Etizolam [C17H15ClN4S] by Asch

Query Query

Results

Date

1 substances in Reaxys

2018-05-20 18h:29m:23s (UTC)

S Cl

1. Query N N N

Search as: As drawn ) AND (IDE.XRN=572740))

1/80

2018-05-20 18:30:51

Reaxys ID 572740 View in Reaxys

1/1 CAS Registry Number: 40054-69-1 Chemical Name: etizolam; Etizolam; ZINC00001402; Depas; 4-(2chloro-phenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepine; etinozolam Linear Structure Formula: C17H15ClN4S Molecular Formula: C17H15ClN4S Molecular Weight: 342.852 Type of Substance: heterocyclic InChI Key: VMZUTJCNQWMAGF-UHFFFAOYSA-N Note:

S Cl

N N N

Substance Label (8) Label References 220

Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki; Drug Metabolism and Disposition; vol. 43; nb. 6; (2015); p. 812 - 818, View in Reaxys

Merck 3904

Sanna, Enrico; Busonero, Fabio; Talani, Giuseppe; Mostallino, Maria Cristina; Mura, Maria Luisa; Pisu, Maria Giuseppina; Maciocco, Elisabetta; Serra, Mariangela; Biggio, Giovanni; European Journal of Pharmacology; vol. 519; nb. 1-2; (2005); p. 31 - 42, View in Reaxys

Kawakami; Kitani; Yuasa; Abe; Moriwaki; Kagoshima; Terasawa; Tahara; European Journal of Medicinal Chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys

Tahara; Mikashima; Terasawa; Maruyama; Chemical and pharmaceutical bulletin; vol. 35; nb. 5; (1987); p. 2119 2121, View in Reaxys

Weber,K.-H. et al.; Justus Liebigs Annalen der Chemie; (1978); p. 1257 - 1265, View in Reaxys

Tahara; Araki; Shiroki; Matsuo; Munakata; Arzneimittel-Forschung/Drug Research; vol. 28; nb. 7; (1978); p. 1153 1158, View in Reaxys

S. 19

Patent; C.H. Boehringer Sohn; FR2318165; (1977); DE2531677; (1977); Chem.Abstr.; vol. 86; nb. 171521, View in Reaxys

Patent; Yoshitomi Pharm.; DE2229845; (1972); Chem.Abstr.; vol. 78; nb. 84416, View in Reaxys

Patent-Specific Data (1) Location in Patent References Claim

Patent; ALTERGON S.A.; EP1273301; (2003); (A2) English, View in Reaxys; Patent; Nippon Shinyaju Co., Ltd.; US5811547; (1998); (A) English, View in Reaxys; Patent; Northern Sydney Area Health Service; US5240922; (1993); (A) English, View in Reaxys; Patent; Golwyn; Daniel H.; US5147872; (1992); (A) English, View in Reaxys

Druglikeness (1) 1 of 1

LogP

5.113

H Bond Donors

H Bond Acceptors

Rotatable Bonds

TPSA

71.31

Lipinski Number

Veber Number

Highest Clinical Phase (1) Highest Clinical Phase Marketed Derivative (2) Comment (Derivative)

References

Dihydrobromid: F: 175grad (Zers)

Patent; Iosilomi Seijaku; JP515397; (1976); Ref. Zh., Khim.; vol. 3; nb. O150; (1977), View in Reaxys

Dihydrochlorid: F: 195-196gradC (Schaeumen bei 175gradC)

Patent; Yoshitomi Pharm.; DE2229845; (1972); Chem.Abstr.; vol. 78; nb. 84416, View in Reaxys

Melting Point (3)

2/80

2018-05-20 18:30:51

1 of 3

Melting Point [°C]

147 - 148

Tahara; Araki; Shiroki; Matsuo; Munakata; Arzneimittel-Forschung/Drug Research; vol. 28; nb. 7; (1978); p. 1153 - 1158, View in Reaxys 2 of 3

Melting Point [°C]

144 - 146

Weber,K.-H. et al.; Justus Liebigs Annalen der Chemie; (1978); p. 1257 - 1265, View in Reaxys; Patent; Boehringer; DE2533924; (1977); Chem.Abstr.; vol. 86; nb. 171518, View in Reaxys; Patent; C.H. Boehringer Sohn; FR2318165; (1977); DE2531677; (1977); Chem.Abstr.; vol. 86; nb. 171521, View in Reaxys 3 of 3

Melting Point [°C]

147 - 148

Solvent (Melting Point)

petroleum ether; acetone

Patent; Iosilomi Seijaku; JP515397; (1976); Ref. Zh., Khim.; vol. 3; nb. O150; (1977), View in Reaxys Electrochemical Behaviour (1) Description (Elec- References trochemical Behaviour) Electrolytic dissoci- Inotsume; Nakano; Chemical and Pharmaceutical Bulletin; vol. 28; nb. 8; (1980); p. 2536 - 2540, View in Reaxys ation / protonation equilibrium Further Information (1) Description (FurReferences ther Information) Further information Patent; Iosilomi Seijaku; JP515397; (1976); Ref. Zh., Khim.; vol. 3; nb. O150; (1977), View in Reaxys Partition octan-1-ol/water (MCS) (2) 1 of 2

log POW

3.03

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 2 of 2

log POW

2.98

Location

supporting information

Stratton, Christopher F.; Newman, David J.; Tan, Derek S.; Bioorganic and Medicinal Chemistry Letters; vol. 25; nb. 21; (2015); p. 4802 - 4807, View in Reaxys Solubility (MCS) (1) 1 of 1

Solubility [g·l-1]

0.164569

Saturation

in solution

Temperature (Solubility (MCS)) [°C]

Solvent (Solubility (MCS))

phosphate buffer

Alelyunas, Yun W.; Empfield, James R.; McCarthy, Dennis; Spreen, Russell C.; Bui, Khanh; Pelosi-Kilby, Luciana; Shen, Cindy; Bioorganic and Medicinal Chemistry Letters; vol. 20; nb. 24; (2010); p. 7312 - 7316, View in Reaxys UV/VIS Spectroscopy (1) 1 of 1

Description (UV/VIS Spectroscopy)

Spectrum

Solvent (UV/VIS Spectroscopy)

aq. HCl

Comment (UV/VIS Spectroscopy)

220 - 370 nm

Inotsume; Nakano; Chemical and Pharmaceutical Bulletin; vol. 28; nb. 8; (1980); p. 2536 - 2540, View in Reaxys Use (24) Use Pattern

References

short-acting hypnotic agent

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Hypnotic agent

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

3/80

2018-05-20 18:30:51

Sleep disturbance

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Obstructive sleep insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Narcolepsy

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Breathing-related sleep disorder

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Circadian rhythm sleep disorder

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Parasomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Sleep apnea insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys

Sleep disorders

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Primary insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Substance induced sleep disorder

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Sleep disorder related to another mental disorder

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Short acting hypnotic agent

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Sleep maintenance insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Insomnia related to another mental disorder

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Substance induced insomnia

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/138413; (2008); (A1) English, View in Reaxys; Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Onstructive sleep apnea

Patent; AVENTIS PHARMACEUTICALS INC.; US2008/139615; (2008); (A1) English, View in Reaxys

Depression disorders

Patent; Takeda Pharmaceutical Company Limited; EP1867641; (2007); (A1) English, View in Reaxys

Anxiety disorders

Patent; Takeda Pharmaceutical Company Limited; EP1867641; (2007); (A1) English, View in Reaxys

Depression of patients having a background od diabetes, hyperlipidemia, hypertension or metabolic syndrome

Patent; Takeda Pharmaceutical Company Limited; EP1867641; (2007); (A1) English, View in Reaxys

Anxiety disorders of patients having a background od diabetes, hyperlipidemia, hypertension or metabolic syndrome

Patent; Takeda Pharmaceutical Company Limited; EP1867641; (2007); (A1) English, View in Reaxys

Antianxiety drug

Patent; Takeda Pharmaceutical Company Limited; EP1867641; (2007); (A1) English, View in Reaxys

Medchem (195) 1 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

4/80

2018-05-20 18:30:51

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.5

Deviation

4.10000

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 2 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

Deviation

0.500000

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 3 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

194.8

5/80

2018-05-20 18:30:51

Deviation

88.9000

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 4 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

