
9348161View in Reaxys
Substance Name
38203
Measurement Parameter
EC50
Unit
nM
Quantitative value
1.6 - 12.5
Measurement pX
8.8
Atwood, Brady K; Huffman, John; Straiker, Alex; MacKie, Ken; British Journal of Pharmacology; vol. 160; nb. 3; (2010); p. 585 - 593, View in Reaxys 5 of 101
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI Sprague Dawley rat ID
6 of 101
Organs/Tissues
brain cortex
Cell Fraction
Membrane
Substance RN
9348161View in Reaxys
Substance Name
18
Substance Dose
0.100000 nM
Measurement Parameter
Ki
Unit
nM
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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7 of 101
Target Species (Bioactivity)
human
Target Transfection
Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Cells/Cell Lines
CHO
Cell Fraction
Membrane
Substance RN
9348161View in Reaxys
Substance Name
18
Substance Dose
0.100000 nM
Measurement Parameter
Ki
Unit
nM
Quantitative value
2.94
Deviation
2.65000
Measurement pX
8.53
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940
Concomitants: Compound role
NSB; RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI Sprague Dawley rat ID Organs/Tissues
brain
Cell Fraction
Cytoplasmic membrane
Substance RN
9348161View in Reaxys
Substance Name
14
Measurement Parameter
Ki
Unit
nM
Quantitative value
9
Deviation
5
Measurement pX
8.05
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8 of 101
Concomitants: Compound RN
6659789; 6659789
Concomitants: Compound name
CP 55940; [3H]-CP 55940; Tris EDTA
Concomitants: Compound role
NSB; RAD; COM
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
9348161View in Reaxys
Substance Name
14
Substance Route of Adm.
intravenous administration
Substance Dosing Regi- Single men
9 of 101
Measurement Parameter
ED50
Unit
µmol/kg
Quantitative value
0.44
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
9348161View in Reaxys
Substance Name
14
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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10 of 101
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
max effect
Qualitative value
#
Quantitative value
0.09
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID
11 of 101
Substance RN
9348161View in Reaxys
Substance Name
14
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
max effect
Quantitative value
1.7
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Spontaneous activity
Biological Species/NCBI Institute for Cancer Research mouse ID Substance RN
9348161View in Reaxys
Substance Name
14
Measurement Parameter
ED50
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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12 of 101
Unit
µmol/kg
Measurement Object
max effect
Quantitative value
3.9
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Target Transfection
Non Transfected
Substance Effect
Antiinflammatory: non-steroidal
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI Sprague Dawley rat ID Substance RN
9348161View in Reaxys
Substance Name
14
Substance Route of Adm.
oral administration
Substance Dosing Regi- Repeated men
13 of 101
Measurement Parameter
ED50
Qualitative value
ND
Concomitants: Compound RN
6659789; 4354308
Concomitants: Compound name
CP 55940; Delta9-THC
Concomitants: Compound role
TRA; TRA
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Percent maximum efficacy of the compound (dissolved in DMSO) towards excitatory postsynaptic potentials (fEPSPs) in rat Coronal prelimbic prefrontal cortex (PFC) slices upon incubation for 20 min at 31 degree C
Biological Species/NCBI Rattus norvegicus ID Cells/Cell Lines
Brain prefrontal cortical cell
Substance RN
9348161View in Reaxys
Measurement Parameter
Emax(%)
Unit
%
Measurement Object
Excitatory Post-Synaptic Field Potentials
Qualitative value
=
Quantitative value
73.5
Deviation
10.8
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 14 of 101
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of compound towards human Cannabinoid receptor 2 stably transfected in CHO cells using [3H]CP-55940 as radioligand determined by LIQUID SCINTILLATION COUNTING ASSAY
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.2
Measurement pX
8.2
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 15 of 101
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of Binding affinity of compound towards human Cannabinoid receptor 2 to that of human Cannabinoid receptor 1 stably transfected in CHO cells using [3H]CP-55940 as radioligand determined by LIQUID SCINTILLATION COUNTING ASSAY
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Parameter
Qualitative
Qualitative value
Not Published
