Reaxys
PubChem
eMolecules
LabNetwork
Bioactivities (982)
SigmaAldrich
Reactions (10)
Substances (12)
Targets (169)
Structure
Citations (621)
N° of preparations All Preps | All Reactions
Structure/Compound Data Reaxys Registry Number: 26138911
CAS Registry Number: 74143-28-5 Molecular Formula: C16H12FN3O3
Linear Structure Formula: C15(11)CH12FN3O3
no reactions.
Available Data
Target
N° of ref.
Druglikeness
Bioactivity
Identification
Show Targets
1
Molecular Weight: 312.277
InChI Key: PPTYJKAXVCCBDU-BJUDXGSMSA-N
1
Synthesize | Hide Details Find similar
Druglikeness Bioactivity In vitro: Efficacy (1) Quantitative Results pX
Parameter
Value (qual)
Value (quant)
Unit
9
Kd
=
1
nM
Katsifis, Andrew; Kassiou, Michael
Action on Target Radioligand (/ligand)
Target Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all) Mini-Reviews in Medicina...
Title/Abstract Full Text View citing articles Show Details
Mini-Reviews in Medicinal Chemistry, 2004 , vol. 4, # 8 p. 909 - 921 Title/Abstract Full Text View citing articles Show Details
Identification Chemical Name: flunitrazepam
2 prep out of 10 reactions.
Reaxys Registry Number: 702691
CAS Registry Number: 1622-62-4 Type of Substance: heterocyclic Molecular Formula: C16H12FN3O3
Linear Structure Formula: C16H12FN3O3
Molecular Weight: 313.288
InChI Key: PPTYJKAXVCCBDU-UHFFFAOYSA-N
2
Druglikeness
Bioactivity
Identification Physical Data (20) Spectra (30) Other Data (25)
Highest Clinical Phase: Marketed
Synthesize | Hide Details Find similar Chemical Names and Synonyms flunitrazepam, 1-methyl-5-(2'-fluoro-phenyl)-7-nitro-1,3-dihydro-2H-1,4-benzodiazepin-2-one, Flunitrazepam, 5-(2-fluorophenyl)-1,3-dihydro-1methyl-7-nitro-2H-1,4-benzodiazepin-2-one, (+/-)-flunitrazepam, [3H]-flunitrazepam, 3H-flunitrazepam Druglikeness Bioactivity In vitro: Efficacy (528) Quantitative Results pX
Parameter
8.24
Kd
Value (qual)
Value (quant)
Unit
5.8
nM
Action on Target
Target
Radioligand (/ligand)
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all)
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
Bmax
103
pmol/g tissue
Radioligand (/ligand)
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
8.64
Kd
2.3
nM
Radioligand (/ligand)
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
Bmax
104
pmol/g tissue
Radioligand (/ligand)
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
5.3
IC50
5
µM
Show Targets
616
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
5.6
IC50
2.5
µM
forebrain
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Wood; Loo; Braunwalder; Yokoyama; Cheney
Journal of Pharmacology and Experimental Therapeutics, 1984 , vol. 231, # 3 p. 572 - 576 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gammaaminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
pX
Parameter
Value (qual)
Value (quant)
Unit
Action on Target
Target
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all)
Emax(%)
100
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
oocyte
Electrophysiology
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Carling, Robert W.; Madin, Andrew; Guiblin, Alec; Russell, Michael G. N.; Moore, Kevin W.; Mitchinson, Andrew; Sohal, Bindi; Pike, Andrew; Cook, Susan M.; Ragan, Ian C.; McKernan, Ruth M.; Quirk, Kathleen; Ferris, Pushpinder; Marshall, George; Thompson, Sally Ann; Wafford, Keith A.; Dawson, Gerard R.; Atack, John R.; Harrison, Timothy; Castro, Jose L.; Street, Leslie J.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7089 - 7092 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
-0.5
%
Thyrotropin-releasing hormone receptor [human]:Wild
CHO-DXB11 cell line
Binding
10 µM
Patent: US5879896 , 19...
Title/Abstract Full Text Show Details
Thyrotropin-releasing hormone receptor [human]:Wild
CHO-DXB11 cell line
Binding
1 mM
Patent: US5879896 , 19...
Title/Abstract Full Text Show Details
Thyrotropin-releasing hormone receptor [human]:Wild
CHO-DXB11 cell line
Binding
100 µM
Patent: US5879896 , 19...
Title/Abstract Full Text Show Details
GABA-A receptor [taurine cattle]:Wild
brain cortex
Binding
0 µM
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Hinuma; Shuji; Hosoya; Masaki; Onda; Haruo
Patent: US5879896 , 1999 ; Title/Abstract Full Text Show Details
1
% Inhibition
-13.7
%
Hinuma; Shuji; Hosoya; Masaki; Onda; Haruo
Patent: US5879896 , 1999 ; Title/Abstract Full Text Show Details
1
% Inhibition
-4
%
Hinuma; Shuji; Hosoya; Masaki; Onda; Haruo
Patent: US5879896 , 1999 ; Title/Abstract Full Text Show Details
8.29
Ki
5.17
nM
Castellano, Sabrina; Taliani, Sabrina; Milite, Ciro; Pugliesi, Isabella; Da Pozzo, Eleonora; Rizzetto, Elisa; Bendinelli, Sara; Costa, Barbara; Cosconati, Sandro; Greco, Giovanni; Novellino, Ettore; Sbardella, Gianluca; Stefancich, Giorgio; Martini, Claudia; Da Settimo, Federico
Journal of Medicinal Chemistry, 2012 , vol. 55, # 9 p. 4506 - 4510 Title/Abstract Full Text View citing articles Show Details
9.55
Ki
0.28 65.6
nM
In Vitro (others)
1.00000E11 M
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Maguire; Mechanick; Davies; Ellis; Meredith; Loew
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 2 p. 842 - 849 Title/Abstract Full Text View citing articles Show Details
6.02
IC50
0.95
µM
In Vitro (others)
50 mM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
In Vitro (others)
0.0500000 mM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
In Vitro (others)
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
In Vitro (others)
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
6.62
IC50
0.238
µM
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
4.86
EC50
13.7
µM
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
4.69
EC50
20.6
µM
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
4.74
EC50
18.2
µM
In Vitro (others)
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
In Vitro (others)
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text Show Details
neocortex
Binding
Molecular Brain Research...
Title/Abstract Full Text Show Details
neocortex
Binding
Molecular Brain Research...
Title/Abstract Full Text Show Details
brain cortex
Binding
Psychopharmacology, 1987...
Title/Abstract Full Text Show Details
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
4.69
EC50
20.2
µM
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
Bmax
4239
fmol/mg protein
Radioligand (/ligand)
Shaw; Scarth
Molecular Brain Research, 1991 , vol. 11, # 3-4 p. 273 - 282 Title/Abstract Full Text Show Details
7.66
Kd
22
nM
Radioligand (/ligand)
Shaw; Scarth
Molecular Brain Research, 1991 , vol. 11, # 3-4 p. 273 - 282 Title/Abstract Full Text Show Details
8.78
Ki
1.66
nM
Arendt; Greenblatt; Liebisch; Luu; Paul
Psychopharmacology, 1987 , vol. 93, # 1 p. 72 - 76 Title/Abstract Full Text Show Details
7.5
Ki
9.8
µg/L
Visser; Wolters; Gubbens-Stibbe; Tukker; Van Der Graaf; Peletier; Danhof, Meindert
Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 88 - 101 Title/Abstract Full Text View citing articles Show Details
fu
26.6
In Vitro (others)
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Visser; Wolters; Gubbens-Stibbe; Tukker; Van Der Graaf; Peletier; Danhof, Meindert
Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 88 - 101 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
0
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Epsilon) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
1 µM
Toxicology Letters, 1998...
Title/Abstract Full Text View citing articles Show Details
Thompson, Sally-Anne; Bonnert, Timothy P.; Whiting, Paul J.; Wafford, Keith A.
Toxicology Letters, 1998 , vol. 100-101, p. 233 - 238 Title/Abstract Full Text View citing articles Show Details
7.94
% Stimulation
121
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit
oocyte
Electrophysiology
# 220 nM
Toxicology Letters, 1998...
Title/Abstract Full Text View citing articles Show Details
alpha-1 [human]:Wild Thompson, Sally-Anne; Bonnert, Timothy P.; Whiting, Paul J.; Wafford, Keith A.
Toxicology Letters, 1998 , vol. 100-101, p. 233 - 238 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.2
nM
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
Toxicology Letters, 1998...
Title/Abstract Full Text View citing articles Show Details
Thompson, Sally-Anne; Bonnert, Timothy P.; Whiting, Paul J.; Wafford, Keith A.
Toxicology Letters, 1998 , vol. 100-101, p. 233 - 238 Title/Abstract Full Text View citing articles Show Details
8.41
IC50
3.9
nM
GABA-A receptor [Rattus norvegicus]:Wild
cerebellum
nerve cell
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
8.62
IC50
2.4
nM
GABA-A receptor [Rattus norvegicus]:Wild
cerebellum
nerve cell
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
8.1
Ki
7.96
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
7.65
Ki
22.44
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
L-M(TK-) cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
8.48
Ki
3.34
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
8.02
Ki
9.57
nM
Gamma-aminobutyric acid receptor subunit
L-M(TK-) cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
8.15
Ki
7.02
nM
Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
7.92
Ki
12.08
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
L-M(TK-) cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Wafford; Bain; Kemp; Palmer; Wilson; Wilcox; Sikela; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 44, # 6 p. 1211 - 1218 Title/Abstract Full Text View citing articles Show Details
7.54
EC50
29
nM
Allosteric Modulator
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
7.62
EC50
24
nM
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
alpha-3 [taurine cattle]:Wild Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [taurine cattle]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 43, # 2 p. 240 - 244 Title/Abstract Full Text View citing articles Show Details
8.48
EC50
3.3
nM
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
123
%
Allosteric Modulator
oocyte
Electrophysiology
1 µM
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
7.58
EC50
26.5
nM
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
81
%
Allosteric Modulator
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 2L) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild +
oocyte
Electrophysiology
1 µM
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
cells
Binding
Patent: WO2003/16265 A...
Title/Abstract Full Text Show Details
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
cells
Binding
Patent: WO2003/16265 A...
Title/Abstract Full Text Show Details
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
Binding
Patent: US2002/198221 ...
Title/Abstract Full Text Show Details
cells
Binding
Patent: EP810879 B1, 2...
Title/Abstract Full Text Show Details
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
Emax(%)
100
%
Allosteric Modulator
oocyte
Electrophysiology
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wafford; Bain; Whiting; Kemp
Molecular Pharmacology, 1993 , vol. 44, # 2 p. 437 - 442 Title/Abstract Full Text View citing articles Show Details
9.1
IC50
#
0.79
nM
EISAI CO., LTD.
Patent: WO2003/16265 A1, 2003 ; Title/Abstract Full Text Show Details
8.82
IC50
#
1.51
nM
EISAI CO., LTD.