11.1

Deviation

4.60000

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 5 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.5

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 6 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

6/80

2018-05-20 18:30:51

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 7 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

194.8

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 8 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

11.1

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 9 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

7/80

2018-05-20 18:30:51

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax i/Cmax

Quantitative value

0.8

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 10 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC i/AUC (0-inf)

Quantitative value

0.58

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 11 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

0.64

8/80

2018-05-20 18:30:51

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 12 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

13.9

Deviation

4.10000

Statistical sgnificance (pvalue)

0.05

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 13 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.4

Deviation

0.700000

9/80

2018-05-20 18:30:51

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 14 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

105.9

Deviation

33.4000

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 15 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

10/80

2018-05-20 18:30:51

Quantitative value

6.8

Deviation

2.80000

Statistical sgnificance (pvalue)

0.01

Concomitants: Compound RN

1246090

Concomitants: Compound name

Carbamazepine

Concomitants: Compound role

ICP

Kondo; Fukasawa; Yasui-Furukori; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 3; (2005); p. 185 - 188, View in Reaxys 16 of 195

17 of 195

Target Name

Platelet-activating factor receptor [Leporidae]

Target Synonyms

platelet-activating factor receptor

Target, Subunit, Species

Platelet-activating factor receptor [Leporidae]

Target Mutant/Chimera Details

Platelet-activating factor receptor [Leporidae]:Wild

Target Species (Bioactivity)

Leporidae

Target Transfection

Non Transfected

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Blood aggregation

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

platelet-rich plasma cell

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

IC50

Unit

µM

Quantitative value

3.8

Measurement pX

5.42

Target Name

Platelet-activating factor receptor [Leporidae]

Target Synonyms

platelet-activating factor receptor

Target, Subunit, Species

Platelet-activating factor receptor [Leporidae]

Target Mutant/Chimera Details

Platelet-activating factor receptor [Leporidae]:Wild

Target Species (Bioactivity)

Leporidae

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

11/80

2018-05-20 18:30:51

18 of 195

19 of 195

Substance Name

Etizolam

Measurement Parameter

IC50

Unit

Quantitative value

Measurement pX

7.66

Target Name

GABA-A receptor [Rattus norvegicus]

Target Synonyms

gaba-a receptor

Target, Subunit, Species

GABA-A receptor [Rattus norvegicus]

Target Mutant/Chimera Details

GABA-A receptor [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Chbb:THOM rat

Organs/Tissues

brain cortex

Cell Fraction

Membrane

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

IC50

Unit

Quantitative value

Measurement pX

8.3

Concomitants: Compound RN

754371; 702691

Concomitants: Compound name

Diazepam; [3H]-Flunitrazepam

Concomitants: Compound role

NSB; RAD

Target Name

Platelet-activating factor receptor [human]

Target Synonyms

paf-r; pafr; platelet-activating factor receptor; ptafr

Target Uniprot ID

p25105

Target PDB ID

2b0x

Target, Subunit, Species

Platelet-activating factor receptor [human]

Target Mutant/Chimera Details

Platelet-activating factor receptor [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Blood aggregation

12/80

2018-05-20 18:30:51

20 of 195

Biological Species/NCBI ID

human

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1.00000E-08 M

Measurement Parameter

IC50

Unit

µM

Quantitative value

0.5

Measurement pX

6.3

Target Name

Platelet-activating factor receptor [Leporidae]

Target Synonyms

platelet-activating factor receptor

Target, Subunit, Species

Platelet-activating factor receptor [Leporidae]

Target Mutant/Chimera Details

Platelet-activating factor receptor [Leporidae]:Wild

Target Species (Bioactivity)

Leporidae

Target Transfection

Non Transfected

Substance Action on Target

Antagonist

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Blood aggregation

Biological Species/NCBI ID

Leporidae

Organs/Tissues

blood

Cells/Cell Lines

platelet-rich plasma cell

Substance RN

572740View in Reaxys

Substance Name

1 (Etizolam)

Measurement Parameter

IC50

Unit

Quantitative value

6730

Deviation

3250

Measurement pX

5.17

Kawakami; Kitani; Yuasa; Abe; Moriwaki; Kagoshima; Terasawa; Tahara; European Journal of Medicinal Chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 21 of 195

Target Name

Platelet-activating factor receptor [human]

Target Synonyms

paf-r; pafr; platelet-activating factor receptor; ptafr

Target Uniprot ID

p25105

Target PDB ID

2b0x

Target, Subunit, Species

Platelet-activating factor receptor [human]

Target Mutant/Chimera Details

Platelet-activating factor receptor [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

13/80

2018-05-20 18:30:51

Bioassay Name

Binding

Biological Species/NCBI ID

human

Organs/Tissues

blood

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Substance Name

1 (Etizolam)

Measurement Parameter

IC50

Unit

Quantitative value

29.5

Deviation

6.20000

Measurement pX

7.53

Kawakami; Kitani; Yuasa; Abe; Moriwaki; Kagoshima; Terasawa; Tahara; European Journal of Medicinal Chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 22 of 195

Target Name

GABA-A receptor [Rattus norvegicus]

Target Synonyms

gaba-a receptor

Target, Subunit, Species

GABA-A receptor [Rattus norvegicus]

Target Mutant/Chimera Details

GABA-A receptor [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

Rattus norvegicus

Organs/Tissues

brain

Cell Fraction

Synaptosome: membrane (P2 fraction)

Substance RN

572740View in Reaxys

Substance Name

1 (Etizolam)

Measurement Parameter

Ki (inhibition constant)

Unit

Quantitative value

2.34

Deviation

0.0700000

Measurement pX

8.63

Concomitants: Compound RN

754371; 754371

Concomitants: Compound name

Diazepam; [3H]-Diazepam

Concomitants: Compound role

NSB; RAD

Kawakami; Kitani; Yuasa; Abe; Moriwaki; Kagoshima; Terasawa; Tahara; European Journal of Medicinal Chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 23 of 195

Target Name

GABA-A receptor [Rattus norvegicus]

Target Synonyms

gaba-a receptor

Target, Subunit, Species

GABA-A receptor [Rattus norvegicus]

14/80

2018-05-20 18:30:51

Target Mutant/Chimera Details

GABA-A receptor [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

CD rat

Organs/Tissues

brain cortex

Cell Fraction

Membrane

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1.00000E-11 M

Measurement Parameter

IC50

Unit

Quantitative value

4.5

Measurement pX

8.35

Concomitants: Compound RN

754371; 702691

Concomitants: Compound name

Diazepam; [3H]-Flunitrazepam

Concomitants: Compound role

NSB; RAD

Sanna, Enrico; Pau, Davide; Tuveri, Francesca; Massa, Federico; Maciocco, Elisabetta; Acquas, Cinzia; Floris, Chiara; Fontana, Simona N.; Maira, Giovanna; Biggio, Giovanni; Arzneimittel-Forschung/Drug Research; vol. 49; nb. 2; (1999); p. 88 - 95, View in Reaxys 24 of 195

Target Name

GABA-A receptor [Rattus norvegicus]

Target Synonyms

gaba-a receptor

Target, Subunit, Species

GABA-A receptor [Rattus norvegicus]

Target Mutant/Chimera Details

GABA-A receptor [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

CD rat

Organs/Tissues

brain cortex

Cell Fraction

Membrane

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

3 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

100

15/80

2018-05-20 18:30:51

Measurement pX

6.8

Concomitants: Compound RN

754371; 702691

Concomitants: Compound name

Diazepam; [3H]-Flunitrazepam

Concomitants: Compound role

NSB; RAD

Target Name

Gamma-aminobutyric acid receptor subunit beta-2 [human];+Gamma-aminobutyric acid receptor subunit alpha-1 [human];+GABA-A receptor (Gamma 2S) [human]

Target Synonyms

gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba(a) receptor subunit alpha-1; gabra1; gamma-aminobutyric acid receptor subunit alpha-1 + gaba-a receptor (gamma 2s)

Target Uniprot ID

p47870 + p14867

Target, Subunit, Species

GABA-A receptor (Gamma 2S) [human]; Gamma-aminobutyric acid receptor subunit alpha-1 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]

Target Mutant/Chimera Details

Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Allosteric Modulator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