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 16 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory concentration of the compound (dissolved in DMSO) against excitatory postsynaptic potentials (fEPSPs) in male Wistar rat Coronal prelimbic prefrontal cortex (PFC) slices upon incubation for 20 min at 31 degree C
Biological Species/NCBI Rattus norvegicus ID Cells/Cell Lines
Brain prefrontal cortical cell
Substance RN
9348161View in Reaxys
Measurement Parameter
IC50
Unit
µM
Measurement Object
Excitatory Post-Synaptic Field Potentials
Qualitative value
=
Quantitative value
0.28
Measurement pX
6.55
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 17 of 101
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of the compound required for cAMP accumulation in CHO cells stably transfected with human Cannabinoid receptor 2 in presence of 0.3 uM forskolin upon incubation for 20 min at 37 degree C
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
pEC50
Measurement Object
cAMP Accumulation
Quantitative value
8.3
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
12/50
2018-02-14 07:05:51
Measurement pX
8.3
Concomitants: Compound name
Forskolin
Concomitants: Compound role
COM
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 18 of 101
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of compound towards human Cannabinoid receptor 1 stably transfected in CHO cells using [3H]CP-55940 as radioligand determined by LIQUID SCINTILLATION COUNTING ASSAY
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.7
Measurement pX
8.7
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 19 of 101
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Effective concentration of compound required to agonize [3H]Arachidonic acid release in CHO cells expressing human Cannabinoid receptor 1 upon incubation at 37 degree C
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
13/50
2018-02-14 07:05:51
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
pEC50
Measurement Object
[3H]arachidonic acid release
Quantitative value
8.3
Measurement pX
8.3
Concomitants: Compound name
[3H]ARACHIDONIC ACID
Concomitants: Compound role
RAD
Blaazer, Antoni R.; Lange, Jos H.M.; Van Der Neut, Martina A.W.; Mulder, Arie; Den Boon, Femke S.; Werkman, Taco R.; Kruse, Chris G.; Wadman, Wytse J.; European Journal of Medicinal Chemistry; vol. 46; nb. 10; (2011); p. 5086 - 5098, View in Reaxys 20 of 101
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1
21 of 101
Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity of the compound towards cannabinoid receptor 1 to that of cannabinoid receptor 2
Substance RN
9348161View in Reaxys
Measurement Parameter
Ratio
Quantitative value
3.23
Target Name
Cannabinoid receptor 2
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2 (cannabinoid receptor 2); cx5; hcb2; mcb2; rcb2
Target, Subunit, Species Cannabinoid receptor 2 Target Mutant/Chimera Details
Cannabinoid receptor 2:Wild
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards Cannabinoid receptor 2
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.94
Deviation
2.65
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
14/50
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22 of 101
Measurement pX
8.53
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro binding affinity of the compound towards cannabinoid receptor 1 of rat whole brain membrane using 1 nM [3H]CP-55940 as radioligand
Biological Species/NCBI Rattus norvegicus ID Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman, John W.; Mabon, Ross; Wu, Ming-Jung; Lu, Jianzhong; Hart, Richard; Hurst, Dow P.; Reggio, Patricia H.; Wiley, Jenny L.; Martin, Billy R.; Bioorganic and Medicinal Chemistry; vol. 11; nb. 4; (2003); p. 539 - 549, View in Reaxys 23 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Details
In vivo effective dose of the compound required for inhibition of spontaneous locomotor activity in Male ICR mouse after 5-15 min upon intravenous administration
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
ED50
Quantitative value
0.09
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 24 of 101
Bioassay Category
In Vivo (Animal models)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
15/50
2018-02-14 07:05:51
Bioassay Details
In vivo effective dose of the compound required for inhibition of spontaneous locomotor activity in Male ICR mouse after 5-15 min upon intravenous administration
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
ED50
Quantitative value
1.7
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 25 of 101
Substance Effect
Cataleptogenic
Bioassay Category
In Vivo (Animal models)
Bioassay Details
In vivo effective dose of the compound required to measure immobility index in Male ICR mouse after 40-45 min upon intravenous administration
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Substance Route of Adm.