Patent: WO2003/16265 A1, 2003 ; Title/Abstract Full Text Show Details
6.94
IC50
114
nM
Dusza, John P.; Tomcufcik, Andrew S.; Albright, Jay D.; Beer, Bernard
Patent: US2002/198221 A1, 2002 ; Title/Abstract Full Text Show Details
8.28
Ki
5.2
nM
Gamma-aminobutyric acid receptor subunit beta-3 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [mammal]:Wild
DAWSON, Gerard, Raphael
Patent: EP810879 B1, 2003 ; Title/Abstract Full Text Show Details
8.6
Ki
2.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [mammal]:Wild
cells
Binding
Patent: EP810879 B1, 2...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit beta-3 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [mammal]:Wild
cells
Binding
Patent: EP810879 B1, 2...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit beta-3 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [mammal]:Wild
cells
Binding
Patent: EP810879 B1, 2...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit beta-3 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [mammal]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [mammal]:Wild
cells
Binding
Patent: EP810879 B1, 2...
Title/Abstract Full Text Show Details
Nuclear receptor subfamily 1 group I member 3 [human]:Wild
JHH-7 cell line
Transactivation assay
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
DAWSON, Gerard, Raphael
Patent: EP810879 B1, 2003 ; Title/Abstract Full Text Show Details
8.32
Ki
4.8
nM
DAWSON, Gerard, Raphael
Patent: EP810879 B1, 2003 ; Title/Abstract Full Text Show Details
8.68
Ki
2.11
nM
DAWSON, Gerard, Raphael
Patent: EP810879 B1, 2003 ; Title/Abstract Full Text Show Details
1
Ki
>
10000
nM
DAWSON, Gerard, Raphael
Patent: EP810879 B1, 2003 ; Title/Abstract Full Text Show Details
Foldincrease
<
1.5
Kobayashi, Kaoru; Yamanaka, Yosuke; Iwazaki, Norihiko; Nakajo, Ikumi; Hosokawa, Masakiyo; Negishi, Masahiko; Chiba, Kan
Drug Metabolism and Disposition, 2005 , vol. 33, # 7 p. 924 - 929 Title/Abstract Full Text View citing articles Show Details
4.24
% Inhibition
51
%
liver
Enzymology inhibition
60 µM
Type: Clinical Pharmacol...
Title/Abstract Full Text Show Details
In Vitro (others)
Biological and Pharmaceu...
Title/Abstract Full Text View citing articles Show Details
Type: Clinical Pharmacology Biopharmaceutics Review, Lab: NDA202258, Owner: SCHERING, Number: 000 2011 Title/Abstract Full Text Show Details
4.49
IC50
32
µM
enzyme:Wild
Usami, Noriyuki; Yamamoto, Tomohiro; Shintani, Syunichi; Higaki, Yu; Ishikura, Shuhei; Katagiri, Yoshihiro; Hara, Akira
Biological and Pharmaceutical Bulletin, 2002 , vol. 25, # 4 p. 441 - 445 Title/Abstract Full Text View citing articles Show Details
4.19
IC50
64
µM
cAMP-specific 3',5'cAMP phosphodiesterase 4:Wild
In Vitro (others)
200 µM
British Journal of Pharm...
Title/Abstract Full Text View citing articles Show Details
Collado, M. Carmen; Beleta, Jorge; Martinez, Ester; Miralpeix, Montse; Domenech, Teresa; Palacios, Jose Maria; Hernandez, Jesus
British Journal of Pharmacology, 1998 , vol. 123, # 6 p. 1047 - 1054 Title/Abstract Full Text View citing articles Show Details
4.18
IC50
66
µM
cGMP-specific 3',5'cyclic phosphodiesterase:Wild
thrombocyte
In Vitro (others)
200 µM
British Journal of Pharm...
Title/Abstract Full Text View citing articles Show Details
Collado, M. Carmen; Beleta, Jorge; Martinez, Ester; Miralpeix, Montse; Domenech, Teresa; Palacios, Jose Maria; Hernandez, Jesus
British Journal of Pharmacology, 1998 , vol. 123, # 6 p. 1047 - 1054 Title/Abstract Full Text View citing articles Show Details
Bmax
4
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Histamine H1 receptor [Rattus norvegicus]:Wild
brain
Binding
Proceedings of the Natio...
Title/Abstract Full Text Show Details
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469 Title/Abstract Full Text Show Details
Bmax
4
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469 Title/Abstract Full Text Show Details
Bmax
0.08
pmol/mg
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469 Title/Abstract Full Text Show Details
Bmax
0.103
pmol/mg
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469 Title/Abstract Full Text Show Details
4.77
Ki
17000
nM
Tran; Chang; Snyder
Proceedings of the National Academy of Sciences of the United States of America, 1978 , vol. 75, # 12 p. 6290 - 6294 Title/Abstract Full Text Show Details
8.3
IC50
5
nM
forebrain
Binding
Nature, 1977 , vol. 266...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
retina
Binding
Brain Research, 1980 , ...
Title/Abstract Full Text Show Details
Squires; Braestrup
Nature, 1977 , vol. 266, # 5604 p. 732 - 734 Title/Abstract Full Text Show Details
Bmax
0.085
pmol/mg
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469 Title/Abstract Full Text Show Details
Bmax
0.015
pmol/mg
Borbe; Mueller; Wollert
Brain Research, 1980 , vol. 182, # 2 p. 466 - 469
Title/Abstract Full Text Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
LTK-
Binding
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Collins, Ian; Davey, William B.; Rowley, Michael; Quirk, Kathleen; Bromidge, Frances A.; McKernan, Ruth M.; Thompson, Sally-Anne; Wafford, Keith A.
Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 12 p. 1381 - 1384 Title/Abstract Full Text View citing articles Show Details
8.96
Ki
1.1
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
LTK-
Binding
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Collins, Ian; Davey, William B.; Rowley, Michael; Quirk, Kathleen; Bromidge, Frances A.; McKernan, Ruth M.; Thompson, Sally-Anne; Wafford, Keith A.
Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 12 p. 1381 - 1384 Title/Abstract Full Text View citing articles Show Details
8.23
Ki
5.9
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
LTK-
Binding
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Collins, Ian; Davey, William B.; Rowley, Michael; Quirk, Kathleen; Bromidge, Frances A.; McKernan, Ruth M.; Thompson, Sally-Anne; Wafford, Keith A.
Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 12 p. 1381 - 1384 Title/Abstract Full Text View citing articles Show Details
7.28
% Stimulation
121
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
oocyte
Electrophysiology
1 µM
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Collins, Ian; Davey, William B.; Rowley, Michael; Quirk, Kathleen; Bromidge, Frances A.; McKernan, Ruth M.; Thompson, Sally-Anne; Wafford, Keith A.
Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 12 p. 1381 - 1384 Title/Abstract Full Text View citing articles Show Details
8.55
IC50
2.8
nM
In Vitro (others)
0.100000 µM
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Katsura, Masashi; Ohkuma, Seitaro; Jun, Xu; Kuriyama, Kinya
European Journal of Pharmacology, 1996 , vol. 298, # 1 p. 71 - 77 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.2
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
LTK-
Binding
1.00000E09 M
Cox, Eric D.; Diaz-Arauzo, Hernando; Huang, Qi; Reddy, Mundla S.; Ma, Chunrong; Harris, Brad; McKernan, Ruth; Skolnick, Phil; Cook, James M.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2537 - 2552 Title/Abstract Full Text View citing articles Show Details
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
8.6
Ki
2.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cox, Eric D.; Diaz-Arauzo, Hernando; Huang, Qi; Reddy, Mundla S.; Ma, Chunrong; Harris, Brad; McKernan, Ruth; Skolnick, Phil; Cook, James M.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2537 - 2552 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
4.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cox, Eric D.; Diaz-Arauzo, Hernando; Huang, Qi; Reddy, Mundla S.; Ma, Chunrong; Harris, Brad; McKernan, Ruth; Skolnick, Phil; Cook, James M.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2537 - 2552 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.1
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cox, Eric D.; Diaz-Arauzo, Hernando; Huang, Qi; Reddy, Mundla S.; Ma, Chunrong; Harris, Brad; McKernan, Ruth; Skolnick, Phil; Cook, James M.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2537 - 2552 Title/Abstract Full Text View citing articles Show Details
5.7
Ki
>
2000
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cox, Eric D.; Diaz-Arauzo, Hernando; Huang, Qi; Reddy, Mundla S.; Ma, Chunrong; Harris, Brad; McKernan, Ruth; Skolnick, Phil; Cook, James M.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2537 - 2552 Title/Abstract Full Text View citing articles Show Details
8.48
Kd
3.28
nM
granule cell
In Vitro (others)
0.300000 nM
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Vale, Carmen; Pomes, Anna; Rodriguez-Farre, Eduard; Sunol, Cristina
European Journal of Pharmacology, 1997 , vol. 319, # 2-3 p. 343 - 353 Title/Abstract Full Text View citing articles Show Details
3.89
IC50
129
µM
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Kimura, Toshiyuki; Kuze, Jiro; Watanabe, Kazuhito; Kondo, Shigemi; Ho, Ing Kang; Yamamoto, Ikuo
European Journal of Pharmacology, 1996 , vol. 311, # 2-3 p. 265 - 269 Title/Abstract Full Text View citing articles Show Details
6.56
Kd
272.7
nM
In Vitro (others)
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Hegener, Oliver; Jordan, Randolf; Haeberlein, Hanns
Journal of Medicinal Chemistry, 2004 , vol. 47, # 14 p. 3600 - 3605 Title/Abstract Full Text View citing articles Show Details
8.23
EC50
5.9
nM
In Vitro (others)
1.00000E10 M
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Derry, Jason M. C.; Martin, Ian L.; Dunn, Susan M. J.
Molecular Pharmacology, 2000 , vol. 58, # 4 p. 756 - 762 Title/Abstract Full Text View citing articles Show Details
7.83
EC50
14.8
nM
In Vitro (others)
1.00000E10 M
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Derry, Jason M. C.; Martin, Ian L.; Dunn, Susan M. J.
Molecular Pharmacology, 2000 , vol. 58, # 4 p. 756 - 762 Title/Abstract Full Text View citing articles Show Details
8.68
Kd
2.1
nM
In Vitro (others)
Journal of applied toxic...
Title/Abstract Full Text View citing articles Show Details
Gordon; Nigam; Weitz; Dave; Doctor; Ved
Journal of applied toxicology : JAT, 2001 , vol. 21 Suppl 1, p. S47-51 Title/Abstract Full Text View citing articles Show Details
1
IC50
>
100
µM
Cholecystokinin receptor [Rattus norvegicus]:Wild
pancreas
Binding
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
brain
Binding
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
brain cortex
Binding
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
GABA-A receptor [Rattus norvegicus]:Wild
hippocampus
Binding
Biochemical Pharmacology...
Title/Abstract Full Text Show Details
GABA-A receptor [Rattus norvegicus]:Wild
cerebellum
Binding
Biochemical Pharmacology...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
brain cortex
cells
Binding
Patent: US6469044 B1, ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
brain cortex
cells
Binding
Patent: US6469044 B1, ...