EC50

Unit

Quantitative value

Measurement pX

7.04

Concomitants: Compound RN

906818

Concomitants: Compound name

GABA

Concomitants: Compound role

AGO

Target Name

Gamma-aminobutyric acid receptor subunit alpha-2 [human];+Gamma-aminobutyric acid receptor subunit beta-2 [human];+GABA-A receptor (Gamma 2S) [human]

Target Synonyms

gaba(a) receptor subunit alpha-2; gabra2; gamma-aminobutyric acid receptor subunit alpha-2 + gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba-a receptor (gamma 2s)

Target Uniprot ID

p47869 + p47870

16/80

2018-05-20 18:30:51

Target, Subunit, Species

GABA-A receptor (Gamma 2S) [human]; Gamma-aminobutyric acid receptor subunit alpha-2 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]

Target Mutant/Chimera Details

Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Allosteric Modulator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

EC50

Unit

Quantitative value

Measurement pX

7.27

Concomitants: Compound RN

906818

Concomitants: Compound name

GABA

Concomitants: Compound role

AGO

Target Name

Gamma-aminobutyric acid receptor subunit beta-2 [human];+GABA-A receptor (Gamma 2S) [human];+Gamma-aminobutyric acid receptor subunit alpha-3 [human]

Target Synonyms

gaba(a) receptor subunit beta-2; gabrb2; gamma-aminobutyric acid receptor subunit beta-2 + gaba-a receptor (gamma 2s) + gaba(a) receptor subunit alpha-3; gabra3; gamma-aminobutyric acid receptor subunit alpha-3

Target Uniprot ID

p47870 + p34903

Target, Subunit, Species

GABA-A receptor (Gamma 2S) [human]; Gamma-aminobutyric acid receptor subunit alpha-3 [human]; Gamma-aminobutyric acid receptor subunit beta-2 [human]

Target Mutant/Chimera Details

Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild

Target Species (Bioactivity)

human

Substance Action on Target

Allosteric Modulator

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Electrophysiology

Biological Species/NCBI ID

Xenopus laevis

Cells/Cell Lines

oocyte

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

EC50

17/80

2018-05-20 18:30:51

Unit

Quantitative value

Measurement pX

7.02

Concomitants: Compound RN

906818

Concomitants: Compound name

GABA

Concomitants: Compound role

AGO

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Brain biochemistry : Others

Biological Species/NCBI ID

CD rat

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

3 mg/kg

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Inhibition

Unit

Measurement Object

Maximal inhibition of basal acetylcholine release

Quantitative value

Concomitants: Compound RN

3615946

Concomitants: Compound name

Neostigmine

Concomitants: Compound role

OCV

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Brain biochemistry : Others

Biological Species/NCBI ID

CD rat

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

3 mg/kg

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Inhibition

Unit

Measurement Object

Maximal inhibition of basal acetylcholine release

18/80

2018-05-20 18:30:51

Quantitative value

Concomitants: Compound RN

3615946

Concomitants: Compound name

Neostigmine

Concomitants: Compound role

OCV

Bioassay Category

In Vivo (Animal models)

Bioassay Name

Brain biochemistry : Others

Biological Species/NCBI ID

CD rat

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1.50000 mg/kg

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

% Inhibition

Unit

Measurement Object

Maximal inhibition of basal acetylcholine release

Quantitative value

Concomitants: Compound RN

3615946

Concomitants: Compound name

Neostigmine

Concomitants: Compound role

OCV

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

CD rat

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

0.500000 mg/kg

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

percentage

Unit

Measurement Object

Increase of acetylcholine release

Quantitative value

57 - 130

19/80

2018-05-20 18:30:51

Concomitants: Compound RN

3615946

Concomitants: Compound name

Neostigmine

Concomitants: Compound role

OCV

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Biological Species/NCBI ID

CD rat

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

0.500000 mg/kg

Substance Route of Adm.

intraperitoneal administration

Substance Dosing Regimen

Single

Measurement Parameter

percentage

Unit

Measurement Object

Increase of acetylcholine release

Quantitative value

78 - 170

Concomitants: Compound RN

3615946

Concomitants: Compound name

Neostigmine

Concomitants: Compound role

OCV

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.3

Deviation

6.80000

20/80

2018-05-20 18:30:51

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 34 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

Deviation

0.500000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 35 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 d)

Unit

ng.h/mL

Quantitative value

105

Deviation

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 36 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

21/80

2018-05-20 18:30:51

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

178

Deviation

122

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 37 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

10.5

Deviation

3.90000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 38 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

20.7

Deviation

6.70000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 39 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

22/80

2018-05-20 18:30:51

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.1

Deviation

0.600000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 40 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 d)

Unit

ng.h/mL

Quantitative value

158

Deviation

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 41 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

287

Deviation

23/80

2018-05-20 18:30:51

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 42 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

14.8

Deviation

4.20000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 43 of 195

Target Name

Cytochrome P450 2C19 [human]

Target Synonyms

(r)-limonene 6-monooxygenase; (s)-limonene 6-monooxygenase; (s)-limonene 7-monooxygenase; cyp2c19; cypiic17; cypiic19; cytochrome p450 2c19; cytochrome p450-11a; cytochrome p450-254c; mephenytoin 4-hydroxylase

Target Uniprot ID

p33261

Target PDB ID

4gqs

Target, Subunit, Species

Cytochrome P450 2C19 [human]

Target Mutant/Chimera Details

Cytochrome P450 2C19 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

fm(E)

Measurement Object

Phenotyping (AUC)

Quantitative value

0.38

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys

24/80

2018-05-20 18:30:51

44 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

15.4

Deviation

5.90000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 45 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

0.7

Deviation

0.300000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 46 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

25/80

2018-05-20 18:30:51

Unit

ng.h/mL

Quantitative value

Deviation

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 47 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

113

Deviation

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 48 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

8.3

Deviation

2.10000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 49 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

26/80

2018-05-20 18:30:51

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

18.7

Deviation

7.50000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 50 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.1

Deviation

0.600000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 51 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

ng.h/mL

Quantitative value

138

Deviation

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 52 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

27/80

2018-05-20 18:30:51

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

224

Deviation

142

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 53 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

Deviation

4.20000

Fukasawa; Yasui-Furukori; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 61; nb. 11; (2005); p. 791 - 795, View in Reaxys 54 of 195

Target Name

Platelet-activating factor receptor [human]

Target Synonyms

paf-r; pafr; platelet-activating factor receptor; ptafr

Target Uniprot ID

p25105

Target PDB ID

2b0x

Target, Subunit, Species

Platelet-activating factor receptor [human]

Target Mutant/Chimera Details

Platelet-activating factor receptor [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Binding

Biological Species/NCBI ID

human

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55 of 195

Organs/Tissues

blood

Cells/Cell Lines

leukocyte

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

Ki (inhibition constant)

Unit

Quantitative value

320

Deviation

Measurement pX

6.49

Bioassay Category

Metabolism/Transport

Bioassay Name

Binding

Biological Species/NCBI ID

human

Organs/Tissues

plasma

Substance RN

572740View in Reaxys

Substance Name

etizolam

Measurement Parameter

fu (unbound fraction)

Quantitative value

0.07

Votano, Joseph R.; Parham, Marc; Hall, L. Mark; Hall, Lowell H.; Kier, Lemont B.; Oloff, Scott; Tropsha, Alexander; Journal of Medicinal Chemistry; vol. 49; nb. 24; (2006); p. 7169 - 7181, View in Reaxys 56 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.7

Deviation

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 57 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

29/80

2018-05-20 18:30:51

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.1

Deviation

0.600000

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 58 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

ng.h/mL

Quantitative value

154

Deviation

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 59 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

213

Deviation

106

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 60 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

30/80

2018-05-20 18:30:51

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

Deviation

5.40000

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 61 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.7

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 62 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.1

31/80

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Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 63 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

ng.h/mL

Quantitative value

154

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 64 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

213

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 65 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

32/80

2018-05-20 18:30:51

Unit

hour

Quantitative value

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 66 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax i/Cmax

Quantitative value

0.99

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 67 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC i/AUC (0-24 h)

Quantitative value

1.25

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 68 of 195

Bioassay Category

Pharmacokinetic

33/80

2018-05-20 18:30:51

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC i/AUC (0-inf)

