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2018-06-02 10h:59m:32s (UTC)
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Reaxys ID 1085184 View in Reaxys
1/1 O
CAS Registry Number: 635-41-6 Chemical Name: trimetozine; Trimetozine; morpholino(3,4,5-trimethoxyphenyl)methanone; 4-(3,4,5-trimethoxybenzoyl)morhpoline; N-(3,4,5-trimethoxybenzoyl)morpholine; Trimetozin; ZINC00000811 Linear Structure Formula: C14H19NO5 Molecular Formula: C14H19NO5 Molecular Weight: 281.309 Type of Substance: heterocyclic InChI Key: XWVOEFLBOSSYGM-UHFFFAOYSA-N Note:
N O O
O O
Substance Label (10) Label References 4ea
Saito, Nozomi; Taniguchi, Takahisa; Hoshiya, Naoyuki; Shuto, Satoshi; Arisawa, Mitsuhiro; Sato, Yoshihiro; Green Chemistry; vol. 17; nb. 4; (2015); p. 2358 - 2361, View in Reaxys
3i
Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys
8a
Pettit, George R.; Grealish, Matthew P.; Herald, Delbert L.; Boyd, Michael R.; Hamel, Ernest; Pettit, Robin K.; Journal of Medicinal Chemistry; vol. 43; nb. 14; (2000); p. 2731 - 2737, View in Reaxys
12
Kar; Pharmazie; vol. 38; nb. 5; (1983); p. 313 - 315, View in Reaxys
11/12
Patent; ESZAKMAGYARORSZAGI VEGYIMOVEK; FR2253735; (1975); DE2365451; Chem.Abstr.; vol. 83; nb. 163852, View in Reaxys
11
Kuhnert-Brandstaetter et al.; Scientia Pharmaceutica; vol. 42; (1974); p. 234,235-248, View in Reaxys
II
Klosa,J.; Journal fuer Praktische Chemie (Leipzig); vol. 19; (1963); p. 45 - 55, View in Reaxys; Pettit et al.; Journal of Medicinal and Pharmaceutical Chemistry; vol. 5; (1962); p. 800,804, View in Reaxys
Ia,R=3,4,5(CH3O)3C6H2CO-
Kasztreiner et al.; Biochemical Pharmacology; vol. 11; (1962); p. 651; Chem.Abstr.; vol. 58; nb. 5667c; (1963), View in Reaxys
3
Patent; Egyesult Gyogyszer es Tapszergyar; GB872350; (1960); Chem.Abstr.; vol. 56; nb. 474; (1962), View in Reaxys
9
Patent; Egyesult Gyogyszer es Tapszergyar; GB872350; (1960); Chem.Abstr.; vol. 56; nb. 474; (1962), View in Reaxys
Druglikeness (1) 1 of 1
LogP
0.646
H Bond Donors
0
H Bond Acceptors
3
Rotatable Bonds
5
TPSA
57.23
Lipinski Number
4
Veber Number
2
Highest Clinical Phase (1) Highest Clinical Phase Marketed Melting Point (8) 1 of 8
Melting Point [°C]
120 - 121
Location
supporting information
Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys 2 of 8
Melting Point [°C]
135
Solvent (Melting Point)
ethanol
Kar; Pharmazie; vol. 38; nb. 5; (1983); p. 313 - 315, View in Reaxys
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3 of 8
Melting Point [°C]
117 - 119
Kuhnert-Brandstaetter et al.; Scientia Pharmaceutica; vol. 42; (1974); p. 234,235-248, View in Reaxys 4 of 8
Melting Point [°C]
113 - 115
Solvent (Melting Point)
aq. methanol
Klosa,J.; Journal fuer Praktische Chemie (Leipzig); vol. 19; (1963); p. 45 - 55, View in Reaxys 5 of 8
Melting Point [°C]
120 - 122
Patent; Gyog. Kut. Int.; HU147687; Chem.Abstr.; vol. 58; nb. 7950b; (1963), View in Reaxys; Patent; Egyesult; AT224644; (1962); Chem.Abstr.; vol. 58; nb. 9091c; (1963), View in Reaxys; Patent; Egyesult Gyogyszer es Tapszergyar; GB872350; (1960); Chem.Abstr.; vol. 56; nb. 474; (1962), View in Reaxys 6 of 8
Melting Point [°C]
120 - 121
Solvent (Melting Point)
methanol
Pettit et al.; Journal of Medicinal and Pharmaceutical Chemistry; vol. 5; (1962); p. 800,804, View in Reaxys 7 of 8
Melting Point [°C]
76 - 77
Kasztreiner et al.; Biochemical Pharmacology; vol. 11; (1962); p. 651; Chem.Abstr.; vol. 58; nb. 5667c; (1963), View in Reaxys 8 of 8
Melting Point [°C]