Title/Abstract Full Text Show Details
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Gould; Lundell; Homnick; Veber
Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1229 - 1239 Title/Abstract Full Text Show Details
1
IC50
>
100
µM
Cholecystokinin receptor [guinea pig]:Wild
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Gould; Lundell; Homnick; Veber
Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1229 - 1239 Title/Abstract Full Text Show Details
8.77
IC50
0.0017
µM
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Gould; Lundell; Homnick; Veber
Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1229 - 1239 Title/Abstract Full Text Show Details
8.57
IC50
2.7
nM
Sieghart; Schuster
Biochemical Pharmacology, 1984 , vol. 33, # 24 p. 4033 - 4038 Title/Abstract Full Text Show Details
8.54
IC50
2.9
nM
Sieghart; Schuster
Biochemical Pharmacology, 1984 , vol. 33, # 24 p. 4033 - 4038 Title/Abstract Full Text Show Details
Bmax
765
µmol/mg protein
Neurim Pharmaceuticals (1991) Ltd.
Patent: US6469044 B1, 2002 ; Title/Abstract Full Text Show Details
Bmax
870
µmol/mg protein
Neurim Pharmaceuticals (1991) Ltd.
Patent: US6469044 B1, 2002 ; Title/Abstract Full Text Show Details
7.82
Ki
15
nM
In Vitro (others)
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Maguire; Davies; Loew
European Journal of Pharmacology, 1995 , vol. 280, # 2 p. 167 - 173 Title/Abstract Full Text View citing articles Show Details
8.3
IC50
0.005
µM
GABA-A receptor [Rattus norvegicus]:Wild
brain
Binding
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Trapani; Franco; Latrofa; Genchi; Liso
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 1 p. 39 - 44 Title/Abstract Full Text View citing articles Show Details
GABA ratio
1.41
GABA-A receptor [Rattus norvegicus]:Wild
brain
Binding
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Trapani; Franco; Latrofa; Genchi; Liso
European Journal of Medicinal Chemistry, 1992 , vol. 27, # 1 p. 39 - 44 Title/Abstract Full Text View citing articles Show Details
8.42
IC50
3.8
nM
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
nerve cell
Binding
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Zhang; Liu; Huang; Koehler; Harris; Skolnick; Cook
European Journal of Medicinal Chemistry, 1995 , vol. 30, # 6 p. 483 - 496 Title/Abstract Full Text View citing articles Show Details
8.49
IC50
3.2
nM
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
8.23
IC50
5.9
nM
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
8.85
Kd
1.4
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
cerebellum
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
Bmax
57
pmol/g
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
cerebellum
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
8.83
Kd
1.48
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
hippocampus
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
Bmax
55.9
pmol/g
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
hippocampus
Binding
Arzneimittel-Forschung/D...
Title/Abstract Full Text View citing articles Show Details
Bechtel; Ensinger; Mierau
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 534 - 540 Title/Abstract Full Text View citing articles Show Details
8.92
IC50
1.2
nM
GABA-A receptor [Rattus norvegicus]:Wild
brain
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
cells
Binding
Farmaco, 1990 , vol. 45...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Duranti; Salvatori; Spadoni; Barone
Farmaco, 1990 , vol. 45, # 10 p. 1111 - 1117 Title/Abstract Full Text View citing articles Show Details
8.34
Ki
4.6
nM
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
8.74
Ki
1.8
nM
Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
8.42
Ki
3.8
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
6.8
Ki
160
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
8.51
Ki
3.1
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
alpha-1 [human]:Mutated Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
7.62
Ki
24
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Mutated
HEK293 cell line
Binding
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Anna Casula; Bromidge, Frances A.; Pillai, Gopalan V.; Wingrove, Peter B.; Martin, Karine; Maubach, Karen; Seabrook, Guy R.; Whiting, Paul J.; Hadingham, Karen L.
Journal of Neurochemistry, 2001 , vol. 77, # 2 p. 445 - 451 Title/Abstract Full Text View citing articles Show Details
8.05
Ki
8.9
nM
GABA-A receptor [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.89
Ki
13
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.82
Ki
15
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.32
Ki
48
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
8.36
Ki
4.4
nM
Gamma-aminobutyric acid receptor subunit
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.1
Ki
79
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.7
Ki
20
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
8
Ki
10
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
8.21
Ki
6.1
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.62
Ki
24
nM
Gamma-aminobutyric acid receptor subunit
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
7.7
Ki
20
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Kucken, Amy M.; Teissere, Jeremy A.; Seffinga-Clark, James; Wagner, David A.; Czajkowski, Cynthia
Molecular Pharmacology, 2003 , vol. 63, # 2 p. 289 - 296 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.19
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
HEK293 cell line
Binding
British Journal of Pharm...
Title/Abstract Full Text Show Details
HEK293 cell line
Binding
10 µM
British Journal of Pharm...
Title/Abstract Full Text Show Details
HEK293 cell line
Binding
10 µM
British Journal of Pharm...
Title/Abstract Full Text Show Details
HEK293 cell line
Binding
10 µM
British Journal of Pharm...
Title/Abstract Full Text Show Details
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
4.55
% Inhibition
26
%
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Mutated
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
1
% Inhibition
2
%
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-4 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
1
% Inhibition
6
%
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
% Stimulation
147.2
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
oocyte
Electrophysiology
British Journal of Pharm...
Title/Abstract Full Text Show Details
oocyte
Electrophysiology
British Journal of Pharm...
Title/Abstract Full Text Show Details
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
% Inhibition
5
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Mutated
Kelly; Smith; Banks; Wingrove; Whiting; Atack; Seabrook; Maubach
British Journal of Pharmacology, 2002 , vol. 135, # 1 p. 248 - 256 Title/Abstract Full Text Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.41
Ki
3.9
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.3
Ki
>
5000
nM
Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.72
EC50
1.9
nM
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39
oocyte
Electrophysiology
1.00000E11 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Title/Abstract Full Text View citing articles Show Details
% Max
104
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Electrophysiology
1.00000E11 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
nH
0.9
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
oocyte
Electrophysiology
1.00000E11 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
8.3
IC50
5
nM
cerebellum
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
8.15
IC50
7
nM
brain cortex
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
IC50
ND
spinal cord
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
8.52
Ki
3
nM
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
8.84
Ki
1.46
nM
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit
HEK293 cell line
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
alpha-2 [Rattus norvegicus]:Wild De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
8.78
Ki
1.66
nM
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
8.82
Ki
1.51
nM
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
1
Ki
>
10000
nM
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
7.94
EC50
11.6
nM
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
8.24
EC50
5.8
nM
Allosteric Modulator
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
beta-2 [Rattus norvegicus]:Wild Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
6.91
EC50
122
nM
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
8.17
EC50
6.8
nM
Allosteric Modulator
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
%
185
%
Allosteric Modulator
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
%
278
%
Allosteric Modulator
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
%
375
%
Allosteric Modulator
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
beta-2 [Rattus norvegicus]:Wild Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
6.2
Ki
629
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
6.23
Ki
587
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.3
Ki
>
5000
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.3
Ki
>
5000
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.78
Ki
1660
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.36
Ki
4390
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild +
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.86
Ki
1380
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
5.3
Ki
>
5000
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
HEK293 cell line
Binding
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
6.09
EC50
813
nM
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
oocyte
Electrophysiology
1.00000E11 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
% Max
91
%
Allosteric Modulator
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Mutated
oocyte
Electrophysiology
1.00000E11 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B; Safo, Patrick; Wheat, Lola; Thompson, Sally A; Wafford, Keith A; Whiting, Paul J
European Journal of Pharmacology, 2002 , vol. 437, # 1-2 p. 31 - 39 Title/Abstract Full Text View citing articles Show Details
7.39
EC50
40.5
nM
Allosteric Modulator
Davies, Martin; Newell, J. Glen; Dunn, Susan M. J.
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
oocyte
Electrophysiology
Journal of Neurochemistr...
Title/Abstract Full Text View citing articles Show Details
Journal of Neurochemistry, 2001 , vol. 79, # 1 p. 55 - 62 Title/Abstract Full Text View citing articles Show Details
8
Ki
10
nM
brain cortex
Binding
European journal of phar...
Title/Abstract Full Text Show Details
GABA-A receptor [Rattus norvegicus]:Wild
thalamus
Binding
Molecular pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-4 [Rattus norvegicus]:Wild
thalamus
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-4 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
GABA-A receptor [Rattus norvegicus]:Wild
thalamus
Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Pisu; Papi; Porcu; Trapani; Latrofa; Biggio; Serra
European journal of pharmacology, 2001 , vol. 432, # 2-3 p. 129 - 134 Title/Abstract Full Text Show Details
8.54
Ki
2.9
nM
Sur; Farrar; Kerby; Whiting; Atack; McKernan
Molecular pharmacology, 1999 , vol. 56, # 1 p. 110 - 115 Title/Abstract Full Text View citing articles Show Details
Ki
ND
Binding
Molecular pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sur; Farrar; Kerby; Whiting; Atack; McKernan
Molecular pharmacology, 1999 , vol. 56, # 1 p. 110 - 115 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
12
%
LTK-
Binding
10 µM
Molecular pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sur; Farrar; Kerby; Whiting; Atack; McKernan
Molecular pharmacology, 1999 , vol. 56, # 1 p. 110 - 115 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
11
%
Binding
10 µM
Molecular pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sur; Farrar; Kerby; Whiting; Atack; McKernan
Molecular pharmacology, 1999 , vol. 56, # 1 p. 110 - 115 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.2
nM
cells
Binding
Neuropsychopharmacology,...
Title/Abstract Full Text View citing articles Show Details
Atack, John R.; Smith, Alison J.; Emms, Frances; McKernan, Ruth M.
Neuropsychopharmacology, 1999 , vol. 20, # 3 p. 255 - 262 Title/Abstract Full Text View citing articles Show Details
8.6
Ki
2.5
nM
Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
cells
Binding
Neuropsychopharmacology,...
Title/Abstract Full Text View citing articles Show Details
Atack, John R.; Smith, Alison J.; Emms, Frances; McKernan, Ruth M.
Neuropsychopharmacology, 1999 , vol. 20, # 3 p. 255 - 262 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
4.5
nM
Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
cells
Binding
Neuropsychopharmacology,...
Title/Abstract Full Text View citing articles Show Details
Atack, John R.; Smith, Alison J.; Emms, Frances; McKernan, Ruth M.
Neuropsychopharmacology, 1999 , vol. 20, # 3 p. 255 - 262 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.1
nM
Gamma-aminobutyric
cells
Binding
Neuropsychopharmacology,...
acid receptor subunit alpha-5 [human]:Wild
Title/Abstract Full Text View citing articles Show Details
Atack, John R.; Smith, Alison J.; Emms, Frances; McKernan, Ruth M.
Neuropsychopharmacology, 1999 , vol. 20, # 3 p. 255 - 262 Title/Abstract Full Text View citing articles Show Details
8.64
Ki
2.3
nM
brain
cells
Binding
0.300000 nM
European Journal of Phar...
Title/Abstract Full Text Show Details
brain
cells
Binding
0.300000 nM
European Journal of Phar...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
Journal of Biological Ch...