Quantitative value

1.53

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 69 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el i/t1/2 el

Quantitative value

1.48

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 70 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

34/80

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Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

unit.h

Quantitative value

2262

Deviation

227

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 71 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

unit.h

Quantitative value

61.4

Deviation

10.2000

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 72 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

Cmax

Unit

ng/mL

Quantitative value

17.3

Deviation

3.70000

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

4290027

35/80

2018-05-20 18:30:51

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 73 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.1

Deviation

0.600000

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 74 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-24 h)

Unit

ng.h/mL

Quantitative value

191

Deviation

Statistical sgnificance (pvalue)

0.001

36/80

2018-05-20 18:30:51

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 75 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

AUC (0-inf)

Unit

ng.h/mL

Quantitative value

326

Deviation

166

Statistical sgnificance (pvalue)

0.001

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 76 of 195

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

t1/2 el

Unit

hour

Quantitative value

17.3

Deviation

7.40000

37/80

2018-05-20 18:30:51

Statistical sgnificance (pvalue)

0.01

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Araki; Yasui-Furukori; Fukasawa; Aoshima; Suzuki; Inoue; Tateishi; Otani; European Journal of Clinical Pharmacology; vol. 60; nb. 6; (2004); p. 427 - 430, View in Reaxys 77 of 195

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Effect : |receptor; binding activity Target : CD-1 mouseBioassay : GABA: 4-aminobutanoic acid 12, 48 or 96 h after discontinuation of treatment cerebral cortex dissected, fresh brain tissue homogenized and centrifuged; binding of tert-butyl-<35S>bicyclophosphorothionate (<35S>TBPS) to GABAA receptor in cerebrocortical membranes determined

Substance RN

572740View in Reaxys

Substance Name

91587

Substance Dose

1.50000 mg/kg

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

no effect of title comp. withdrawal on <35S>TBPS binding at any of time points examined; table

Measurement Parameter

qualitative

Substance Effect

Anticonvulsant

Bioassay Category

In Vivo (Animal models)

Bioassay Name

In vivo Measurement

Bioassay Details

Target : CD-1 mouseBioassay : mice injected with title comp. (challenge dose) together with 200 mg/kg s.c. isoniazid 36 h after (or without) chronic title comp. treatment; latency of convulsions, no. of animals with convulsions and no. of animals dying observed for 3 h

Substance RN

572740View in Reaxys

Substance Name

91587

Substance Dose

1 mg/kg

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

challenge dose of title comp. delayed onset of seizures (from 47 to 85 min); chronic title comp. treatment slightly reduced anticonvulsant activity, while challenge dose after chronic treatment antagonised seizure activity and death; table

Measurement Parameter

qualitative

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : GABAA receptor gene expression; effect onBioassay : α1 and α4 subunit abundance determined by immunocytofluorescence analysis; GABA: 4-aminobutanoic acid; α2S: short splice variant of α2 neurons exposed to title comp. for 5 d with replacement of culture medium daily, then incubated (or not) for 6 h in title comp.-free medium; amount of α1, α2, α3, α4, α5 and α2S subunit mRNAs of receptor determined by RNase protection assay

Biological Species/NCBI ID

Rattus norvegicus

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Cells/Cell Lines

nerve cell

Substance RN

572740View in Reaxys

Substance Name

91587

Substance Dose

10 µM

Qualitative Results

chronic treatment: decreased α5 and α2S subunit mRNAs; withdrawal: increased α2 and α3 subunit mRNAs and returned α5 subunit mRNA to control; diagrams

Measurement Parameter

qualitative

Target Name

GABA-A receptor

Target Synonyms

gaba-a receptor; gaba-a receptor activity; ionotropic gaba receptor

Target, Subunit, Species

GABA-A receptor

Target Mutant/Chimera Details

GABA-A receptor:Wild

Target Transfection

Non Transfected

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Bioassay Details

Effect : GABAA receptor function; effect onBioassay : GABA: 4-aminobutanoic acid; reference: flumazenil neurons exposed to 10 μmol/l title comp. for 5 d, then incubated (or not) for 6 h in title comp.-free medium; acute effect of 1 μmol/l title comp. on 3 μmol/l GABA-induced Cl(-) current measured by whole-cell electrophysiological recording

Biological Species/NCBI ID

Rattus norvegicus

Cells/Cell Lines

nerve cell

Substance RN

572740View in Reaxys

Substance Name

91587

Substance Dose

1 µM

Qualitative Results

acute title comp. treatment potentiated GABA-induced Cl(-) current by 104 percent, which effect was not significantly altered after chronic title comp. treatment or title comp. withdrawal; diagrams

Measurement Parameter

qualitative

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

1,8-cineole 2-exo-monooxygenase; albendazole monooxygenase; albendazole sulfoxidase; cholesterol 25-hydroxylase; cyp3a3; cyp3a4; cypiiia3; cypiiia4; cytochrome p450 3a3; cytochrome p450 3a4; cytochrome p450 hlp; cytochrome p450 nf-25; cytochrome p450-pcn1; nifedipine oxidase; quinine 3-monooxygenase; taurochenodeoxycholate 6-alpha-hydroxylase

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

39/80

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82 of 195

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

50 µM

Measurement Parameter

Km (Michaelis constant)

Unit

µM

Measurement Object

ALL

Quantitative value

219

Deviation

Measurement pX

3.66

Concomitants: Compound RN

19279336

Concomitants: Compound name

NADPH regenerating System

Concomitants: Compound role

COM

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

50 µM

Measurement Parameter

Vmax

Unit

pmol/min/mg protein

Measurement Object

ALL

Quantitative value

3244

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83 of 195

84 of 195

Deviation

124

Concomitants: Compound RN

19279336

Concomitants: Compound name

NADPH regenerating System

Concomitants: Compound role

COM

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology substrate

Biological Species/NCBI ID

human

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

50 µM

Measurement Parameter

CLint

Unit

µL/min/mg protein

Measurement Object

ALL

Quantitative value

14.8

Concomitants: Compound RN

19279336

Concomitants: Compound name

NADPH regenerating System

Concomitants: Compound role

COM

Substance Effect

Anxiolytic

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

qualitative

Qualitative value

; (2012); Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00, View in Reaxys

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85 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

In Vitro (others)

Substance RN

572740View in Reaxys

Substance Name

91587

Qualitative Results

ability to antagonize PAF-induced platelet aggregation (rabbit PRP); IC 50: 1.3 μg/ml and bronchoconstriction (guinea pig); 100 percent

Measurement Parameter

qualitative

Tahara; Mikashima; Terasawa; Maruyama; Chemical and pharmaceutical bulletin; vol. 35; nb. 5; (1987); p. 2119 - 2121, View in Reaxys 86 of 195

87 of 195

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Substance Dose

1 mg

Substance Route of Adm.

oral administration

Substance Dosing Regimen

Single

Measurement Parameter

fm(E)

Measurement Object

Chemical inhibition

Quantitative value

0.35

Concomitants: Compound RN

4290027

Concomitants: Compound name

Itraconazole

Concomitants: Compound role

ICP

Target Name

Cytochrome P450 2C19 [human]

Target Synonyms

Target Uniprot ID

p33261

42/80

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88 of 195

Target PDB ID

4gqs

Target, Subunit, Species

Cytochrome P450 2C19 [human]

Target Mutant/Chimera Details

Cytochrome P450 2C19 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Non Transfected

Bioassay Category

Pharmacokinetic

Bioassay Name

Pharmacokinetic

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Substance Name

Etizolam

Measurement Parameter

fm(E)

Measurement Object

Phenotyping

Quantitative value

0.38

Bioassay Category

Pharmacokinetic

Bioassay Details

Percent excretion of unchanged compound in urine of human upon oral administration

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

percentage of dose excreted in urine

Unit

Measurement Object

AMOUNT OF UNCHANGED DRUG EXCRETED

Qualitative value

Quantitative value

0.3

Benet, Leslie Z.; Broccatelli, Fabio; Oprea, Tudor I.; AAPS Journal; vol. 13; nb. 4; (2011); p. 519 - 547, View in Reaxys 89 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration time curve in rat after 10 mg/Kg compound oral dose in presence of Tokisyakuyakusan (0.1 g/kg); control= 34+/-4.9 ug.min/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