120 - 122
Solvent (Melting Point)
aq. ethanol
Patent; Egyesult Gyogyszer es Tapszergyar; GB872350; (1960); Chem.Abstr.; vol. 56; nb. 474; (1962), View in Reaxys Crystal Property Description (3) Colour & Other Location Properties
References
yellow
supporting informa- Saito, Nozomi; Taniguchi, Takahisa; Hoshiya, Naoyuki; Shuto, Satoshi; Arisawa, Mitsuhiro; tion Sato, Yoshihiro; Green Chemistry; vol. 17; nb. 4; (2015); p. 2358 - 2361, View in Reaxys
white
supporting informa- Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; tion (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys
yellow
Khan, Khalid Mohammed; Khan, Muhammad Zarrar; Taha, Muhammad; Maharvi, Ghulam Murtaza; Saify, Zafar Saeed; Parveen, Shahnaz; Choudhary, Muhammad Iqbal; Natural Product Research; vol. 23; nb. 5; (2009); p. 479 - 484, View in Reaxys
Liquid/Liquid Systems (MCS) (1) 1 of 1
Description (Liquid/Liquid Distribution between solvent 1 + 2 Systems (MCS)) Partner (Liquid/Liquid Systems (MCS))
aqueous buffer sol./Et2O (pH=3...11), or CHCl3 (pH=3)
Muller; Pharmazie; vol. 38; nb. 7; (1983); p. 462 - 466, View in Reaxys Liquid/Solid Systems (MCS) (1) 1 of 1
Description (Liquid/Solid Systems (MCS))
Eutectic
Kuhnert-Brandstaetter et al.; Scientia Pharmaceutica; vol. 42; (1974); p. 234,235-248, View in Reaxys Partition octan-1-ol/water (MCS) (1) 1 of 1
log POW
0.38
Palos, Isidro; Lara-Ramirez, Edgar E.; Lopez-Cedillo, Julio Cesar; Garcia-Perez, Carlos; Kashif, Muhammad; Bocanegra-Garcia, Virgilio; Nogueda-Torres, Benjamin; Rivera, Gildardo; Molecules; vol. 22; nb. 6; (2017); Art.No: 1015, View in Reaxys NMR Spectroscopy (5) 1 of 5
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
1H
Coupling Nuclei
1H
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Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 500 scopy) [MHz] Location
supporting information
Saito, Nozomi; Taniguchi, Takahisa; Hoshiya, Naoyuki; Shuto, Satoshi; Arisawa, Mitsuhiro; Sato, Yoshihiro; Green Chemistry; vol. 17; nb. 4; (2015); p. 2358 - 2361, View in Reaxys 2 of 5
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 125 scopy) [MHz] Location
supporting information
Saito, Nozomi; Taniguchi, Takahisa; Hoshiya, Naoyuki; Shuto, Satoshi; Arisawa, Mitsuhiro; Sato, Yoshihiro; Green Chemistry; vol. 17; nb. 4; (2015); p. 2358 - 2361, View in Reaxys 3 of 5
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 300 scopy) [MHz] Location
supporting information
Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys 4 of 5
Description (NMR Spectroscopy)
Chemical shifts; Spectrum
Nucleus (NMR Spectroscopy)
13C
Solvents (NMR Spectroscopy)
chloroform-d1
Frequency (NMR Spectro- 75 scopy) [MHz] Location
supporting information
Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys 5 of 5
Description (NMR Spectroscopy)
Chemical shifts
Nucleus (NMR Spectroscopy)
1H
Solvents (NMR Spectroscopy)
CDCl3
Frequency (NMR Spectro- 300 scopy) [MHz] Pettit, George R.; Grealish, Matthew P.; Herald, Delbert L.; Boyd, Michael R.; Hamel, Ernest; Pettit, Robin K.; Journal of Medicinal Chemistry; vol. 43; nb. 14; (2000); p. 2731 - 2737, View in Reaxys IR Spectroscopy (2)
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1 of 2
Description (IR Spectroscopy)
Bands
Solvent (IR Spectroscopy)
potassium bromide
Location
supporting information
Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys 2 of 2
Description (IR Spectroscopy)
Bands