Title/Abstract Full Text View citing articles Show Details
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
8.64
Ki
2.3
nM
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
8.52
Ki
3
nM
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
6.3
Ki
502
nM
Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Mutated
HEK293 cell line
Binding
Journal of Biological Ch...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
8.14
Ki
7.2
nM
Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Mutated
HEK293 cell line
Binding
Journal of Biological Ch...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
8.35
Kd
4.5
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Mutated
HEK293 cell line
Binding
Journal of Biological Ch...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
7.74
Kd
18
nM
Radioligand
Gamma-aminobutyric
HEK293 cell
Binding
Journal of Biological Ch...
(/ligand)
acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Mutated
line
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
nH
1
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Mutated
HEK293 cell line
Binding
Journal of Biological Ch...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Baur, Roland; Sigel, Erwin
Journal of Biological Chemistry, 1997 , vol. 272, # 18 p. 11799 - 11804 Title/Abstract Full Text View citing articles Show Details
4.42
Kd
37.74
µM
Radioligand (/ligand)
GABA-A receptor (Gamma 1) [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Wingrove, Peter B.; Thompson, Sally A.; Wafford, Keith A.; Whiting, Paul J.
Molecular Pharmacology, 1997 , vol. 52, # 5 p. 874 - 881 Title/Abstract Full Text View citing articles Show Details
8.52
Ki
3
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild +
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sigel, Erwin; Schaerer, Martin T.; Buhr, Andreas; Baur, Roland
Molecular Pharmacology, 1998 , vol. 54, # 6 p. 1097 - 1105 Title/Abstract Full Text View citing articles Show Details
6.3
Ki
500
nM
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sigel, Erwin; Schaerer, Martin T.; Buhr, Andreas; Baur, Roland
Molecular Pharmacology, 1998 , vol. 54, # 6 p. 1097 - 1105 Title/Abstract Full Text View citing articles Show Details
7.44
Ki
36
nM
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild Sigel, Erwin; Schaerer, Martin T.; Buhr, Andreas; Baur, Roland
Molecular Pharmacology, 1998 , vol. 54, # 6 p. 1097 - 1105 Title/Abstract Full Text View citing articles Show Details
8.1
Ki
8
nM
Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Sigel, Erwin; Schaerer, Martin T.; Buhr, Andreas; Baur, Roland
Molecular Pharmacology, 1998 , vol. 54, # 6 p. 1097 - 1105 Title/Abstract Full Text View citing articles Show Details
8
Kd
9.9
nM
Radioligand (/ligand)
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
Bmax
0.65
pmol/mg
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
7.95
Kd
11.3
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Chimera + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
Bmax
0.34
pmol/mg
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Chimera + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
7.88
Kd
13.3
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Chimera +
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
Bmax
0.57
pmol/mg
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Chimera + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Boileau, Andrew J.; Kucken, Amy M.; Evers, Amy R.; Czajkowski, Cynthia
Molecular Pharmacology, 1998 , vol. 53, # 2 p. 295 - 303 Title/Abstract Full Text View citing articles Show Details
Ki
ND
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
7
Ki
>
100
nM
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
Ki
ND
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
Ki
ND
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
pX
Parameter
8.03
Kd
Value (qual)
Value (quant)
Unit
9.3
nM
Action on Target Radioligand (/ligand)
Target
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all)
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
LTK-
Binding
Neuropharmacology, 1996 ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
LTK-
Binding
Neuropharmacology, 1996 ...
Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
LTK-
Binding
Neuropharmacology, 1996 ...
Title/Abstract Full Text View citing articles Show Details
Davies; Martin; Bateson; Hadingham; Whiting; Dunn
Neuropharmacology, 1996 , vol. 35, # 9-10 p. 1199 - 1208 Title/Abstract Full Text View citing articles Show Details
7.82
Kd
15.3
nM
Radioligand (/ligand)
Davies; Martin; Bateson; Hadingham; Whiting; Dunn
Neuropharmacology, 1996 , vol. 35, # 9-10 p. 1199 - 1208 Title/Abstract Full Text View citing articles Show Details
Kd
ND
Radioligand (/ligand)
Davies; Martin; Bateson; Hadingham; Whiting; Dunn
Neuropharmacology, 1996 , vol. 35, # 9-10 p. 1199 - 1208 Title/Abstract Full Text View citing articles Show Details
6.28
% Inhibition
100
%
GABA-A receptor [taurine cattle]:Wild
brain cortex
Binding
10 µM
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Selleri, Silvia; Bruni, Fabrizio; Costagli, Camilla; Costanzo, Annarella; Guerrini, Gabriella; Ciciani, Giovanna; Costa, Barbara; Martini, Claudia
Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 12 p. 2705 - 2711 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.17
nM
GABA-A receptor [taurine cattle]:Wild
brain cortex
Binding
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Selleri, Silvia; Bruni, Fabrizio; Costagli, Camilla; Costanzo, Annarella; Guerrini, Gabriella; Ciciani, Giovanna; Costa, Barbara; Martini, Claudia
Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 12 p. 2705 - 2711 Title/Abstract Full Text View citing articles Show Details
7.37
Kd
43
nM
Radioligand (/ligand)
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
Bmax
#
400
fmol/mg protein
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Mutated + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Buhr, Andreas; Schaerer, Martin T.; Baur, Roland; Sigel, Erwin
Molecular Pharmacology, 1997 , vol. 52, # 4 p. 676 - 682 Title/Abstract Full Text View citing articles Show Details
8.59
Ki
2.6
nM
In Vitro (others)
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
8.33
Ki
4.7
nM
In Vitro (others)
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
8.23
Ki
5.9
nM
In Vitro (others)
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
8.49
Ki
3.2
nM
In Vitro (others)
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
8.47
Kd
3.4
nM
In Vitro (others)
0.100000 nM
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
8.37
Kd
4.3
nM
In Vitro (others)
0.100000 nM
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
7.72
% Inhibition
100
%
GABA-A receptor [Rattus norvegicus]:Wild
brain
GABA-A receptor
brain
cells
Binding
360 nM
Farmaco, 1989 , vol. 44...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
1
%
21.7
%
cells
Binding
0.0360000
Farmaco, 1989 , vol. 44...
Inhibition
[Rattus norvegicus]:Wild
nM
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
9.37
% Inhibition
45.9
%
GABA-A receptor [Rattus norvegicus]:Wild
brain
GABA-A receptor [Rattus norvegicus]:Wild
brain
GABA-A receptor [Rattus norvegicus]:Wild
brain
GABA-A receptor [Rattus norvegicus]:Wild
brain
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
cells
Binding
0.360000 nM
Farmaco, 1989 , vol. 44...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
9.24
% Inhibition
86.3
%
cells
Binding
3.60000 nM
Farmaco, 1989 , vol. 44...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
8.72
% Inhibition
98.8
%
cells
Binding
36 nM
Farmaco, 1989 , vol. 44...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
9.16
IC50
0.688
nM
cells
Binding
Farmaco, 1989 , vol. 44...
Title/Abstract Full Text View citing articles Show Details
Balsamini; Spadoni; Duranti; Cerrini; Lamba; Fedeli
Farmaco, 1989 , vol. 44, # 4 p. 399 - 413 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.2
nM
LTK-
Binding
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Yu, Shu; Ma, Chunrong; He, Xiaohui; McKernan, Ruth; Cook, James M.
Medicinal Chemistry Research, 1999 , vol. 9, # 2 p. 71 - 88 Title/Abstract Full Text View citing articles Show Details
8.6
Ki
2.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Yu, Shu; Ma, Chunrong; He, Xiaohui; McKernan, Ruth; Cook, James M.
Medicinal Chemistry Research, 1999 , vol. 9, # 2 p. 71 - 88 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
4.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
LTK-
Binding
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Yu, Shu; Ma, Chunrong; He, Xiaohui; McKernan, Ruth; Cook, James M.
Medicinal Chemistry Research, 1999 , vol. 9, # 2 p. 71 - 88 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.1
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild
LTK-
Binding
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Yu, Shu; Ma, Chunrong; He, Xiaohui; McKernan, Ruth; Cook, James M.
Medicinal Chemistry Research, 1999 , vol. 9, # 2 p. 71 - 88 Title/Abstract Full Text View citing articles Show Details
5.7
Ki
>
2000
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild
LTK-
Binding
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Yu, Shu; Ma, Chunrong; He, Xiaohui; McKernan, Ruth; Cook, James M.
Medicinal Chemistry Research, 1999 , vol. 9, # 2 p. 71 - 88 Title/Abstract Full Text View citing articles Show Details
8.52
IC50
3
nM
brain cortex
Binding
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
In Vitro (others)
Analytical Chemistry, 20...
Title/Abstract Full Text View citing articles Show Details
Dodd; Ouannes; Potier; Prado de Carvalho; Rossier
Journal of Medicinal Chemistry, 1987 , vol. 30, # 7 p. 1248 - 1254 Title/Abstract Full Text Show Details
9.09
Kd
0.81
nM
Kitabatake; Moaddel; Cole; Gandhari; Frazier; Hartenstein; Rosenberg; Bernier; Wainer
Analytical Chemistry, 2008 , vol. 80, # 22 p. 8673 - 8680 Title/Abstract Full Text View citing articles Show Details
8.98
Kd
1.05
nM
In Vitro (others)
Analytical Chemistry, 20...
Title/Abstract Full Text View citing articles Show Details
Kitabatake; Moaddel; Cole; Gandhari; Frazier; Hartenstein; Rosenberg; Bernier; Wainer
Analytical Chemistry, 2008 , vol. 80, # 22 p. 8673 - 8680 Title/Abstract Full Text View citing articles Show Details
8.89
Kd
1.3
nM
Radioligand (/ligand)
Ionotropic gamma aminobutyric acid receptor [Rattus norvegicus]:Wild
brain cortex
cells
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Holland; Mckeon; Covey; Ferrendelli
Journal of Pharmacology and Experimental Therapeutics, 1990 , vol. 254, # 2 p. 578 - 583 Title/Abstract Full Text View citing articles Show Details
Bmax
0.84
pmol/mg protein
Radioligand (/ligand)
Ionotropic gamma aminobutyric acid receptor [Rattus norvegicus]:Wild
brain cortex
cells
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Holland; Mckeon; Covey; Ferrendelli
Journal of Pharmacology and Experimental Therapeutics, 1990 , vol. 254, # 2 p. 578 - 583 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
NA
Gamma hydroxybutyric acid receptor [Rattus norvegicus]:Wild
brain cortex
Mehta, Ashok K.; Muschaweck, Nicole M.; Maeda, Dean Y.; Coop, Andrew; Ticku, Maharaj K.
Journal of Pharmacology and Experimental Therapeutics, 2001 , vol. 299, # 3 p. 1148 - 1153
cells
Binding
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Title/Abstract Full Text View citing articles Show Details
1
%
NA
Gamma hydroxybutyric acid receptor [Rattus norvegicus]:Wild
brain cortex
cells
Binding
10 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Mehta, Ashok K.; Muschaweck, Nicole M.; Maeda, Dean Y.; Coop, Andrew; Ticku, Maharaj K.
Journal of Pharmacology and Experimental Therapeutics, 2001 , vol. 299, # 3 p. 1148 - 1153 Title/Abstract Full Text View citing articles Show Details
1
Ki
>
10000
nM
Gamma-aminobutyric acid receptor subunit alpha-6 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
Nature, 1990 , vol. 346...