AUC

Unit

µg.min/mL

Qualitative value

Quantitative value

23.3

Deviation

4.3

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 90 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (1 g/kg); Control= 12.2+/-1.2 min

43/80

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Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

Activity

Unit

nmol

Measurement Object

recovery

Qualitative value

Quantitative value

11.9

Deviation

1.3

Concomitants: Compound name

Kamisyoyosan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 91 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Variance of residence time of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (1 g/kg); control= 4450+/-1260 min.min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

qualitative

Measurement Object

VRT

Concomitants: Compound name

Kamisyoyosan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 92 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum plasma concentration of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (1 g/kg); Control= 17.5+/-2.8 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

Activity

Unit

nmol

Measurement Object

recovery

Qualitative value

Quantitative value

21.3

Deviation

4.5

44/80

2018-05-20 18:30:51

Concomitants: Compound name

Tokisyakuyakusan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 93 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Half Life of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (1 g/ kg); control= 39.1+/-2.6 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

Measurement Parameter

t1/2

Unit

minute

Measurement Object

Half Life

Qualitative value

Quantitative value

29.9

Deviation

4.2

Concomitants: Compound name

Tokisyakuyakusan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 94 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Variance of residence time of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (1 g/kg); control= 1240+/-171 min.min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

qualitative

Measurement Object

VRT

Concomitants: Compound name

Kamisyoyosan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 95 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Mean residence time of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (1 g/kg); control= 53.4+/-3.2 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

45/80

2018-05-20 18:30:51

Qualitative Results

Measurement Parameter

MRT

Unit

minute

Measurement Object

Mean residence time

Qualitative value

Quantitative value

50.3

Deviation

4.1

Concomitants: Compound name

Kamisyoyosan (0.1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 96 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration time curve in rat after 10 mg/Kg compound oral dose in presence of Kamisyoyosan (1 g/kg); control= 34+/-4.9 ug.min/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

AUC

Unit

µg.min/mL

Qualitative value

Quantitative value

30.5

Deviation

5.2

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 97 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Area under plasma concentration time curve in rat after 10 mg/Kg compound oral dose in presence of Tokisyakuyakusan ((1 g/kg); control= 22.6+/-3.2 ug.min/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

AUC

Unit

µg.min/mL

Qualitative value

Quantitative value

18.3

Deviation

3.1

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 98 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Mean residence time of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (1 g/kg); control= 42.5+/-3.5 min

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2018-05-20 18:30:51

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

MRT

Unit

minute

Measurement Object

Mean residence time

Qualitative value

Quantitative value

45.5

Deviation

2.9

Concomitants: Compound name

Kamisyoyosan (0.1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 99 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Variance of residence time of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (0.1 g/kg); control= 1240+/-171 min.min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

qualitative

Measurement Object

VRT

Concomitants: Compound name

Tokisyakuyakusan (0.1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 100 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Effect of Tokisyakuyakusan (1 g/kg) on maximum plasma concentration of the compound in rat after oral administration at a dose of 10 mg/kg; Control= 486+/-60 ng/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

MRT

Unit

minute

Qualitative value

Quantitative value

299

Deviation

47/80

2018-05-20 18:30:51

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 101 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Effect of Kamisyoyosan (1 g/kg) on maximum plasma concentration of the compound in rat after oral administration at a dose of 10 mg/kg; Control= 677+/-55 ng/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

Activity

Unit

nmol

Measurement Object

recovery

Qualitative value

Quantitative value

651

Deviation

126

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 102 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Mean residence time of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (0.1 g/kg); control= 42.5+/-3.5 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

MRT

Unit

minute

Measurement Object

Mean residence time

Qualitative value

Quantitative value

40.5

Deviation

4.3

Concomitants: Compound name

Kamisyoyosan (0.1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 103 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Half Life of the compound in rat after 10 mg/Kg oral dose in presence of Kamisyoyosan (1 g/kg); control= 36.2+/-5.4 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

t1/2

48/80

2018-05-20 18:30:51

Unit

minute

Measurement Object

Half Life

Qualitative value

Quantitative value

44.9

Deviation

6.8

Concomitants: Compound name

Kamisyoyosan (1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 104 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Effect of Tokisyakuyakusan (0.1 g/kg) on maximum plasma concentration of the compound in rat after oral administration at a dose of 10 mg/kg; Control= 677+/-55 ng/ml

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

Activity

Unit

nmol

Measurement Object

recovery

Qualitative value

Quantitative value

534

Deviation

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 105 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Time taken to reach maximum plasma concentration of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (0.1g/kg); Control= 12.2+/-1.2 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

MRT

Unit

minute

Qualitative value

Quantitative value

Deviation

0.9

Concomitants: Compound name

Tokisyakuyakusan (0.1g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 106 of 195

Bioassay Category

Pharmacokinetic

49/80

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Bioassay Details

Half Life of the compound in rat after 10 mg/Kg oral dose in presence of Tokisyakuyakusan (0.1 g/ kg); control= 36.2+/-5.4 min

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

Measurement Parameter

t1/2

Unit

minute

Measurement Object

Half Life

Qualitative value

Quantitative value

37.9

Deviation

5.4

Concomitants: Compound name

Tokisyakuyakusan (0.1 g/kg)

Concomitants: Compound role

COM

Makino, Toshiaki; Inagaki, Takahiro; Komatsu, Ken-ichi; Kano, Yoshihiro; Biological and pharmaceutical bulletin; vol. 28; nb. 2; (2005); p. 280 - 284, View in Reaxys 107 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Partition Coefficient of the compound was determined

Substance RN

572740View in Reaxys

Measurement Parameter

qualitative

Measurement Object

Partition coefficient

Qualitative value

Not Published

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon subcutaneous administration

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Qualitative Results

5000

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

5000

Oyo yakuri; vol. 16; (1978); p. 1021, View in Reaxys 109 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon intravenous administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

> 5000

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

5000

50/80

2018-05-20 18:30:51

Oyo yakuri; vol. 16; (1978); p. 1021, View in Reaxys 110 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon intraperitoneal administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

825

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

825

Oyo yakuri; vol. 16; (1978); p. 1021, View in Reaxys 111 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon p.o. administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

3509

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

3509

Oyo yakuri; vol. 16; (1978); p. 1021, View in Reaxys 112 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon intraperitoneal administration

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Qualitative Results

783

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

783

Oyo yakuri; vol. 16; (1978); p. 1021, View in Reaxys 113 of 195

Target Name

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Synonyms

bzrap1; peripheral-type benzodiazepine receptor-associated protein 1; prax-1; rbp1; rim-bp1; rimsbinding protein 1; tspo-associated protein 1; tspoap1

Target Uniprot ID

q9jir0

Target, Subunit, Species

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Inhibitor

51/80

2018-05-20 18:30:51

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of the compound against Benzodiazepine receptor using 2 nM 3H-DZP at pH 7.4 in synaptosomal memebrane of rat brain

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Measurement Parameter

Ki (inhibition constant)

Unit

Quantitative value

2.34

Measurement pX

8.63

Concomitants: Compound name

[3H]DZP

Concomitants: Compound role

RAD

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasaw; T Tahara; European journal of medicinal chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 114 of 195

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested in vitro for concentration required to inhibit rabbit platelet aggregation induced by platelet activating factor (PAF)

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

6730

Measurement pX

5.17

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasaw; T Tahara; European journal of medicinal chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 115 of 195

Target Name

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Synonyms

bzrap1; peripheral-type benzodiazepine receptor-associated protein 1; prax-1; rbp1; rim-bp1; rimsbinding protein 1; tspo-associated protein 1; tspoap1

Target Uniprot ID

q9jir0

Target, Subunit, Species

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for inhibitory effect of the compound against specific binding of 3H-diazepam to synaptosomal membrane of rat brains

Biological Species/NCBI ID

Rattus norvegicus

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Substance RN

572740View in Reaxys

Measurement Parameter

Ki (inhibition constant)

Unit

Qualitative value

Quantitative value

2.34

Measurement pX

8.63

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasaw; T Tahara; European journal of medicinal chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 116 of 195

Target Name

Platelet-activating factor receptor [Leporidae]

Target Synonyms

platelet-activating factor receptor

Target, Subunit, Species

Platelet-activating factor receptor [Leporidae]