intravenous administration
Qualitative Results
RANGE = 3-9 umol/Kg
Measurement Parameter
Qualitative
Measurement Object
ED50
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 26 of 101
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity of the compound towards human Cannabinoid receptor 1 to that of human Cannabinoid receptor 2
Biological Species/NCBI human ID Substance RN
9348161View in Reaxys
Measurement Parameter
Qualitative
Qualitative value
Not Published
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
16/50
2018-02-14 07:05:51
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 27 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Details
In vivo effective dose of the compound required for inhibition of spontaneous locomotor activity in Male ICR mouse after 5-15 min upon intravenous administration
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Substance Route of Adm.
intravenous administration
Measurement Parameter
ED50
Unit
µmol/kg
Measurement Object
ED50
Quantitative value
0.44
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 28 of 101
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro binding affinity of the compound towards human Cannabinoid receptor 1 expressed in HEK 293 cells using 0.5 nM of [3H]CP-55940 as radioligand upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI human ID Cells/Cell Lines
HEK 293
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 29 of 101
Target Name
Cannabinoid receptor 2 [human]
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
17/50
2018-02-14 07:05:51
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vitro binding affinity of the compound towards human Cannabinoid receptor 2 expressed in CHO cells using 0.5 nM of [3H]CP-55490 as radioligand upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]CP-55490
Concomitants: Compound role
RAD
Wiley, Jenny L.; Smith, Valerie J.; Chen, Jianhong; Martin, Billy R.; Huffman, John W.; Bioorganic and Medicinal Chemistry; vol. 20; nb. 6; (2012); p. 2067 - 2081, View in Reaxys 30 of 101
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards human cannabinoid receptor 2 expressed in CHO cells using [3H]CP 55,940 as radioligand upon incubation at 30 degree C for 1 h
Biological Species/NCBI human ID Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
18/50
2018-02-14 07:05:51
31 of 101
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards cannabinoid receptor 1 using [3H]CP 55,940 as radioligand in rat brain membranes
Biological Species/NCBI Rattus norvegicus ID
32 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
19/50
2018-02-14 07:05:51
Bioassay Details
Ratio of binding affinity of human cannabinoid receptor 2 expressed in CHO cells to that of rat cannabinoid receptor 1
Biological Species/NCBI human ID
33 of 101
Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
Ratio
Quantitative value
3.3
Target Name
Cannabinoid receptor 2 [Mus musculus]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cnr2; mcb2
Target Uniprot ID
p47936
Target, Subunit, Species Cannabinoid receptor 2 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 2 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition of [3H]SR141716A (0.5 nM) or [3H]CP55940 (0.5 nM) binding to mouse cannabinoid receptor 2 upon incubation for 60 min at 37 degree C with compound dissolved in DMSO
Biological Species/NCBI Mus musculus ID
34 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Qualitative
Qualitative value
Not Published
Concomitants: Compound name
[3H]SR 141716A or [3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibition of [3H]SR141716A (0.5 nM) or [3H]CP55940 (0.5 nM) binding to mouse cannabinoid receptor 1 upon incubation for 60 min at 37 degree C with compound dissolved in DMSO
Biological Species/NCBI Mus musculus ID
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
20/50
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35 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Qualitative
Qualitative value
Not Published
Concomitants: Compound name
[3H]SR 141716A or [3H]CP-55940
Concomitants: Compound role
RAD
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured spontaneous activity(SA) in mouse
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Spontaneous activity
Qualitative value
=
Quantitative value
0.44
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 36 of 101
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory constant of the compound against cannabinoid receptor 1 using [3H] CP-55,940 as radioligand in rat brain membrane
Biological Species/NCBI Rattus norvegicus ID Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9.5
Deviation
4.5
Measurement pX
8.02
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
21/50
2018-02-14 07:05:51
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 37 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured hypothermia (as decrease in rectal temperature, RT) in mouse
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Hypothermia