Pettit et al.; Journal of Medicinal and Pharmaceutical Chemistry; vol. 5; (1962); p. 800,804, View in Reaxys Mass Spectrometry (2) Description (Mass Location Spectrometry)
References
electrospray ionisa- supporting informa- Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; tion (ESI); spection (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys trum high resolution supporting informa- Bathini, Thulasiram; Rawat, Vikas S.; Bojja, Sreedhar; Tetrahedron Letters; vol. 56; nb. 41; mass spectrometry tion (2015); p. 5656 - 5660; Art.No: 46650, View in Reaxys (HRMS); tandem mass spectrometry; electrospray ionisation (ESI); time-offlight mass spectra (TOFMS); spectrum UV/VIS Spectroscopy (1) 1 of 1
Description (UV/VIS Spectroscopy)
UV/VIS
Kuhnert-Brandstaetter et al.; Scientia Pharmaceutica; vol. 42; (1974); p. 234,235-248, View in Reaxys Medchem (30) 1 of 30
Target Name
Cytochrome P450 3A [human]
Target Synonyms
cytochrome p450 3a
Target, Subunit, Species
Cytochrome P450 3A [human]
Target Mutant/Chimera Details
Cytochrome P450 3A [human]:Wild
Target Species (Bioactivity)
human
Target Transfection
Non Transfected
Bioassay Category
Metabolism/Transport
Bioassay Name
Enzymology inhibition
Biological Species/NCBI ID
human
Organs/Tissues
liver
Cell Fraction
Microsome
Substance RN
1085184View in Reaxys
Substance Name
Trimetozine
Substance Dose
1 µM
Measurement Parameter
% Inhibition
Unit
%
Qualitative value
<
Quantitative value
10
Measurement pX
1
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2 of 30
Metabolite RN
899031
Metabolite name
1'-Hydroxymidazolam
Concomitants: Compound RN
625572; 506008; 506008; 77911; 77911
Concomitants: Compound name
Midazolam; DMSO; DMSO; NADPH; NADPH
Concomitants: Compound role
SUB; SLV; SLV; COE; COE
Substance Effect
Antidepressant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Fighting behaviour
Biological Species/NCBI ID
Swiss Webster mouse
Substance RN
1085184View in Reaxys
Substance Name
Trioxazine
Substance Dose
50 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
% Inhibition
Unit
%
Measurement Object
of aggressive behavior
Quantitative value
25 - 50
Valzelli; Giacalone; Garattini; European journal of pharmacology; vol. 2; nb. 2; (1967); p. 144 - 146, View in Reaxys 3 of 30
Substance Effect
Antidepressant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Fighting behaviour
Biological Species/NCBI ID
Swiss Webster mouse
Substance RN
1085184View in Reaxys
Substance Name
Trioxazine
Substance Dose
75 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
% Inhibition
Unit
%
Measurement Object
of aggressive behavior
Quantitative value
25 - 75
Valzelli; Giacalone; Garattini; European journal of pharmacology; vol. 2; nb. 2; (1967); p. 144 - 146, View in Reaxys 4 of 30
Substance Effect
Antidepressant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Fighting behaviour
Biological Species/NCBI ID
Swiss Webster mouse
Substance RN
1085184View in Reaxys
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Substance Name
Trioxazine
Substance Dose
50 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
time
Unit
hour
Measurement Object
Inhibition
Quantitative value
1
Valzelli; Giacalone; Garattini; European journal of pharmacology; vol. 2; nb. 2; (1967); p. 144 - 146, View in Reaxys 5 of 30
Substance Effect
Antidepressant
Bioassay Category
In Vivo (Animal models)
Bioassay Name
Fighting behaviour
Biological Species/NCBI ID
Swiss Webster mouse
Substance RN
1085184View in Reaxys
Substance Name
Trioxazine
Substance Dose
75 mg/kg
Substance Route of Adm.