Title/Abstract Full Text Show Details
HEK293T cell line
Binding
Patent: WO2007/2359 A3...
Title/Abstract Full Text Show Details
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Lueddens; Pritchett; Koehler; Killisch; Keinaenen; Monyer; Sprengel; Seeburg
Nature, 1990 , vol. 346, # 6285 p. 648 - 651 Title/Abstract Full Text Show Details
6
Ki
>>
1000
nM
Gamma-aminobutyric acid receptor subunit alpha-4 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit delta [Rattus norvegicus]:Wild
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; WALLNER, Martin; OLSEN, Richard, W.; HANCHAR, Harry, J.
Patent: WO2007/2359 A3, 2007 ; Title/Abstract Full Text Show Details
8.66
Ki
2.2
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
LTK-
Huang, Qi; He, Xiaohui; Ma, Chunrong; Liu, Ruiyan; Yu, Shu; Dayer, Charlotte A.; Wenger, Galen R.; McKernan, Ruth; Cook, James M.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 71 - 95 Title/Abstract Full Text View citing articles Show Details
8.6
Ki
2.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; He, Xiaohui; Ma, Chunrong; Liu, Ruiyan; Yu, Shu; Dayer, Charlotte A.; Wenger, Galen R.; McKernan, Ruth; Cook, James M.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 71 - 95 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
4.5
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; He, Xiaohui; Ma, Chunrong; Liu, Ruiyan; Yu, Shu; Dayer, Charlotte A.; Wenger, Galen R.; McKernan, Ruth; Cook, James M.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 71 - 95 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.1
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; He, Xiaohui; Ma, Chunrong; Liu, Ruiyan; Yu, Shu; Dayer, Charlotte A.; Wenger, Galen R.; McKernan, Ruth; Cook, James M.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 71 - 95 Title/Abstract Full Text View citing articles Show Details
5.7
Ki
>
2000
nM
Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-6 [human]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild
LTK-
Binding
1.00000E09 M
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; He, Xiaohui; Ma, Chunrong; Liu, Ruiyan; Yu, Shu; Dayer, Charlotte A.; Wenger, Galen R.; McKernan, Ruth; Cook, James M.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 1 p. 71 - 95 Title/Abstract Full Text View citing articles Show Details
8.55
Ki
2.8
nM
GABA-A receptor [Rattus norvegicus]:Wild
forebrain
Binding
European Journal of Phar...
Title/Abstract Full Text Show Details
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
0.350000 nM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Braestrup; Squires
European Journal of Pharmacology, 1978 , vol. 48, # 3 p. 263 - 270 Title/Abstract Full Text Show Details
kon
0.25
nM1.min-1
Radioligand (/ligand)
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
koff
0.045
min-1
Radioligand (/ligand)
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
0.350000 nM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
9.74
Kd
0.18
nM
Radioligand (/ligand)
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
0.350000 nM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
t1/2 off
4.6
minute
Radioligand (/ligand)
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
0.350000 nM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
8.78
Ki
Richelson; Nelson; Neeper
1.66
nM
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
8.21
Ki
6.2
nM
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
nH
0.89
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Richelson; Nelson; Neeper
Journal of Pharmacology and Experimental Therapeutics, 1991 , vol. 256, # 3 p. 897 - 901 Title/Abstract Full Text View citing articles Show Details
8.89
Kd
1.3
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
8.82
Kd
1.5
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
hippocampus
nerve cell
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
Bmax
190
fmol/mg protein
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit beta-3 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit gamma-2 [Rattus norvegicus]:Wild
HEK293 cell line
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
Bmax
1712
fmol/mg protein
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
hippocampus
nerve cell
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
8.82
Kd
1.5
nM
Radioligand (/ligand)
GABA-A receptor [Rattus norvegicus]:Wild
brain cortex
nerve cell
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
Bmax
1160
fmol/mg protein
Radioligand (/ligand)
GABA-A receptor [Rattus
brain cortex
nerve cell
Binding
0 nM
The Journal of pharmacol...
Title/Abstract Full Text View citing articles Show Details
norvegicus]:Wild
Skolnick; Hu; Cook; Hurt; Trometer; Liu; Huang
The Journal of pharmacology and experimental therapeutics, 1997 , vol. 283, # 2 p. 488 - 493 Title/Abstract Full Text View citing articles Show Details
5.5
Ki
3136
nM
GABA-A receptor [Rattus norvegicus]:Wild
parotid gland
GABA-A receptor [Rattus norvegicus]:Wild
submandibular gland
parotid gland
cells
Binding
1.00000E10 M
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Yamagishi, Hisako; Kawaguchi, Mitsuru
Biochemical Pharmacology, 1998 , vol. 55, # 2 p. 209 - 214 Title/Abstract Full Text View citing articles Show Details
5.46
Ki
3450
nM
cells
Binding
1.00000E10 M
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Yamagishi, Hisako; Kawaguchi, Mitsuru
Biochemical Pharmacology, 1998 , vol. 55, # 2 p. 209 - 214 Title/Abstract Full Text View citing articles Show Details
7.83
Ki
14.9
nM
cells
Binding
1.00000E10 M
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Yamagishi, Hisako; Kawaguchi, Mitsuru
Biochemical Pharmacology, 1998 , vol. 55, # 2 p. 209 - 214 Title/Abstract Full Text View citing articles Show Details
7.39
Ki
40.4
nM
submandibular gland
cells
Binding
1.00000E10 M
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Yamagishi, Hisako; Kawaguchi, Mitsuru
Biochemical Pharmacology, 1998 , vol. 55, # 2 p. 209 - 214 Title/Abstract Full Text View citing articles Show Details
8.05
Ki
8.9
nM
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
LTK-
Binding
Proceedings of the Natio...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Harkness; McKernan; Quirk; Le Bourdelles; Horne; Kemp; Barnard; Ragan; Whiting
Proceedings of the National Academy of Sciences of the United States of America, 1992 , vol. 89, # 14 p. 6378 - 6382 Title/Abstract Full Text View citing articles Show Details
%
184
%
Agonist
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-1 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
LTK-
Electrophysiology
100 nM
Proceedings of the Natio...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Harkness; McKernan; Quirk; Le Bourdelles; Horne; Kemp; Barnard; Ragan; Whiting
Proceedings of the National Academy of Sciences of the United States of America, 1992 , vol. 89, # 14 p. 6378 - 6382 Title/Abstract Full Text View citing articles Show Details
8.66
Ki
2.2
nM
In Vitro (others)
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; Zhang, Weijiang; Liu, Ruiyan; McKernan, Ruth M.; Cook, James M.
Medicinal Chemistry Research, 1996 , vol. 6, # 6 p. 384 - 391 Title/Abstract Full Text View citing articles Show Details
8.6
Ki
2.5
nM
In Vitro (others)
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; Zhang, Weijiang; Liu, Ruiyan; McKernan, Ruth M.; Cook, James M.
Medicinal Chemistry Research, 1996 , vol. 6, # 6 p. 384 - 391 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
4.5
nM
In Vitro (others)
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; Zhang, Weijiang; Liu, Ruiyan; McKernan, Ruth M.; Cook, James M.
Medicinal Chemistry Research, 1996 , vol. 6, # 6 p. 384 - 391 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.1
nM
In Vitro (others)
1.00000E09 M
Medicinal Chemistry Rese...
Title/Abstract Full Text View citing articles Show Details
Huang, Qi; Zhang, Weijiang; Liu, Ruiyan; McKernan, Ruth M.; Cook, James M.
Medicinal Chemistry Research, 1996 , vol. 6, # 6 p. 384 - 391 Title/Abstract Full Text View citing articles Show Details
8.68
Ki
2.11
nM
In Vitro (others)
European Journal of Phar...
Title/Abstract Full Text Show Details
In Vitro (others)
European Journal of Phar...
Title/Abstract Full Text Show Details
In Vitro (others)
European Journal of Phar...
Title/Abstract Full Text Show Details
In Vitro (others)
European Journal of Phar...
Title/Abstract Full Text Show Details
Hadingham; Wafford; Thompson; Palmer; Whiting
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 3 p. 301 - 309 Title/Abstract Full Text Show Details
7.96
Ki
11
nM
Hadingham; Wafford; Thompson; Palmer; Whiting
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 3 p. 301 - 309 Title/Abstract Full Text Show Details
8.16
EC50
6.9
nM
Hadingham; Wafford; Thompson; Palmer; Whiting
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 3 p. 301 - 309 Title/Abstract Full Text Show Details
6.95
EC50
110.7
nM
Hadingham; Wafford; Thompson; Palmer; Whiting
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 3 p. 301 - 309 Title/Abstract Full Text Show Details
8.57
Ki
2.72
nM
brain cortex
Binding
Life Sciences, 1978 , v...
Title/Abstract Full Text Show Details
brain cortex
Binding
Life Sciences, 1978 , v...
Title/Abstract Full Text Show Details
frontal cortex
Binding
Life Sciences, 1978 , v...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild
hippocampus
Binding
Neuropharmacology, 1996 ...
Title/Abstract Full Text Show Details
Speth; Wastek; Johnson; Yamamura
Life Sciences, 1978 , vol. 22, # 10 p. 859 - 866 Title/Abstract Full Text Show Details
nH
1.095
Speth; Wastek; Johnson; Yamamura
Life Sciences, 1978 , vol. 22, # 10 p. 859 - 866 Title/Abstract Full Text Show Details
8.66
Ki
2.2
nM
Mohler; Okada; Heitz Ph.; Ulrich
Life Sciences, 1978 , vol. 22, # 11 p. 985 - 996 Title/Abstract Full Text Show Details
8.19
Ki
6.51
nM
Quirk; Blurton; Fletcher; Leeson; Tang; Mellilo; Ragan; McKernan
Neuropharmacology, 1996 , vol. 35, # 9-10 p. 1331 - 1335 Title/Abstract Full Text Show Details
nH
0.94
Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild
hippocampus
Binding
Neuropharmacology, 1996 ...