Qualitative value
=
Quantitative value
1.7
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 38 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose of the compound measured antinociception (as tail flick, TF) in mouse
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Measurement Object
Antinociception
Qualitative value
=
Quantitative value
0.09
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 39 of 101
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Inhibitory constant of the compound against cannabinoid receptor 2 using [3H] WIN-55,212 as radioligand in human spleen membrane
Biological Species/NCBI human ID Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
22/50
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Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]WIN 55212-2
Concomitants: Compound role
RAD
Huffman; Current pharmaceutical design; vol. 6; nb. 13; (2000); p. 1323 - 1337, View in Reaxys 40 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effective dose required for spontaneous activity was determined in mouse
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
ED50
Unit
µM/kg
Qualitative value
=
Quantitative value
0.44
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 41 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo effect on hypothermia was determined in mouse by measuring the decrease in rectal temperature
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
Activity
Measurement Object
Decrease in rectal temperature
Quantitative value
1.7
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 42 of 101
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards Cannabinoid receptor 1 (40 ug) from rat forebrain synaptosomal membranes using 0.76 nM [3H]CP-55,940 as radioligand upon incubation for 1 h at 30 degree C
Biological Species/NCBI Rattus norvegicus ID Substance RN
9348161View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
23/50
2018-02-14 07:05:51
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 43 of 101
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
In vivo antinociceptive activity was determined in mouse using tail flick method
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
Activity
Unit
µM/kg
Measurement Object
Antinociceptive activity
Qualitative value
~
Quantitative value
0.09
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 44 of 101
Target Name
Cannabinoid receptor 2 [Mus musculus]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cnr2; mcb2
Target Uniprot ID
p47936
Target, Subunit, Species Cannabinoid receptor 2 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 2 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards Cannabinoid receptor 2 (40 ug) from mouse spleen membranes using 0.76 nM [3H]CP-55,940 as radioligand upon incubation for 1 h at 30 degree C
Biological Species/NCBI Mus musculus ID Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Huffman; Padgett; Current Medicinal Chemistry; vol. 12; nb. 12; (2005); p. 1395 - 1411, View in Reaxys 45 of 101
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards rat cannabinoid receptor 1 in brain homogenates
Biological Species/NCBI Rattus norvegicus ID
46 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.045
Measurement pX
8.05
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity of the compound towards rat brain homogenate cannabinoid receptor 1 to that of cloned human cannabinoid receptor 2
Biological Species/NCBI Rattus norvegicus ID
47 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Ratio
Quantitative value
0.942
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards cloned human cannabinoid receptor 2 was determined
Biological Species/NCBI human ID
48 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.538
Measurement pX
8.54
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human cannabinoid receptor 2 expressed in CHO membranes using 102.9 Ci/mmol [3H]CP 55940 as radioligand upon incubation in 50 mM Tris-HCl, pH 7.4 for 1 h at 30 degree C
Biological Species/NCBI human ID
49 of 101
Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Qualitative Results
Ki not calculated
Measurement Parameter
Qualitative
Measurement Object
Ki
Concomitants: Compound name
[3H]CP 55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Negative logarithm of binding affinity of the compound towards human cannabinoid receptor 2 expressed in CHO membranes using 102.9 Ci/mmol [3H]CP 55940 as radioligand upon incubation in 50 mM Tris-HCl, pH 7.4 for 1 h at 30 degree C
Biological Species/NCBI human ID
50 of 101
Cells/Cell Lines
CHO
Substance RN
9348161View in Reaxys
Measurement Parameter
pKi
Quantitative value
8.537
Measurement pX
8.54
Concomitants: Compound name
[3H]CP 55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [human]
Target Synonyms
cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p21554; p21554-3
Target, Subunit, Species Cannabinoid receptor 1 [human] Target Mutant/Chimera Details