Target Mutant/Chimera Details

Platelet-activating factor receptor [Leporidae]:Wild

Target Species (Bioactivity)

Leporidae

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for inhibitory effect of the compound against specific binding of 3H-Platelet activating factor receptor to washed platelets of rabbit

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

29.5

Measurement pX

7.53

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasaw; T Tahara; European journal of medicinal chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 117 of 195

Bioassay Category

In Vivo (Animal models)

Bioassay Details

Tested in vivo for effective dose required to prevent PAF-induced mortality in male ICR mice by 50 on peroral administration; not tested

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

ED50

Qualitative value

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasaw; T Tahara; European journal of medicinal chemistry; vol. 31; nb. 9; (1996); p. 683 - 692, View in Reaxys 118 of 195

Target Name

Peripheral-type benzodiazepine receptor-associated protein 1

Target Synonyms

bzrap1; kiaa0612; pbr-ip; peripheral benzodiazepine receptor-interacting protein; peripheral-type benzodiazepine receptor-associated protein 1; prax-1; rbp1; rim-bp1; rimbp1; rims-binding protein 1; tspo-associated protein 1; tspoap1

Target, Subunit, Species

Peripheral-type benzodiazepine receptor-associated protein 1

53/80

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Target Mutant/Chimera Details

Peripheral-type benzodiazepine receptor-associated protein 1:Wild

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Values of the receptor dissociation constant (Kd) of the compound was determined

Substance RN

572740View in Reaxys

Measurement Parameter

Kd (dissociation constant)

Unit

Measurement Object

Dissociation constant

Qualitative value

Quantitative value

4.9

Measurement pX

8.31

Ito, Kiyomi; Asakura, Akiko; Yamada, Yasuhiko; Nakamura, Kouichi; Sawada, Yasufumi; Iga, Tatsuji; Biopharmaceutics and Drug Disposition; vol. 18; nb. 4; (1997); p. 293 - 303, View in Reaxys 119 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Plasma binding of the compound was determined

Substance RN

572740View in Reaxys

Qualitative Results

93.2

Measurement Parameter

plasma protein binding

Unit

Measurement Object

Plasma binding

Quantitative value

93.2

Substance Action on Target

Radioligand (/ligand)

Bioassay Category

Pharmacokinetic

Bioassay Details

Maximum plasma concentration of the compound was determined

Substance RN

572740View in Reaxys

Qualitative Results

0.0388

Measurement Parameter

Cmax

Unit

µM

Quantitative value

0.0388

Bioassay Category

Pharmacokinetic

Bioassay Details

Time to peak plasma concentration of compound upon single oral administration to healthy males

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

0.9

Measurement Parameter

tmax

Unit

hour

Quantitative value

0.9

Clarke's Analysis of Drugs and Poisons, View in Reaxys 122 of 195

Bioassay Category

Toxicity/Safety Pharmacology

54/80

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Bioassay Details

Lethal doe in rat;Intraperitoneal

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

intraperitoneal administration

Measurement Parameter

LD50

Unit

g/kg

Qualitative value

Quantitative value

825

Material Safety Data Sheet, View in Reaxys 123 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal doe in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

3070

Material Safety Data Sheet, View in Reaxys 124 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal doe in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

783

Material Safety Data Sheet, View in Reaxys 125 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Etizolam is rapidly absorbed after oral administration

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Measurement Parameter

Absorption

Qualitative value

Clarke's Analysis of Drugs and Poisons, View in Reaxys 126 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration of compound upon oral administration in healthy males for 0.9 h

Biological Species/NCBI ID

human

55/80

2018-05-20 18:30:51

Substance RN

572740View in Reaxys

Qualitative Results

0.0083

Measurement Parameter

Cmax

Unit

µg/mL

Quantitative value

0.0083

Clarke's Analysis of Drugs and Poisons, View in Reaxys 127 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Time to peak plasma concentration of compound upon multiple oral administration in healthy males for 12 h for 1 week

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

1.2

Measurement Parameter

tmax

Unit

hour

Quantitative value

1.2

Clarke's Analysis of Drugs and Poisons, View in Reaxys 128 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Clearance value of compound upon oral administration; Range is 10.4-19.3

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

5.36

Measurement Parameter

CL (drug clearance)

Unit

mL/min/kg

Quantitative value

5.36

Clarke's Analysis of Drugs and Poisons, View in Reaxys 129 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Half Life value of compound

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

~3.4

Measurement Parameter

t1/2 el

Unit

hour

Measurement Object

Half Life

Quantitative value

3.4

Clarke's Analysis of Drugs and Poisons, View in Reaxys 130 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lowest published lethal dose in mouse

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

56/80

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Unit

g/kg

Qualitative value

Quantitative value

Material Safety Data Sheet, View in Reaxys 131 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Volume of distribution upon oral administration

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

1.0

Measurement Parameter

Vd (volume of distribution)

Unit

L/kg

Quantitative value

Clarke's Analysis of Drugs and Poisons, View in Reaxys 132 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration of compound upon oral administration in healthy males for 12 h for 1 week

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

0.0099

Measurement Parameter

Cmax

Unit

µg/mL

Quantitative value

0.0099

Clarke's Analysis of Drugs and Poisons, View in Reaxys 133 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Plasma protein binding

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

Measurement Parameter

plasma protein binding

Unit

Measurement Object

Plasma binding

Quantitative value

Clarke's Analysis of Drugs and Poisons, View in Reaxys 134 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Peak plasma concentration of metabolite alpha-hydroxyetizolam upon oral administration in healthy males for 12 h for 1 week

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

0.0093

Measurement Parameter

Cmax

Unit

µg/mL

57/80

2018-05-20 18:30:51

Quantitative value

0.0093

Clarke's Analysis of Drugs and Poisons, View in Reaxys 135 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Time to peak plasma concentration of metabolite alpha-hydroxyetizolam upon multiple oral administration in healthy males for 12 h for 1 week

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Qualitative Results

2.5

Measurement Parameter

tmax

Unit

hour

Quantitative value

2.5

Clarke's Analysis of Drugs and Poisons, View in Reaxys 136 of 195

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of the compound against platelet activating factor induced aggregation in human thrombocytes

Biological Species/NCBI ID

human

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Measurement Parameter

IC50

Unit

µM

Measurement Object

Platelet activating factor induced aggregation in human thrombocytes

Qualitative value

Quantitative value

Measurement pX

5.3

Patent; Casals-Stenzel, Jorge, Dr.; Weber, Karl-Heinz, Dr.; Walther, Gerhard, Dr.; Harreus, Albrecht, Dr.; Muacevic, Gojki, Dr.; EP176927; (A2); (1986), View in Reaxys 137 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in mouse upon p.o. administration

Biological Species/NCBI ID

Mus musculus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Qualitative Results

3070

Measurement Parameter

LD50

Unit

mg/kg

Measurement Object

Lethal dose

Quantitative value

3070

Patent; Boehringer Ingelheim GmbH; US4094984; (1978); (A) English, View in Reaxys 138 of 195

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

58/80

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Bioassay Details

Inhibitory concentration of the compound against Platelet aggregating factor receptor using 1 nM [3H]PAF in platelets of rabbit

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Measurement Parameter

IC50

Unit

Qualitative value

Quantitative value

29.5

Deviation

6.2

Measurement pX

7.53

Concomitants: Compound name

[3H]PAF

Concomitants: Compound role

RAD

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasawa; T Tahara; European journal of medicinal chemistry; vol. 31; (1996); p. 683 - 692, View in Reaxys 139 of 195

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of compound required to inhibit rabbit platelet aggregation induced by platelet activating factor (PAF) incubated at 37 degree C

Biological Species/NCBI ID

Leporidae

Cells/Cell Lines

thrombocyte

Substance RN

572740View in Reaxys

Measurement Parameter

IC50

Unit

Measurement Object

Inhibit rabbit platelet aggregation induced by platelet activating factor (PAF)

Qualitative value

Quantitative value

6730

Measurement pX

5.17

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasawa; T Tahara; European journal of medicinal chemistry; vol. 31; (1996); p. 683 - 692, View in Reaxys 140 of 195