Title/Abstract Full Text Show Details
HEK293 cell line
Electrophysiology
0.00100000 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Quirk; Blurton; Fletcher; Leeson; Tang; Mellilo; Ragan; McKernan
Neuropharmacology, 1996 , vol. 35, # 9-10 p. 1331 - 1335 Title/Abstract Full Text Show Details
7.51
EC50
31
nM
Agonist
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [Rattus norvegicus]:Wild
Knoflach; Drescher; Scheurer; Malherbe; Mohler
Journal of Pharmacology and Experimental Therapeutics, 1993 , vol. 266, # 1 p. 385 - 391 Title/Abstract Full Text View citing articles Show Details
8.7
EC50
2
nM
Agonist
Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild
HEK293 cell line
Electrophysiology
0.00100000 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Knoflach; Drescher; Scheurer; Malherbe; Mohler
Journal of Pharmacology and Experimental Therapeutics, 1993 , vol. 266, # 1 p. 385 - 391 Title/Abstract Full Text View citing articles Show Details
7.28
% Stimulation
128
%
Agonist
Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [Rattus norvegicus]:Wild
HEK293 cell line
Electrophysiology
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Knoflach; Drescher; Scheurer; Malherbe; Mohler
Journal of Pharmacology and Experimental Therapeutics, 1993 , vol. 266, # 1 p. 385 - 391 Title/Abstract Full Text View citing articles Show Details
8.28
% Stimulation
155
%
Agonist
Gamma-aminobutyric acid receptor subunit alpha-5 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + GABA-A receptor (Gamma 2S) [Rattus norvegicus]:Wild
HEK293 cell line
Electrophysiology
100 nM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Knoflach; Drescher; Scheurer; Malherbe; Mohler
Journal of Pharmacology and Experimental Therapeutics, 1993 , vol. 266, # 1 p. 385 - 391 Title/Abstract Full Text View citing articles Show Details
8.28
Ki
5.2
nM
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
6
Ki
1000
nM
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
7.85
IC50
14
nM
In Vitro (others)
1.00000E10 M
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
6.68
IC50
210
nM
In Vitro (others)
1.00000E10 M
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
7.94
Ki
11.5
nM
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-1 [human]:Wild + GABA-A receptor (Gamma 2S) [human]:Wild
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Le Bourdelles; Palmer; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 43, # 6 p. 970 - 975 Title/Abstract Full Text View citing articles Show Details
8.28
Ki
5.2
nM
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Le Bourdelles; Palmer; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 43, # 6 p. 970 - 975 Title/Abstract Full Text View citing articles Show Details
7.8
Ki
15.7
nM
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
Hadingham; Wingrove; Le Bourdelles; Palmer; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 43, # 6 p. 970 - 975 Title/Abstract Full Text View citing articles Show Details
8.26
Ki
5.5
nM
Hadingham; Wingrove; Le Bourdelles; Palmer; Ragan; Whiting
Molecular Pharmacology, 1993 , vol. 43, # 6 p. 970 - 975 Title/Abstract Full Text View citing articles Show Details
HEK293 cell line
Binding
Molecular Pharmacology, ...
Title/Abstract Full Text View citing articles Show Details
7.64
EC50
23.1
nM
Allosteric Modulator
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
fibroblast
Electrophysiology
British journal of pharm...
Title/Abstract Full Text Show Details
GABA-A receptor (Gamma 2L) [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
fibroblast
Electrophysiology
British journal of pharm...
Title/Abstract Full Text Show Details
GABA-A receptor [taurine cattle]:Wild
brain cortex
Binding
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Horne; Hadingham; Macaulay; Whiting; Kemp
British journal of pharmacology, 1992 , vol. 107, # 3 p. 732 - 737 Title/Abstract Full Text Show Details
Emax(%)
208
%
Allosteric Modulator
Horne; Hadingham; Macaulay; Whiting; Kemp
British journal of pharmacology, 1992 , vol. 107, # 3 p. 732 - 737 Title/Abstract Full Text Show Details
8.29
Ki
5.17
nM
Anzini, Maurizio; Valenti, Salvatore; Braile, Carlo; Cappelli, Andrea; Vomero, Salvatore; Alcaro, Stefano; Ortuso, Francesco; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Daniele, Simona; Martini, Claudia; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5694 - 5711 Title/Abstract Full Text View citing articles Show Details
8.19
Ki
6.5
nM
ionotropic gamma aminobutyric acid a receptor [human]:Wild
brain cortex
Binding
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Anzini, Maurizio; Valenti, Salvatore; Braile, Carlo; Cappelli, Andrea; Vomero, Salvatore; Alcaro, Stefano; Ortuso, Francesco; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Daniele, Simona; Martini, Claudia; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5694 - 5711 Title/Abstract Full Text View citing articles Show Details
1
IC50
>
100
µM
Cholecystokinin receptor type A [Rattus norvegicus]:Wild
pancreas
Binding
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Lundell; Veber; Anderson; Chang; Lotti; Cerino; Chen; Kling; Kunkel; Springer; Hirshfield
Journal of Medicinal Chemistry, 1988 , vol. 31, # 12 p. 2235 - 2246 Title/Abstract Full Text Show Details
1
IC50
>
100
µM
Gastrin/cholecystokinin type B receptor [guinea pig]:Wild
brain cortex
Binding
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Lundell; Veber; Anderson; Chang; Lotti; Cerino; Chen; Kling; Kunkel; Springer; Hirshfield
Journal of Medicinal Chemistry, 1988 , vol. 31, # 12 p. 2235 - 2246 Title/Abstract Full Text Show Details
8.77
IC50
0.0017
µM
brain
Binding
Evans; Rittle; Bock; DiPardo; Freidinger; Whitter; Lundell; Veber; Anderson; Chang; Lotti; Cerino; Chen; Kling; Kunkel; Springer; Hirshfield
Journal of Medicinal Chemistry, 1988 , vol. 31, # 12 p. 2235 - 2246 Title/Abstract Full Text Show Details
8.62
Ki
2.4
nM
brain
Binding
British Journal of Clini...
Title/Abstract Full Text Show Details
Binding
1.00000E09 M
European Journal of Phar...
Title/Abstract Full Text Show Details
Dorow; Seidler; Schneider
British Journal of Clinical Pharmacology, 1982 , vol. 13, # 4 p. 561 - 565 Title/Abstract Full Text Show Details
8.82
IC50
1.52
nM
Giorgi; Lecca; Cancedda; Serra; Corda
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 290, # 1 p. 37 - 47 Title/Abstract Full Text Show Details
8.61
IC50
2.46
nM
Binding
1.00000E10 M
European Journal of Phar...
Title/Abstract Full Text Show Details
Binding
1.00000E09 M
European Journal of Phar...
Title/Abstract Full Text Show Details
Binding
1.00000E10 M
European Journal of Phar...
Title/Abstract Full Text Show Details
In Vitro (others)
1.00000E09 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Giorgi; Lecca; Cancedda; Serra; Corda
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 290, # 1 p. 37 - 47 Title/Abstract Full Text Show Details
8.86
IC50
1.37
nM
Giorgi; Lecca; Cancedda; Serra; Corda
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 290, # 1 p. 37 - 47 Title/Abstract Full Text Show Details
8.12
IC50
7.62
nM
Giorgi; Lecca; Cancedda; Serra; Corda
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 290, # 1 p. 37 - 47 Title/Abstract Full Text Show Details
5.08
IC50
8.4
µM
Fuchs; Zezula; Slany; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 289, # 1 p. 87 - 95 Title/Abstract Full Text View citing articles Show Details
6.92
IC50
120
nM
In Vitro (others)
1.00000E09 M
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Fuchs; Zezula; Slany; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 289, # 1 p. 87 - 95 Title/Abstract Full Text View citing articles Show Details
7.98
Kd
10.52 11.69
nM
In Vitro (others)
0.800000 nM
Biological and Pharmaceu...
Title/Abstract Full Text View citing articles Show Details
Srivastava, Kalpana; Hatanaka, Tomomi; Katayama, Kazunori; Koizumi, Tamotsu
Biological and Pharmaceutical Bulletin, 1999 , vol. 22, # 3 p. 288 - 294 Title/Abstract Full Text View citing articles Show Details
pIC50
-0.58
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1:Wild
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild +
oocyte
Patent: WO1998/23742 A...
Title/Abstract Full Text Show Details
Maddalena; Johnston
Journal of Medicinal Chemistry, 1995 , vol. 38, # 4 p. 715 - 724 Title/Abstract Full Text Show Details
pIC50
-0.58
Radioligand (/ligand)
Maddalena; Johnston
Journal of Medicinal Chemistry, 1995 , vol. 38, # 4 p. 715 - 724 Title/Abstract Full Text Show Details
%
=
0
%
Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild MERCK SHARP and DOHME LIMITED
Patent: WO1998/23742 A1, 1998 ; Title/Abstract Full Text Show Details
8.66
Ki
=
2.2
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Patent: WO1998/23742 A...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
oocyte
Patent: WO1998/23742 A...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
MERCK SHARP and DOHME LIMITED
Patent: WO1998/23742 A1, 1998 ; Title/Abstract Full Text Show Details
%
=
121
%
MERCK SHARP and DOHME LIMITED
Patent: WO1998/23742 A1, 1998 ; Title/Abstract Full Text Show Details
8.14
Ki
=
7.2
nM
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
8.1
Kd
=
7.9
nM
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
receptor subunit alpha1:Wild Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
8.42
Kd
=
3.8
nM
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
7.74
Ki
=
18
nM
Inhibitor
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
7.62
IC50
=
24
nM
Inhibitor
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
spinal cord
Bioorganic and Medicinal...
Title/Abstract Full Text Show Details
Bioorganic and Medicinal...
Title/Abstract Full Text Show Details
spinal cord
Bioorganic and Medicinal...
Title/Abstract Full Text Show Details
cerebellum cell
Bioorganic and Medicinal...
Title/Abstract Full Text Show Details
Bioorganic and medicinal...
Title/Abstract Full Text Show Details
Schove; Chen; Beatty; Maguire; Davies; Loew
Bioorganic and Medicinal Chemistry, 1995 , vol. 3, # 11 p. 1547 - 1561 Title/Abstract Full Text Show Details
8.82
Ki
=
1.5
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Schove; Chen; Beatty; Maguire; Davies; Loew
Bioorganic and Medicinal Chemistry, 1995 , vol. 3, # 11 p. 1547 - 1561 Title/Abstract Full Text Show Details
7.62
IC50
=
24
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Schove; Chen; Beatty; Maguire; Davies; Loew
Bioorganic and Medicinal Chemistry, 1995 , vol. 3, # 11 p. 1547 - 1561 Title/Abstract Full Text Show Details
8.82
Ki
=
1.5
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Schove; Chen; Beatty; Maguire; Davies; Loew
Bioorganic and Medicinal Chemistry, 1995 , vol. 3, # 11 p. 1547 - 1561 Title/Abstract Full Text Show Details
11.2
ED50
=
0.007
nM
Agonist
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Schove; Perez; Loew
Bioorganic and medicinal chemistry, 1994 , vol. 2, # 10 p. 1029 - 1049 Title/Abstract Full Text Show Details
8.83
Ki
=
1.49
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Bioorganic and medicinal...
Title/Abstract Full Text Show Details
Bioorganic and medicinal...
Title/Abstract Full Text Show Details
Chemical Biology and Dru...
Title/Abstract Full Text View citing articles Show Details
Schove; Perez; Loew
Bioorganic and medicinal chemistry, 1994 , vol. 2, # 10 p. 1029 - 1049 Title/Abstract Full Text Show Details
8.83
Ki
=
1.49
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Schove; Perez; Loew
Bioorganic and medicinal chemistry, 1994 , vol. 2, # 10 p. 1029 - 1049 Title/Abstract Full Text Show Details
1
IC50
>
50
µM
Menezes, Carla M.S.; Rivera, Gildardo; Alves, Marina A.; Do Amaral, Daniel N.; Thibaut, Jean Pierre B.; Noel, Francois; Barreiro, Eliezer J.; Lima, Lidia M.