Cannabinoid receptor 1 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human cannabinoid receptor 1
Biological Species/NCBI human ID
51 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards human cannabinoid receptor 2
Biological Species/NCBI human ID
52 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards rat brain cannabinoid receptor 1 using [3H] CP 55,940 upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI Rattus norvegicus ID
53 of 101
Organs/Tissues
brain
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
9
Deviation
5
Measurement pX
8.05
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1 [Rattus norvegicus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1); skr6
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Uniprot ID
p20272
Target, Subunit, Species Cannabinoid receptor 1 [Rattus norvegicus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Rattus norvegicus]:Wild
Target Species (Bioactivity)
Rattus norvegicus
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Ratio of binding affinity towards rat brain cannabinoid receptor 1 to that of human cannabinoid receptor 2
Biological Species/NCBI Rattus norvegicus ID
54 of 101
Organs/Tissues
brain
Substance RN
9348161View in Reaxys
Measurement Parameter
Ratio
Measurement Object
Ratio
Quantitative value
3.3
Target Name
Cannabinoid receptor 2 [human]
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2; cx5; hcb2
Target Uniprot ID
p34972
Target, Subunit, Species Cannabinoid receptor 2 [human] Target Mutant/Chimera Details
Cannabinoid receptor 2 [human]:Wild
Target Species (Bioactivity)
human
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity towards human cannabinoid receptor 2 using [3H] CP 55,940 upon incubation in 50 mM Tris-HCl, pH 7.4 at 30 degree C for 1 hour
Biological Species/NCBI human ID
55 of 101
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Deviation
2.6
Measurement pX
8.54
Concomitants: Compound name
[3H]CP-55940
Concomitants: Compound role
RAD
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Substance RN
9348161View in Reaxys
Substance Name
1-Table 1, structure number 1
Measurement Parameter
Ki
Unit
µM
Quantitative value
4.31
Measurement pX
5.37
Concomitants: Compound RN
6659789
Concomitants: Compound name
[3H]-CP 55940
Concomitants: Compound role
RAD
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; RESEARCH TRIANGLE INSTITUTE; SPIGELMAN, Igor; SELTZMAN, Herbert, H.; SHINER, Craig; WO2014/15298; (2014); (A1) English, View in Reaxys 56 of 101
Target Name
Cannabinoid receptor 2
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2 (cannabinoid receptor 2); cx5; hcb2; mcb2; rcb2
Target, Subunit, Species Cannabinoid receptor 2 Target Mutant/Chimera Details
Cannabinoid receptor 2:Wild
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Substance RN
9348161View in Reaxys
Substance Name
1-Table 1, structure number 1
Measurement Parameter
Ki
Unit
µM
Quantitative value
7.38
Measurement pX
5.13
Concomitants: Compound RN
6659789
Concomitants: Compound name
[3H]-CP 55940
Concomitants: Compound role
RAD
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; RESEARCH TRIANGLE INSTITUTE; SPIGELMAN, Igor; SELTZMAN, Herbert, H.; SHINER, Craig; WO2014/15298; (2014); (A1) English, View in Reaxys 57 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI mouse NIH/Swiss ID Substance RN
9348161View in Reaxys
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Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Substance Dosing Regi- Single men Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
discrimination between vehicle and delta9-THC (3 mg/kg)
Quantitative value
0.58
Deviation
0.230000
Concomitants: Compound RN
4354308
Concomitants: Compound name
Delta9-THC
Concomitants: Compound role
TRA
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 58 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI mouse NIH/Swiss ID Substance RN
9348161View in Reaxys
Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
tail flick latency increase
Quantitative value
2.52
Deviation
0.610000
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 59 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI mouse NIH/Swiss ID Substance RN
9348161View in Reaxys
Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
ID10
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Unit
mg/kg
Measurement Object
Rectal temperature
Quantitative value
3.89
Deviation
0.350000
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 60 of 101
Bioassay Category
In Vivo (Animal models)
Bioassay Name
In vivo Measurement
Biological Species/NCBI mouse NIH/Swiss ID Substance RN
9348161View in Reaxys
Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
ID50
Unit
mg/kg
Measurement Object
Respiratory rate
Quantitative value
1.43
Deviation
0.180000
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 61 of 101
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Binding
Biological Species/NCBI mouse NIH/Swiss ID Organs/Tissues