Target Name

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Synonyms

bzrap1; peripheral-type benzodiazepine receptor-associated protein 1; prax-1; rbp1; rim-bp1; rimsbinding protein 1; tspo-associated protein 1; tspoap1

Target Uniprot ID

q9jir0

Target, Subunit, Species

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]

Target Mutant/Chimera Details

Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild

Target Species (Bioactivity)

Rattus norvegicus

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

59/80

2018-05-20 18:30:51

Bioassay Details

Inhibitory concentration of the compound against Benzodiazepine receptor using 2 nM 3H-DZP at pH 7.4 in synaptosomal memebrane of rat brain

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Measurement Parameter

Ki (inhibition constant)

Unit

Qualitative value

Quantitative value

2.34

Deviation

0.07

Measurement pX

8.63

Concomitants: Compound name

[3H]DZP

Concomitants: Compound role

RAD

Y Kawakami; H Kitani; S Yuasa; M Abe; M Moriwaki; M Kagoshima; M Terasawa; T Tahara; European journal of medicinal chemistry; vol. 31; (1996); p. 683 - 692, View in Reaxys 141 of 195

142 of 195

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

In vitro fraction of clearance of compound in human hepatic cells mediated by CYTOCHROME P450 3A4 was determined

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Measurement Parameter

Activity

Measurement Object

Quantitative value

0.35

Target Name

Cytochrome P450 3A4 [human]

Target Synonyms

Target Uniprot ID

p08684

Target PDB ID

1tqn; 1w0e; 1w0f; 1w0g; 2j0d; 2v0m; 3nxu; 3tjs; 3ua1; 4d6z; 4d75; 4d78; 4d7d; 4i3q; 4i4g; 4i4h; 4k9t; 4k9u; 4k9v; 4k9w; 4k9x; 4ny4; 5a1p; 5a1r; 5te8

Target, Subunit, Species

Cytochrome P450 3A4 [human]

Target Mutant/Chimera Details

Cytochrome P450 3A4 [human]:Wild

60/80

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143 of 195

Target Species (Bioactivity)

human

Bioassay Category

Metabolism/Transport

Bioassay Details

In vitro fraction of clearance of compound in human hepatic cells mediated by CYTOCHROME P450 3A4 was determined

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Measurement Parameter

Activity

Measurement Object

Quantitative value

0.36

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal dose of the compound in rat upon subcutaneous administration

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

> 5000

Measurement Parameter

LD50

Unit

mg/kg

Quantitative value

5000

Tsumagari; Nakajima; Fukuda; Shuto; Kenjo; Morimoto; Takigawa; Arzneimittel-Forschung/Drug Research; vol. 28; nb. 7; (1978); p. 1158 - 1164, View in Reaxys 144 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal doe in rat;Oral

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

oral administration

Measurement Parameter

LD50

Unit

mg/kg

Qualitative value

Quantitative value

3509

Tsumagari; Nakajima; Fukuda; Shuto; Kenjo; Morimoto; Takigawa; Arzneimittel-Forschung/Drug Research; vol. 28; nb. 7; (1978); p. 1158 - 1164, View in Reaxys 145 of 195

Bioassay Category

Toxicity/Safety Pharmacology

Bioassay Details

Lethal doe in rat;Subcutaneous

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Substance Route of Adm.

subcutaneous administration

Measurement Parameter

LD50

Unit

g/kg

Qualitative value

Quantitative value

Tsumagari; Nakajima; Fukuda; Shuto; Kenjo; Morimoto; Takigawa; Arzneimittel-Forschung/Drug Research; vol. 28; nb. 7; (1978); p. 1158 - 1164, View in Reaxys

61/80

2018-05-20 18:30:51

146 of 195

Bioassay Category

Metabolism/Transport

Bioassay Details

Half life of compound in rat

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Measurement Parameter

t1/2 el

Unit

hour

Qualitative value

Quantitative value

6.9

Hirase, Masahiro; Ishida, Takayuki; Kamei, Chiaki; European Journal of Pharmacology; vol. 597; nb. 1-3; (2008); p. 46 - 50, View in Reaxys 147 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Half life of the compound in human

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Substance Route of Adm.

intravenous administration

Measurement Parameter

t1/2 el

Unit

hour

Qualitative value

Quantitative value

6.2

Mandrioli, Roberto; Mercolini, Laura; Raggi, Maria Augusta; Current drug metabolism; vol. 9; nb. 8; (2008); p. 827 - 844, View in Reaxys 148 of 195

Bioassay Category

Pharmacokinetic

Bioassay Details

Time taken to reach maximum blood concentration of the compound in human

Biological Species/NCBI ID

human

Substance RN

572740View in Reaxys

Measurement Parameter

tmax

Unit

hour

Measurement Object

Time taken to reach maximum blood concentration

Qualitative value

Quantitative value

3.2

Mandrioli, Roberto; Mercolini, Laura; Raggi, Maria Augusta; Current drug metabolism; vol. 9; nb. 8; (2008); p. 827 - 844, View in Reaxys 149 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for the anticonvulsant activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and effective

Measurement Parameter

Activity

Measurement Object

Anticonvulsant activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 150 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for its muscle relaxant activity; Potent and Effective

62/80

2018-05-20 18:30:51

Substance RN

572740View in Reaxys

Qualitative Results

Potent and Effective

Measurement Parameter

Activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 151 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was evaluated for anxiolytic activity

Substance RN

572740View in Reaxys

Qualitative Results

Active

Measurement Parameter

Activity

Qualitative value

Richard C. Allen; Annual reports in medicinal chemistry; vol. 20; (1985); p. 315 - 352, View in Reaxys 152 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for selectivity preventing and reversing PAF-induced hypotension in rats; Active

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

Acitve

Measurement Parameter

Activity

Qualitative value

Kelvin Cooper; M. John Parry; Annual reports in medicinal chemistry; vol. 24; (1989); p. 81 - 90, View in Reaxys 153 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for selectivity preventing and reversing PAF-induced hypotension in rats; Active

Biological Species/NCBI ID

Rattus norvegicus

Substance RN

572740View in Reaxys

Qualitative Results

Active

Measurement Parameter

Activity

Qualitative value

Kelvin Cooper; M. John Parry; Annual reports in medicinal chemistry; vol. 24; (1989); p. 81 - 90, View in Reaxys 154 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for its anxiolytic activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and Effective

Measurement Parameter

Activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 155 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for its anticonvulsant activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and Effective

Measurement Parameter

Activity

Qualitative value

63/80

2018-05-20 18:30:51

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 156 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for the muscle relaxant activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and effective

Measurement Parameter

Activity

Measurement Object

Muscle relaxant activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 157 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for the sedative activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and effective

Measurement Parameter

Activity

Measurement Object

sedative activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 158 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Tested for its sedative activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and Effective

Measurement Parameter

Activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 159 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Compound was tested for the anxiolytic activity; Potent and Effective

Substance RN

572740View in Reaxys

Qualitative Results

Potent and effective

Measurement Parameter

Activity

Qualitative value

Joel G. Berger; Louis C. Iorio; Annual reports in medicinal chemistry; vol. 14; nb. 19; (1979); p. 22 - 30, View in Reaxys 160 of 195

Target Name

Bromodomain-containing protein 3

Target Synonyms

brd3; bromodomain-containing fsh-like protein fsrg2; bromodomain-containing protein 3; fsrg2; kiaa0043; ring3-like protein; ring3l

Target, Subunit, Species

Bromodomain-containing protein 3

Target Mutant/Chimera Details

Bromodomain-containing protein 3:Wild

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of the compound against His6-tagged Bromodomain containing 3 upon incubation in 50 mM HEPES, pH 7.4 at RT for 60 min using fluorescence anisotropy assay

Substance RN

572740View in Reaxys

Measurement Parameter

pIC50

64/80

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161 of 195

162 of 195

163 of 195

Qualitative value

Quantitative value

4.8

Measurement pX

4.8

Target Name

Bromodomain-containing protein 4

Target Synonyms

brd4; bromodomain-containing protein 4; hunk1; mcap; mitotic chromosome-associated protein; protein hunk1

Target, Subunit, Species

Bromodomain-containing protein 4

Target Mutant/Chimera Details

Bromodomain-containing protein 4:Wild

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of the compound against His6-tagged Bromodomain-containing protein 4 upon incubation in 50 mM HEPES, pH 7.4 at RT for 60 min using fluorescence anisotropy assay