intraperitoneal administration
Substance Dosing Regimen
Single
Measurement Parameter
time
Unit
hour
Measurement Object
Inhibition
Quantitative value
6
Valzelli; Giacalone; Garattini; European journal of pharmacology; vol. 2; nb. 2; (1967); p. 144 - 146, View in Reaxys 6 of 30
Substance Effect
Anti-Leishmaniasis
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Bioassay Details
Effect : leishmanicidal
Biological Species/NCBI ID
Leishmania major
Substance RN
1085184View in Reaxys
Substance Name
6
Measurement Parameter
IC50
Unit
µg/mL
Quantitative value
100
Measurement pX
3.45
Khan, Khalid Mohammed; Khan, Muhammad Zarrar; Taha, Muhammad; Maharvi, Ghulam Murtaza; Saify, Zafar Saeed; Parveen, Shahnaz; Choudhary, Muhammad Iqbal; Natural Product Research; vol. 23; nb. 5; (2009); p. 479 - 484, View in Reaxys 7 of 30
Substance Effect
Cytotoxic
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Name
Cell/tumor cell: proliferation/viability/growth
Bioassay Details
Effect : cell growth
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Cells/Cell Lines
PC12
Substance RN
1085184View in Reaxys
Substance Name
III-8
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
100
Measurement pX
1
Yang, Xiao-Dong; Zeng, Xiang-Hui; Zhao, Yuan-Hong; Wang, Xue-Quan; Pan, Zhi-Qiang; Li, Liang; Zhang, Hong-Bin; Journal of Combinatorial Chemistry; vol. 12; nb. 3; (2010); p. 307 - 310, View in Reaxys 8 of 30
Substance Effect
Cytotoxic
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Name
Cell/tumor cell: proliferation/viability/growth
Bioassay Details
Effect : cell growth
Cells/Cell Lines
U-937
Substance RN
1085184View in Reaxys
Substance Name
III-8
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
100
Measurement pX
1
Yang, Xiao-Dong; Zeng, Xiang-Hui; Zhao, Yuan-Hong; Wang, Xue-Quan; Pan, Zhi-Qiang; Li, Liang; Zhang, Hong-Bin; Journal of Combinatorial Chemistry; vol. 12; nb. 3; (2010); p. 307 - 310, View in Reaxys 9 of 30
Substance Effect
Cytotoxic
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Name
Cell/tumor cell: proliferation/viability/growth
Bioassay Details
Effect : cell growthBioassay : tumor AGZY cells
Substance RN
1085184View in Reaxys
Substance Name
III-8
Measurement Parameter
IC50
Unit
µM
Qualitative value
>
Quantitative value
100
Measurement pX
1
Yang, Xiao-Dong; Zeng, Xiang-Hui; Zhao, Yuan-Hong; Wang, Xue-Quan; Pan, Zhi-Qiang; Li, Liang; Zhang, Hong-Bin; Journal of Combinatorial Chemistry; vol. 12; nb. 3; (2010); p. 307 - 310, View in Reaxys 10 of 30
Substance Effect
Anxiolytic
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
1085184View in Reaxys
Substance Name
Trimetozine
Measurement Parameter
qualitative
Qualitative value
@
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; (2012); Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00, View in Reaxys 11 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Name
In Vitro (others)
Substance RN
1085184View in Reaxys
Substance Name
273917
Qualitative Results
LD50: > 500 mg/kg i.p. (mice)
Measurement Parameter
qualitative
Kar; Pharmazie; vol. 38; nb. 5; (1983); p. 313 - 315, View in Reaxys 12 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Oral lethal dose in rat
Biological Species/NCBI ID
rat
Substance RN
1085184View in Reaxys
Substance Route of Adm.
oral administration
Measurement Parameter
LD50
Unit
mg/kg
Qualitative value
=
Quantitative value
1800
Knoll; Fuerst; Meszaros; Arzneimittel-Forschung; vol. 21; nb. 5; (1971); p. 719 - 727, View in Reaxys 13 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in rat upon oral administration
Biological Species/NCBI ID
rat
Substance RN
1085184View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
1800
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1800
Knoll; Fuerst; Meszaros; Arzneimittel-Forschung; vol. 21; nb. 5; (1971); p. 719 - 727, View in Reaxys 14 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in mouse upon subcutaneous administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Qualitative Results
1550
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1550
BOISSIER; SIMON; FICHELLE-PAGNY; Thérapie; vol. 20; (1965); p. 401 - 408, View in Reaxys 15 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in mouse upon parenteral administration
Biological Species/NCBI ID
mouse
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Substance RN
1085184View in Reaxys
Substance Route of Adm.