brain
Cell Fraction
Homogenate
Substance RN
9348161View in Reaxys
Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Measurement Parameter
Ki
Unit
nM
Quantitative value
0.97
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Deviation
0.120000
Measurement pX
9.01
Concomitants: Compound RN
6659789; 4913623
Concomitants: Compound name
[3H]-CP 55940; Win 55212-2
Concomitants: Compound role
RAD; NSB
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 62 of 101
Target Name
cannabinoid receptor [Mus musculus]
Target Synonyms
cannabinoid receptor
Target, Subunit, Species cannabinoid receptor [Mus musculus] Target Mutant/Chimera Details
cannabinoid receptor [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
Adenylate cyclase activity
Cells/Cell Lines
Neuro 2A
Substance RN
9348161View in Reaxys
Substance Name
page 353, paragraph 5+page 354, paragraph 1+2, page 355, paragraph 1+2, page 356, paragraph 2, compound JWH-018
Measurement Parameter
IC50
Unit
nM
Quantitative value
5.31
Deviation
0.400000
Measurement pX
8.27
Concomitants: Compound RN
3555164; 521500
Concomitants: Compound name
IBMX; [3H]-Adenine
Concomitants: Compound role
IND; MAR
Brents, Lisa K.; Zimmerman, Sarah M.; Saffell, Amanda R.; Prather, Paul L.; Fantegrossi, William E.; Journal of Pharmacology and Experimental Therapeutics; vol. 346; nb. 3; (2013); p. 350 - 361, View in Reaxys 63 of 101
Target Name
Cannabinoid receptor 1 [Mus musculus]
Target Synonyms
brain-type cannabinoid receptor; cannabinoid receptor 1; cb-r; cb1; cnr1 (cannabinoid receptor 1)
Target Uniprot ID
p47746
Target, Subunit, Species Cannabinoid receptor 1 [Mus musculus] Target Mutant/Chimera Details
Cannabinoid receptor 1 [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Target Transfection
Non Transfected
Substance Action on Target
Agonist
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
GTPgammaS
Biological Species/NCBI Mus musculus ID Organs/Tissues
brain
Cell Fraction
Membrane
Substance RN
9348161View in Reaxys
Substance Name
JWH-018-figure 8B, page 36, paragraph 3.3
Measurement Parameter
EC50
Unit
nM
Quantitative value
8
Measurement pX
8.1
Concomitants: Compound RN
9743845; 10309076
Concomitants: Compound name
[35S]-GTPgS; GDP; BSA
Concomitants: Compound role
MAR; COM; COM
Patent; THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS; THE UNIVERSITY OF KANSAS; PRATHER, Paul, L.; PRISINZANO, Thomas, E.; FANTEGROSSI, William, E.; BRENTS, Lisa, K.; MORAN, Jeffery; RADOMINSKA-PANDYA, Anna; VASILJEVIK, Tamara; WO2013/106349; (2013); (A1) English, View in Reaxys 64 of 101
Target Name
Cannabinoid receptor 2
Target Synonyms
cannabinoid receptor 2; cb-2; cb2; cb2a; cb2b; cnr2 (cannabinoid receptor 2); cx5; hcb2; mcb2; rcb2
Target, Subunit, Species Cannabinoid receptor 2
65 of 101
Target Mutant/Chimera Details
Cannabinoid receptor 2:Wild
Substance Action on Target
Radioligand (/ligand)
Substance Effect
binding activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards Cannabinoid receptor 2
Substance RN
9348161View in Reaxys
Measurement Parameter
Ki
Unit
nM
Qualitative value
=
Quantitative value
2.9
Measurement pX
8.54
Target Name
Cannabinoid receptor 1
Target Synonyms
brain-type cannabinoid receptor; cann6; cannabinoid receptor 1; cb-r; cb1; cnr; cnr1 (cannabinoid receptor 1); skr6 (cannabinoid receptor 1)
Target, Subunit, Species Cannabinoid receptor 1
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66 of 101
Target Mutant/Chimera Details
Cannabinoid receptor 1:Wild
Substance Action on Target
Radioligand (/ligand)
Substance Effect
binding activity
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Binding affinity of the compound towards Cannabinoid receptor 1
Substance RN
9348161View in Reaxys
Measurement Parameter
Qualitative
Unit
nM
Qualitative value
=
Quantitative value
9.5
Bioassay Category
Metabolism/Transport
Biological Species/NCBI human ID Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
9348161View in Reaxys
Substance Name
naphthalen-1-yl-(1-pentylindol-3-yl)methanone
Substance Dose
5 μM
Measurement Parameter
Concentration
Unit
ng/ml
Qualitative value
<
Quantitative value
15
Metabolite RN
22431920
Concomitants: Compound RN
79324
Concomitants: Compound name
NADH
Concomitants: Compound role
SUB
Holm, Niels Bjerre; Noble, Carolina; Linnet, Kristian; Toxicology Letters; vol. 259; (2016); p. 35 - 43, View in Reaxys 67 of 101
Bioassay Category
Metabolism/Transport
Biological Species/NCBI human ID Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
9348161View in Reaxys
Substance Name
naphthalen-1-yl-(1-pentylindol-3-yl)methanone
Substance Dose
5 μM
Measurement Parameter
Clint
Unit
μl/min/mg protein
Quantitative value
7.1
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Metabolite RN
22431925
Holm, Niels Bjerre; Noble, Carolina; Linnet, Kristian; Toxicology Letters; vol. 259; (2016); p. 35 - 43, View in Reaxys 68 of 101
Bioassay Category
Metabolism/Transport
Biological Species/NCBI human ID Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