Chemical Biology and Drug Design, 2012 , vol. 79, # 6 p. 943 - 949 Title/Abstract Full Text View citing articles Show Details
pIC50
-0.58
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1:Wild
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta-
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
So; Karplus
Journal of Medicinal Chemistry, 1996 , vol. 39, # 26 p. 5246 - 5256 Title/Abstract Full Text View citing articles Show Details
pIC50
-0.58
Radioligand (/ligand)
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
So; Karplus
Journal of Medicinal Chemistry, 1996 , vol. 39, # 26 p. 5246 - 5256 Title/Abstract Full Text View citing articles Show Details
%
=
0.75
%
L-M(TK-) cell line
British Journal of Pharm...
Title/Abstract Full Text View citing articles Show Details
Lambert; Belelli
British Journal of Pharmacology, 2002 , vol. 136, # 7 p. 957 - 959 Title/Abstract Full Text View citing articles Show Details
%
=
-3.1
%
L-M(TK-) cell line
British Journal of Pharm...
Title/Abstract Full Text View citing articles Show Details
Lambert; Belelli
British Journal of Pharmacology, 2002 , vol. 136, # 7 p. 957 - 959 Title/Abstract Full Text View citing articles Show Details
Activity
=
3
nM
Nature chemical biology,...
Title/Abstract Full Text Show Details
2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild Richter, Lars; de Graaf, Chris; Sieghart, Werner; Varagic, Zdravko; Moerzinger, Martina; de Esch, Iwan J P; Ecker, Gerhard F; Ernst, Margot
Nature chemical biology, 2012 , vol. 8, # 5 p. 455 - 464 Title/Abstract Full Text Show Details
4.82
IC50
=
15
µM
Inhibitor
Aldo-keto reductase family 1 member C1 [human]:Wild
Biological and pharmaceu...
Title/Abstract Full Text Show Details
Biological and pharmaceu...
Title/Abstract Full Text Show Details
Biological and pharmaceu...
Title/Abstract Full Text Show Details
Biological and pharmaceu...
Title/Abstract Full Text Show Details
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Usami, Noriyuki; Yamamoto, Tomohiro; Shintani, Syunichi; Ishikura, Shuhei; Higaki; Katagiri, Yoshihiro; Hara, Akira
Biological and pharmaceutical bulletin, 2002 , vol. 25, # 4 p. 441 - 445 Title/Abstract Full Text Show Details
4.89
IC50
=
13
µM
Inhibitor
Aldo-keto reductase family 1 member C2 [human]:Wild
Usami, Noriyuki; Yamamoto, Tomohiro; Shintani, Syunichi; Ishikura, Shuhei; Higaki; Katagiri, Yoshihiro; Hara, Akira
Biological and pharmaceutical bulletin, 2002 , vol. 25, # 4 p. 441 - 445 Title/Abstract Full Text Show Details
4.49
IC50
=
32
µM
Inhibitor
Aldo-keto reductase family 1 member C4 [human]:Wild
Usami, Noriyuki; Yamamoto, Tomohiro; Shintani, Syunichi; Ishikura, Shuhei; Higaki; Katagiri, Yoshihiro; Hara, Akira
Biological and pharmaceutical bulletin, 2002 , vol. 25, # 4 p. 441 - 445 Title/Abstract Full Text Show Details
4.24
IC50
=
58
µM
Inhibitor
Aldo-keto reductase family 1 member C3 [human]:Wild
Usami, Noriyuki; Yamamoto, Tomohiro; Shintani, Syunichi; Ishikura, Shuhei; Higaki; Katagiri, Yoshihiro; Hara, Akira
Biological and pharmaceutical bulletin, 2002 , vol. 25, # 4 p. 441 - 445 Title/Abstract Full Text Show Details
MED
=
1.5
µM/kg
Agonist
Peripheral-type benzodiazepine receptor-associated protein 1:Wild
Harris, Danni L; Loew, Gilda
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 11 p. 2527 - 2538 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
=
4.5
nM
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Marder, Mariel; Estiu, Guillermina; Blanch, Luis Bruno; Viola, Haydee; Wasowski, Cristina; Medina, Jorge H.; Paladini, Alejandro C.
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 323 - 335 Title/Abstract Full Text View citing articles Show Details
5.7
Ki
>
2000
nM
Inhibitor
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Marder, Mariel; Estiu, Guillermina; Blanch, Luis Bruno; Viola, Haydee; Wasowski, Cristina; Medina, Jorge H.; Paladini, Alejandro C.
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 323 - 335 Title/Abstract Full Text View citing articles Show Details
8.35
Ki
=
4.5
nM
Inhibitor
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
receptor subunit alpha1:Wild Marder, Mariel; Estiu, Guillermina; Blanch, Luis Bruno; Viola, Haydee; Wasowski, Cristina; Medina, Jorge H.; Paladini, Alejandro C.
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 323 - 335 Title/Abstract Full Text View citing articles Show Details
5.7
Ki
>
2
µM
Inhibitor
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Marder, Mariel; Estiu, Guillermina; Blanch, Luis Bruno; Viola, Haydee; Wasowski, Cristina; Medina, Jorge H.; Paladini, Alejandro C.
Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 323 - 335 Title/Abstract Full Text View citing articles Show Details
8.42
IC50
=
3.8
nM
Inhibitor
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
European journal of medi...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Chemical reviews, 1994 ,...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [taurine cattle]:Wild
Chemical Reviews, 2004 ,...
Title/Abstract Full Text View citing articles Show Details
W Zhang; R Liu; Q Huang; P Zhang; KF Koehler; B Harris; P Skolnick; JM Cook
European journal of medicinal chemistry, 1995 , vol. 30, # 6 p. 483 - 496 Title/Abstract Full Text Show Details
MED
=
4.19
mg/kg
Blair; Webb
Journal of Medicinal Chemistry, 1977 , vol. 20, # 9 p. 1206 - 1210 Title/Abstract Full Text Show Details
ED50
=
2.49
mg/kg
Blair; Webb
Journal of Medicinal Chemistry, 1977 , vol. 20, # 9 p. 1206 - 1210 Title/Abstract Full Text Show Details
MED
=
2.59
mg/kg
Blair; Webb
Journal of Medicinal Chemistry, 1977 , vol. 20, # 9 p. 1206 - 1210 Title/Abstract Full Text Show Details
MED
=
2.59
mg/kg
Blair; Webb
Journal of Medicinal Chemistry, 1977 , vol. 20, # 9 p. 1206 - 1210 Title/Abstract Full Text Show Details
2.42
pIC50
2.42
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
8.66
pKi
8.664
Hadjipavlou-Litina; Garg, Rajni; Hansch, Corwin
Chemical Reviews, 2004 , vol. 104, # 9 p. 3751 - 3793 Title/Abstract Full Text View citing articles Show Details
2.42
pIC50
2.42
Chemical reviews, 1994 ,...
Title/Abstract Full Text Show Details
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
8.42
pIC50
8.42
Inhibitor
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Chemical reviews, 1994 ,...
Title/Abstract Full Text Show Details
Inhibitor
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Chemical reviews, 1994 ,...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
brain cell
= 40 µm
European journal of medi...
Title/Abstract Full Text Show Details
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
European journal of medi...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [Rattus norvegicus]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [Rattus norvegicus]:Wild
European journal of medi...
Title/Abstract Full Text Show Details
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
brain cell
European journal of medi...
Title/Abstract Full Text Show Details
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
8.42
pIC50
8.42
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
=
2.59
mM/kg
Lukovits
Journal of Medicinal Chemistry, 1983 , vol. 26, # 8 p. 1104 - 1109 Title/Abstract Full Text Show Details
=
2.59
mM/kg
Lukovits
Journal of Medicinal Chemistry, 1983 , vol. 26, # 8 p. 1104 - 1109 Title/Abstract Full Text Show Details
8.3
IC50
=
0.005
µM
Inhibitor
G Trapani; M Franco; A Latrofa; G Genchi; G Liso
European journal of medicinal chemistry, 1992 , vol. 27, p. 39 - 44 Title/Abstract Full Text Show Details
8.3
IC50
=
5
nM
Radioligand (/ligand)
G Trapani; M Franco; A Latrofa; G Genchi; G Liso
European journal of medicinal chemistry, 1992 , vol. 27, p. 39 - 44 Title/Abstract Full Text Show Details
Ratio
1.41
G Trapani; M Franco; A Latrofa; G Genchi; G Liso
European journal of medicinal chemistry, 1992 , vol. 27, p. 39 - 44 Title/Abstract Full Text Show Details
Ratio
1.41
G Trapani; M Franco; A Latrofa; G Genchi; G Liso
European journal of medicinal chemistry, 1992 , vol. 27, p. 39 - 44
Title/Abstract Full Text Show Details
Binding Score
@
Radioligand (/ligand)
Glucocorticoid receptor:Wild
ChemMedChem, 2009 , vol...
Title/Abstract Full Text View citing articles Show Details
Spreafico, Morena; Ernst, Beat; Lill, Markus A.; Smiesko, Martin; Vedani, Angelo
ChemMedChem, 2009 , vol. 4, # 1 p. 100 - 109 Title/Abstract Full Text View citing articles Show Details
8.42
IC50
=
3.8
nM
Inhibitor
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
European journal of medi...
Title/Abstract Full Text Show Details
oocyte
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
W Zhang; R Liu; Q Huang; P Zhang; KF Koehler; B Harris; P Skolnick; JM Cook
European journal of medicinal chemistry, 1995 , vol. 30, p. 483 - 496 Title/Abstract Full Text Show Details
%
=
234
%
Modulator
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Werner; Swihart; Rau; Jia; Borghese; McCracken; Iyer; Fanselow; Oh; Sonner; Eger II; Harrison; Harris; Homanics
Journal of Pharmacology and Experimental Therapeutics, 2011 , vol. 336, # 1 p. 134 - 144 Title/Abstract Full Text View citing articles Show Details
%
=
200
%
Modulator
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
oocyte
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Werner; Swihart; Rau; Jia; Borghese; McCracken; Iyer; Fanselow; Oh; Sonner; Eger II; Harrison; Harris; Homanics
Journal of Pharmacology and Experimental Therapeutics, 2011 , vol. 336, # 1 p. 134 - 144 Title/Abstract Full Text View citing articles Show Details
pKm
-2.1892
Cytochrome P450 3A4 [human]:Wild
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Wang, Yong-Hua; Li, Yan; Li, Yan-Hong; Yang, Sheng-Li; Yang, Ling
Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 18 p. 4076 - 4084 Title/Abstract Full Text View citing articles Show Details
Activity
6.5
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
8.82
IC50
=
1.5
nM
Radioligand (/ligand)
Francis; Cash; Barbaz; Bernard; Lovell; Mazzenga; Friedmann; Hyun; Braunwalder; Loo; Bennett
Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 281 - 290 Title/Abstract Full Text Show Details
8.82
IC50
=
1.5
nM
Radioligand (/ligand)
Peripheral-type benzodiazepine receptor-associated protein 1 [Rattus norvegicus]:Wild
brain
Francis; Cash; Barbaz; Bernard; Lovell; Mazzenga; Friedmann; Hyun; Braunwalder; Loo; Bennett
Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 281 - 290 Title/Abstract Full Text Show Details
Activity
5.8
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
Dihydropteridine reductase [Escherichia coli]:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
Activity
5.5
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
Activity
5.5
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
Activity
6.5
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
Activity
5.8
Aoyama; Suzuki; Ichikawa
Journal of Medicinal Chemistry, 1990 , vol. 33, # 9 p. 2583 - 2590 Title/Abstract Full Text Show Details
kcat
=
7150
min-1
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
Vmax
=
5960.01
µM/min
Dihydropteridine reductase [Escherichia coli]:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
4.63
Km
=
23.17
µM
Dihydropteridine reductase [Escherichia coli]:Wild
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
8.28
Ki
=
5.3
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Sf9
= 10 µm
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Harris, Danni; Clayton, Terry; Cook, James; Sahbaie, Peyman; Halliwell, Robert F.; Furtmueller, Roman; Huck, Sigismund; Sieghart, Werner; DeLorey, Timothy M.