intravenous administration
Qualitative Results
1200
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1200
Comparative biochemistry and physiology. C, Comparative pharmacology and toxicology; vol. 33; (1970); p. 70, View in Reaxys 16 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in mouse upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
1150
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1150
Yakuri to Chiryo Pharmacol. Ther.; vol. 4; (1976); p. 2487, View in Reaxys 17 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in mouse upon oral administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
oral administration
Qualitative Results
2400
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
2400
Yakuri to Chiryo Pharmacol. Ther.; vol. 4; (1976); p. 2487, View in Reaxys 18 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in rat upon intraperitoneal administration
Biological Species/NCBI ID
rat
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Qualitative Results
1080
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1080
Yakuri to Chiryo Pharmacol. Ther.; vol. 4; (1976); p. 2487, View in Reaxys 19 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Subcutaneous lethal dose in Mouse
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Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Measurement Parameter
LD50
Unit
mg/kg
Qualitative value
=
Quantitative value
1550
BOISSIER; SIMON; FICHELLE-PAGNY; Thérapie; vol. 20; (1965); p. 401 - 408, View in Reaxys 20 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in rat upon subcutaneous administration
Biological Species/NCBI ID
rat
Substance RN
1085184View in Reaxys
Qualitative Results
1400
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
1400
Yakuri to Chiryo Pharmacol. Ther.; vol. 4; (1976); p. 2487, View in Reaxys 21 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose of compound in mouse upon intravenous administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Qualitative Results
960
Measurement Parameter
LD50
Unit
mg/kg
Quantitative value
960
Psychotropic Drugs and Related Compounds, 2nd ed., 1972, (), 312; (1972); p. 312, View in Reaxys 22 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Activity of the compound against spontaneous motility in mouse was determined upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
Activity
Measurement Object
relative activity
Quantitative value
1
Hankovszky; Kideg; Journal of medicinal chemistry; vol. 9; nb. 1; (1966); p. 151 - 153, View in Reaxys 23 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Sedative activity of the compound tested for antagonism against deoxyephedrine in mouse upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View 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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Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
Activity
Measurement Object
relative activity
Quantitative value
1
Hankovszky; Kideg; Journal of medicinal chemistry; vol. 9; nb. 1; (1966); p. 151 - 153, View in Reaxys 24 of 30
Substance Action on Target
Antagonist
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Effective dose tested for antagonism against deoxyephedrine in mouse upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
mg/kg
Qualitative value
=
Quantitative value
180
Hankovszky; Kideg; Journal of medicinal chemistry; vol. 9; nb. 1; (1966); p. 151 - 153, View in Reaxys 25 of 30
Bioassay Category
Toxicity/Safety Pharmacology
Bioassay Details
Lethal dose was determined in mice upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
LD50
Unit
mg/kg
Qualitative value
=
Quantitative value
1300
Hankovszky; Kideg; Journal of medicinal chemistry; vol. 9; nb. 1; (1966); p. 151 - 153, View in Reaxys 26 of 30
Bioassay Category
In Vivo (Animal models)
Bioassay Details
Effective dose that cause spontaneous motility in mouse was determined upon intraperitoneal administration
Biological Species/NCBI ID
mouse
Substance RN
1085184View in Reaxys
Substance Route of Adm.
intraperitoneal administration
Measurement Parameter
ED50
Unit
mg/kg
Measurement Object
spontaneous motility
Qualitative value
=
Quantitative value
65
Hankovszky; Kideg; Journal of medicinal chemistry; vol. 9; nb. 1; (1966); p. 151 - 153, View in Reaxys 27 of 30
Bioassay Category
In Vitro (Efficacy)
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Bioassay Details
Sedative effect of the compound was determined in human at a dose of 300-1500 mg per day; Effective
Biological Species/NCBI ID
human
Substance RN
1085184View in Reaxys
Qualitative Results
Effective
Measurement Parameter
Activity
Qualitative value
@
Cornelius K. Cain; Annual reports in medicinal chemistry; vol. 2; (1966); p. 24 - 32, View in Reaxys 28 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Compound was tested for sedative action in animals
Substance RN
1085184View in Reaxys
Measurement Parameter
Activity
Qualitative value
ND
Cornelius K. Cain; Annual reports in medicinal chemistry; vol. 1; (1965); p. 30 - 39, View in Reaxys 29 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Tranquilizing effect of the compound was determined in children; mild
Biological Species/NCBI ID
human
Substance RN
1085184View in Reaxys
Measurement Parameter
Activity
Measurement Object
Tranquilizing activity
Qualitative value
ND
R. Ian Fryer; Annual reports in medicinal chemistry; vol. 5; (1969); p. 1 - 30, View in Reaxys 30 of 30
Bioassay Category
In Vitro (Efficacy)
Bioassay Details
Dose of the compound required for chronic psychotic patients
Biological Species/NCBI ID
human
Substance RN
1085184View in Reaxys
Measurement Parameter
dose
Unit
mg/day
Measurement Object
Chronic psychotic patients
Qualitative value
=
Quantitative value
2100
Irwin J. Pachter; Alan A. Rubin; Annual reports in medicinal chemistry; vol. 3; (1967); p. 1 - 13, 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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