Substance RN

572740View in Reaxys

Measurement Parameter

pIC50

Qualitative value

Quantitative value

4.1

Measurement pX

4.1

Target Name

Bromodomain-containing protein 2

Target Synonyms

brd2; bromodomain-containing protein 2; female sterile homeotic-related protein 1; fsrg-1; fsrg1; kiaa4005; kiaa9001; o27.1.1; protein ring3; really interesting new gene 3 protein; ring3

Target, Subunit, Species

Bromodomain-containing protein 2

Target Mutant/Chimera Details

Bromodomain-containing protein 2:Wild

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Bioassay Details

Inhibitory concentration of the compound against His6-tagged Bromodomain containing 2 upon incubation in 50 mM HEPES, pH 7.4 at RT for 60 min using fluorescence anisotropy assay

Substance RN

572740View in Reaxys

Measurement Parameter

pIC50

Qualitative value

Quantitative value

4.6

Measurement pX

4.6

Target Name

Carboxylesterase 1 [human]

Target Synonyms

carboxylesterase 1

Target, Subunit, Species

Carboxylesterase 1 [human]

Target Mutant/Chimera Details

Carboxylesterase 1 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology inhibition

Cells/Cell Lines

Sf21 cell line

65/80

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164 of 195

165 of 195

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

1281877

Concomitants: Compound name

4-Nitrophenyl acetate

Concomitants: Compound role

SUB

Target Name

Carboxylesterase 2 [human]

Target Synonyms

carboxylesterase 2

Target, Subunit, Species

Carboxylesterase 2 [human]

Target Mutant/Chimera Details

Carboxylesterase 2 [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

Bioassay Category

Metabolism/Transport

Bioassay Name

Enzymology inhibition

Cells/Cell Lines

Sf21 cell line

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

3.61

Concomitants: Compound RN

1281877

Concomitants: Compound name

4-Nitrophenyl acetate

Concomitants: Compound role

SUB

Target Name

Arylacetamide deacetylase [human]

Target Synonyms

aadac; arylacetamide deacetylase; dac

Target Uniprot ID

p22760

Target, Subunit, Species

Arylacetamide deacetylase [human]

Target Mutant/Chimera Details

Arylacetamide deacetylase [human]:Wild

Target Species (Bioactivity)

human

Target Transfection

Transfected

66/80

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166 of 195

Bioassay Category

In Vitro (Efficacy)

Bioassay Name

Enzymology inhibition

Cells/Cell Lines

Sf21 cell line

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

100 µM

Measurement Parameter

% Inhibition

Qualitative value

Measurement pX

Concomitants: Compound RN

1281877

Concomitants: Compound name

4-Nitrophenyl acetate

Concomitants: Compound role

SUB

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

4890356; 78881

Concomitants: Compound role

SUB; COM

Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki; Drug Metabolism and Disposition; vol. 43; nb. 6; (2015); p. 812 - 818, View in Reaxys 167 of 195

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

67/80

2018-05-20 18:30:51

Bioassay Category

In Vitro (Efficacy)

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

4.24

Concomitants: Compound RN

4890356; 78881

Concomitants: Compound role

SUB; COM

Target Name

UDP-glucuronosyltransferase 1-8

Target Synonyms

a3; gnt1; udp-glucuronosyltransferase 1-8; udp-glucuronosyltransferase 1-h; udp-glucuronosyltransferase 1a8; udpgt 1-8; ugt-1h; ugt1; ugt1*8; ugt1-08; ugt1.8; ugt1a8; ugt1h

Target, Subunit, Species

UDP-glucuronosyltransferase 1-8

Target Mutant/Chimera Details

UDP-glucuronosyltransferase 1-8:Wild

Target Transfection

Transfected

Substance Action on Target

Inhibitor

Bioassay Category

In Vitro (Efficacy)

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

20 μM

Measurement Parameter

% Inhibition

Unit

Quantitative value

Measurement pX

Concomitants: Compound RN

4890356; 78881

Concomitants: Compound role

SUB; COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Fg (intestinal availability)

68/80

2018-05-20 18:30:51

Unit

Quantitative value

0.88

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Yamamoto, Takehito; Furihata, Kenichi; Hisaka, Akihiro; Moritoyo, Takashi; Ogoe, Kazuaki; Kusayama, Shizuko; Motohashi, Keiju; Mori, Akiko; Iwatsubo, Takeshi; Suzuki, Hiroshi; Journal of Clinical Pharmacology; vol. 57; nb. 11; (2017); p. 1491 - 1499, View in Reaxys 170 of 195

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Fg (intestinal availability)

Unit

Quantitative value

0.81

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Metabolism/Transport

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Organs/Tissues

liver

Cell Fraction

Microsome

Substance RN

572740View in Reaxys

Substance Name

etizolam

Measurement Parameter

fm(E) vitro

Unit

μM

Quantitative value

0.6

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

69/80

2018-05-20 18:30:51

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Cmax

Unit

ng/ml

Quantitative value

5.41

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Cmax

Unit

ng/ml

Quantitative value

6.69

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

tmax

Unit

70/80

2018-05-20 18:30:51

Quantitative value

1.3

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

tmax

Unit

Quantitative value

1.4

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

t1/2

Unit

Quantitative value

25.6

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

71/80

2018-05-20 18:30:51

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

AUC (0-24 h)

Unit

ng*h/ml

Quantitative value

102

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

AUC (0-inf)

Unit

ng*h/ml

Quantitative value

212

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

72/80

2018-05-20 18:30:51

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Cl/F

Unit

ml/min

Quantitative value

19.7

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Vd/F

Unit

Quantitative value

42.1

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

73/80

2018-05-20 18:30:51

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

t1/2

Unit

Quantitative value

7.6

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

AUC (0-24 h)

Unit

ng*h/ml

Quantitative value

50.4

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

AUC (0-inf)

74/80

2018-05-20 18:30:51

Unit

ng*h/ml

Quantitative value

56.8

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Cl/F

Unit

ml/min

Quantitative value

73.4

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Bioassay Category

Pharmacokinetic

Biological Species/NCBI ID

Japanese (people)

Population State

Healthy

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

0.25 mg

Substance Route of Adm.

oral administration

Measurement Parameter

Vd/F

Unit

Quantitative value

47.4

Statistical sgnificance (Qualitative)

75/80

2018-05-20 18:30:51

Concomitants: Compound RN

6042047

Concomitants: Compound name

itraconazole

Concomitants: Compound role

COM

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

<= 20 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% change

Measurement Object

cutaneous temperature

Qualitative value

Not active

Measurement pX

Miyazono, Sadaharu; Hasegawa, Kaede; Miyazaki, Seri; Sakakima, Hikari; Konno, Shun; Meguro, Saori; Sasajima, Hitoshi; Noguchi, Tomohiro; Osada, Kazumi; Kashiwayanagi, Makoto; European Journal of Pharmacology; vol. 824; (2018); p. 157 - 162, View in Reaxys 187 of 195

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Unit

Measurement Object

cutaneous temperature

Qualitative value

Quantitative value

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

76/80

2018-05-20 18:30:51

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

1.7 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

cutaneous temperature

Qualitative value

Not active

Measurement pX

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% change

Measurement Object

Fos immunoreactive signal

Qualitative value

Not active

Measurement pX

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

Qualitative value

Active

Statistical sgnificance (Qualitative)

77/80

2018-05-20 18:30:51

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

Qualitative value

Active

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

Qualitative value

Active

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

78/80

2018-05-20 18:30:51

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

Qualitative value

Active

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

Qualitative value

Active

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

Substance Effect

Anxiolytic

Bioassay Category

In Vivo (Animal models)

Biological Species/NCBI ID

Bagg albino mouse

Substance RN

572740View in Reaxys

Substance Name

etizolam

Substance Dose

5 mg/kg

Substance Route of Adm.

intragastric administration

Measurement Parameter

% decrease

Measurement Object

Fos immunoreactive signal

79/80

2018-05-20 18:30:51

Qualitative value

Active

Statistical sgnificance (Qualitative)

Concomitants: Compound RN

32387355

Concomitants: Compound role

IND

80/80

2018-05-20 18:30:51