9348161View in Reaxys
Substance Name
naphthalen-1-yl-(1-pentylindol-3-yl)methanone
Substance Dose
5 μM
Measurement Parameter
Clint
Unit
μl/min/mg protein
Quantitative value
104
Concomitants: Compound RN
79324
Concomitants: Compound name
NADH
Concomitants: Compound role
SUB
Holm, Niels Bjerre; Noble, Carolina; Linnet, Kristian; Toxicology Letters; vol. 259; (2016); p. 35 - 43, View in Reaxys 69 of 101
Bioassay Category
Metabolism/Transport
Biological Species/NCBI human ID Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
9348161View in Reaxys
Substance Name
naphthalen-1-yl-(1-pentylindol-3-yl)methanone
Substance Dose
5 μM
Measurement Parameter
Concentration
Unit
ng/ml
Quantitative value
0.4
Metabolite RN
22431925
Concomitants: Compound RN
79324
Concomitants: Compound name
NADH
Concomitants: Compound role
SUB
Holm, Niels Bjerre; Noble, Carolina; Linnet, Kristian; Toxicology Letters; vol. 259; (2016); p. 35 - 43, View in Reaxys 70 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
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Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Decrease
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 71 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Inhibition
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 72 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Inhibition
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 73 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
6 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Increase
Measurement Object
of catalepsy
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 74 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Decrease
Measurement Object
Rectal temperature
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 75 of 101
Bioassay Category
Toxicity/Safety Pharmacology
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Decrease
Measurement Object
of ventral fur temperature
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 76 of 101
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Increase
Measurement Object
Pain threshold
Qualitative value
Active
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 77 of 101
Substance Effect
Analgesic
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1/ICR mouse ID Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Increase
Measurement Object
Pain threshold
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 78 of 101
Bioassay Category
In Vivo (Animal models)
Substance RN
9348161View in Reaxys
Substance Name
naphthalen‐1‐yl‐(1‐pentylindol‐3‐yl)methanone
Substance Dose
0.01 - 100 mg/kg
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
% Inhibition
Qualitative value
Active
Canazza, Isabella; Ossato, Andrea; Vincenzi, Fabrizio; Gregori, Adolfo; Di Rosa, Fabiana; Nigro, Federica; Rimessi, Alessandro; Pinton, Paolo; Varani, Katia; Borea, Pier Andrea; Marti, Matteo; Human Psychopharmacology; vol. 32; nb. 3; (2017); Art.No: E2601, View in Reaxys 79 of 101
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI C57BL 6 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
μmol/kg
Quantitative value
0.27
Thomas, Brian F.; Lefever, Timothy W.; Cortes, Ricardo A.; Grabenauer, Megan; Kovach, Alexander L.; Cox, Anderson O.; Patel, Purvi R.; Pollard, Gerald T.; Marusich, Julie A.; Kevin, Richard C.; Gamage, Thomas F.; Wiley, Jenny L.; Journal of Pharmacology and Experimental Therapeutics; vol. 361; nb. 1; (2017); p. 162 - 171, View in Reaxys 80 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 81 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 82 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 83 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 84 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 85 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 86 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 87 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men
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Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Active
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 88 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Active
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 89 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Active
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 90 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID
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Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 91 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 92 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 93 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 94 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 95 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
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Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Measurement Object
Total distance travelled
Qualitative value
Not active
Measurement pX
1
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 96 of 101
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% Inhibition
Unit
%
Measurement Object
Binding
Qualitative value
~
Quantitative value
39
Concomitants: Compound RN
25433222; 4354534
Concomitants: Compound name
[123I]-2β-carbomethoxy-3β-(4-iodophenyl)-N-(3-fluoropropyl)nortropane
Concomitants: Compound role
RAD; RAD
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 97 of 101
Substance Effect
Psychostimulant
Bioassay Category
In Vivo (Animal models)
Biological Species/NCBI CD-1 mouse ID Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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Substance Dose
0.3 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regi- Single men Measurement Parameter
% increase
Unit
%
Measurement Object
Concentration
Qualitative value
~
Quantitative value
150
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 98 of 101
Target Name
Sodium-dependent dopamine transporter [Mus musculus]
Target Synonyms
da transporter; dat; dat1; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
q61327
Target, Subunit, Species Sodium-dependent dopamine transporter [Mus musculus] Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Stimulator
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI Mus musculus ID Organs/Tissues
neostriatum
Cell Fraction
Synaptosome
Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
100 nM
Measurement Parameter
% Inhibition
Measurement Object
release
Qualitative value
Not active
Measurement pX
1
Concomitants: Compound RN
1072822
Concomitants: Compound name
dopamine
Concomitants: Compound role
SUB
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys
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99 of 101
Target Name
Sodium-dependent dopamine transporter [Mus musculus]
Target Synonyms
da transporter; dat; dat1; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
q61327
Target, Subunit, Species Sodium-dependent dopamine transporter [Mus musculus] Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Inhibitor
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI Mus musculus ID Organs/Tissues
neostriatum
Cell Fraction
Synaptosome
Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Substance Dose
100 nM
Measurement Parameter
% Inhibition
Measurement Object
uptake
Qualitative value
Not active
Measurement pX
1
Concomitants: Compound RN
1072822
Concomitants: Compound name
dopamine
Concomitants: Compound role
SUB
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 100 of 101 Target Name
Sodium-dependent dopamine transporter [human]
Target Synonyms
da transporter; dat; dat1; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
q01959
Target, Subunit, Species Sodium-dependent dopamine transporter [human] Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Transfected
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Cells/Cell Lines
CHO cell line
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Cell Fraction
Membrane
Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Measurement Parameter
Ki
Unit
nM
Measurement Object
Binding
Quantitative value
7183
Measurement pX
5.14
Concomitants: Compound RN
4354534
Concomitants: Compound role
RAD
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca, Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys 101 of 101 Target Name
Sodium-dependent dopamine transporter [Mus musculus]
Target Synonyms
da transporter; dat; dat1; slc6a3; sodium-dependent dopamine transporter; solute carrier family 6 member 3
Target Uniprot ID
q61327
Target, Subunit, Species Sodium-dependent dopamine transporter [Mus musculus] Target Mutant/Chimera Details
Sodium-dependent dopamine transporter [Mus musculus]:Wild
Target Species (Bioactivity)
Mus musculus
Target Transfection
Non Transfected
Substance Action on Target
Radioligand (/ligand)
Bioassay Category
In Vitro (Efficacy)
Biological Species/NCBI Mus musculus ID Organs/Tissues
neostriatum
Cell Fraction
Synaptosome
Substance RN
9348161View in Reaxys
Substance Name
1-pentyl-3-(1-naphthoyl)indole
Measurement Parameter
Ki
Unit
nM
Measurement Object
Binding
Qualitative value
>
Quantitative value
10000
Measurement pX
1
Concomitants: Compound RN
4354534
Concomitants: Compound role
RAD
Ossato, Andrea; Bilel, Sabrine; Canazza, Isabella; Beggiato, Sarah; Ferraro, Luca; Marti, Matteo; De-Giorgio, Fabio; Uccelli, Licia; Boschi, Alessandra; Di Domenico, Giovanni; Pasquali, Micol; Pupillo, Gaia; De Luca,
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Maria Antonietta; Vincenzi, Fabrizio; Varani, Katia; Borea, Pier Andrea; Rimondo, Claudia; Serpelloni, Giovanni; ; vol. 8; nb. AUG; (2017); Art.No: 130, View in Reaxys
Copyright © 2018 Reed Elsevier Properties SA. All rights reserved. Authorized use only. Reaxys® and the Reaxys® trademark are owned and protected by Reed Elsevier Properties SA and used under license.
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