Journal of Medicinal Chemistry, 2008 , vol. 51, # 13 p. 3788 - 3803 Title/Abstract Full Text View citing articles Show Details
Ratio
1.68
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
delta [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
Anzini, Maurizio; Braile, Carlo; Valenti, Salvatore; Cappelli, Andrea; Vomero, Salvatore; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Norcini, Monica; Makovec, Francesco; Giorgi, Gianluca; Fryer, R. Ian
Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4730 - 4743 Title/Abstract Full Text View citing articles Show Details
8.19
Ki
=
6.5
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Anzini, Maurizio; Braile, Carlo; Valenti, Salvatore; Cappelli, Andrea; Vomero, Salvatore; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Norcini, Monica; Makovec, Francesco; Giorgi, Gianluca; Fryer, R. Ian
Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4730 - 4743 Title/Abstract Full Text View citing articles Show Details
8.29
Ki
=
5.17
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Anzini, Maurizio; Braile, Carlo; Valenti, Salvatore; Cappelli, Andrea; Vomero, Salvatore; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Norcini, Monica; Makovec, Francesco; Giorgi, Gianluca; Fryer, R. Ian
Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4730 - 4743 Title/Abstract Full Text View citing articles Show Details
Ratio
1.6
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Anzini, Maurizio; Braile, Carlo; Valenti, Salvatore; Cappelli, Andrea; Vomero, Salvatore; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Norcini, Monica; Makovec, Francesco; Giorgi, Gianluca; Fryer, R. Ian
Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4730 - 4743 Title/Abstract Full Text View citing articles Show Details
8.35
Kd
=
4.5
nM
Gamma-aminobutyric acid receptor subunit delta:Wild + Gammaaminobutyric acid receptor subunit beta2:Wild + Gammaaminobutyric acid receptor subunit alpha1:Wild
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Harris, Danni; Clayton, Terry; Cook, James; Sahbaie, Peyman; Halliwell, Robert F.; Furtmueller, Roman; Huck, Sigismund; Sieghart, Werner; DeLorey, Timothy M.
Journal of Medicinal Chemistry, 2008 , vol. 51, # 13 p. 3788 - 3803 Title/Abstract Full Text View citing articles Show Details
Dose
=
2
mg
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
William J. Houlihan; Gregory B. Bennett
Annual reports in medicinal chemistry, 1978 , vol. 13, p. 21 - 30 Title/Abstract Full Text Show Details
Dose
=
2
mg
Title/Abstract Full Text Show Details
Joel G. Berger; Louis C. Iorio
Annual reports in medicinal chemistry, 1979 , vol. 14, # 19 p. 22 - 30 Title/Abstract Full Text Show Details
Dose
=
1
mg
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
William J. Houlihan; Gregory B. Bennett
Annual reports in medicinal chemistry, 1978 , vol. 13, p. 21 - 30 Title/Abstract Full Text Show Details
Activity
ND
Charles L. Zirkle; Carl Kaiser
Annual reports in medicinal chemistry, 1972 , vol. 7, p. 6 - 17 Title/Abstract Full Text Show Details
Activity
ND
R. Ian Fryer
Annual reports in medicinal chemistry, 1970 , vol. 6, p. 1 - 14 Title/Abstract Full Text Show Details
Activity
2.5
Radioligand (/ligand)
Leslie J. Browne; Kenneth J. Shaw
Annual reports in medicinal chemistry, 1991 , vol. 26, p. 1 - 10 Title/Abstract Full Text Show Details
Activity
ND
R. Ian Fryer
Annual reports in medicinal chemistry, 1970 , vol. 6, p. 1 - 14 Title/Abstract Full Text Show Details
Dose
=
2.5
mg
William J. Houlihan; Gregory B. Bennett
Annual reports in medicinal chemistry, 1977 , vol. 12, p. 10 - 19 Title/Abstract Full Text Show Details
Activity
ND
R. Ian Fryer
Annual reports in medicinal chemistry, 1970 , vol. 6, p. 1 - 14 Title/Abstract Full Text Show Details
Activity
ND
R. Ian Fryer
Annual reports in medicinal chemistry, 1970 , vol. 6, p. 1 - 14 Title/Abstract Full Text Show Details
Activity
1.4
Radioligand (/ligand)
Leslie J. Browne; Kenneth J. Shaw
Annual reports in medicinal chemistry, 1991 , vol. 26, p. 1 - 10 Title/Abstract Full Text Show Details
Dose
=
2
mg
Joel G. Berger; Louis C. Iorio
Annual reports in medicinal chemistry, 1979 , vol. 14, # 19 p. 22 - 30
Title/Abstract Full Text Show Details
Activity
ND
Annual reports in medici...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Translocator protein:Wild
Annual reports in medici...
Title/Abstract Full Text Show Details
Gamma-aminobutyric acid receptor subunit delta [taurine cattle]:Wild + Gammaaminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Annual reports in medici...
Title/Abstract Full Text Show Details
Peripheral-type benzodiazepine
Annual reports in medici...
Title/Abstract Full Text Show Details
A.D. Rudzik; W. Friis
Annual reports in medicinal chemistry, 1972 , vol. 7, p. 39 - 46 Title/Abstract Full Text Show Details
Activity
ND
Radioligand (/ligand)
Joseph P.Yevich; James S. New; Michael S. Eison
Annual reports in medicinal chemistry, 1984 , vol. 19, p. 11 - 20 Title/Abstract Full Text Show Details
Activity
ND
Marvin Cohen
Annual reports in medicinal chemistry, 1976 , vol. 11, p. 13 - 22 Title/Abstract Full Text Show Details
Activity
234
Radioligand (/ligand)
Leslie J. Browne; Kenneth J. Shaw
Annual reports in medicinal chemistry, 1991 , vol. 26, p. 1 - 10 Title/Abstract Full Text Show Details
1
Activity
NA
Radioligand (/ligand)
Joseph P.Yevich; James S. New; Michael S. Eison
Annual reports in medicinal chemistry, 1984 , vol. 19, p. 11 - 20 Title/Abstract Full Text Show Details
Activity
ND
Charles L. Zirkle; Carl Kaiser
Annual reports in medicinal chemistry, 1972 , vol. 7, p. 6 - 17 Title/Abstract Full Text Show Details
Activity
ND
Marvin Cohen
Annual reports in medicinal chemistry, 1976 , vol. 11, p. 13 - 22 Title/Abstract Full Text Show Details
Dose
=
1
mg
William J. Houlihan; Gregory B. Bennett
Annual reports in medicinal chemistry, 1978 , vol. 13, p. 21 - 30 Title/Abstract Full Text Show Details
Activity
@
Radioligand (/ligand)
receptor-associated protein 1:Wild
Joseph P. Yevich; James S. New; Michael S. Eison
Annual reports in medicinal chemistry, 1983 , vol. 18, p. 11 - 20 Title/Abstract Full Text Show Details
1
% Inhibition
NA
Arylacetamide deacetylase [human]:Wild
Sf21 cell line
Enzymology inhibition
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Shimizu, Mai; Fukami, Tatsuki; Nakajima, Miki; Yokoi, Tsuyoshi
Drug Metabolism and Disposition, 2014 , vol. 42, # 7 p. 1103 - 1109 Title/Abstract Full Text View citing articles Show Details
5
% increase
Active
THP-1 cell line
10 μM
Patent: WO2015/25180 A...
Title/Abstract Full Text Show Details
THP-1 cell line
10 μM
Patent: WO2015/25180 A...
Title/Abstract Full Text Show Details
Solute carrier family 22 member 5 [human]:Wild
HEK293 cell line
200 μM
PLoS ONE, 2015 , vol. 1...
Title/Abstract Full Text View citing articles Show Details
GLASGOW CALEDONIAN UNIVERSITY; GRAHAM, Annette
Patent: WO2015/25180 A1, 2015 ; Title/Abstract Full Text Show Details
5
% increase
Active
GLASGOW CALEDONIAN UNIVERSITY; GRAHAM, Annette
Patent: WO2015/25180 A1, 2015 ; Title/Abstract Full Text Show Details
3.83
% Inhibition
57.5
%
Inhibitor
Hacker, Kristina; Maas, Renke; Kornhuber, Johannes; Fromm, Martin F.; Zolk, Oliver
PLoS ONE, 2015 , vol. 10, # 9 art. no. E0136451 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
5.1
%
Inhibitor
Solute carrier family 22 member 5 [human]:Wild
HEK293 cell line
20 μM
PLoS ONE, 2015 , vol. 1...
Title/Abstract Full Text View citing articles Show Details
Hacker, Kristina; Maas, Renke; Kornhuber, Johannes; Fromm, Martin F.; Zolk, Oliver
PLoS ONE, 2015 , vol. 10, # 9 art. no. E0136451 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
14
%
Inhibitor
UDPglucuronosyltransferase 1-8:Wild
20 μM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki
Drug Metabolism and Disposition, 2015 , vol. 43, # 6 p. 812 - 818 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
19
%
Inhibitor
UDPglucuronosyltransferase 1-8:Wild
20 μM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki
Drug Metabolism and Disposition, 2015 , vol. 43, # 6 p. 812 - 818 Title/Abstract Full Text View citing articles Show Details
4.33
% Inhibition
30
%
Inhibitor
UDPglucuronosyltransferase 1-8:Wild
20 μM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Oda, Shingo; Fujiwara, Ryoichi; Kutsuno, Yuki; Fukami, Tatsuki; Itoh, Tomoo; Yokoi, Tsuyoshi; Nakajima, Miki
Drug Metabolism and Disposition, 2015 , vol. 43, # 6 p. 812 - 818 Title/Abstract Full Text View citing articles Show Details
8.6
Ki
=
2.5
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gammaaminobutyric acid receptor subunit alpha-
binding activity
Patent: US6426343 B1, ...
Title/Abstract Full Text Show Details
2:Wild Gerard Raphael Dawson
Patent: US6426343 B1, 2002 ; Title/Abstract Full Text Show Details
8.32
Ki
=
4.8
nM
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gammaaminobutyric acid receptor subunit alpha3:Wild
binding activity
Patent: US6426343 B1, ...
Title/Abstract Full Text Show Details
Gerard Raphael Dawson
Patent: US6426343 B1, 2002 ; Title/Abstract Full Text Show Details
pX
Parameter
Value (qual)
Value (quant)
Unit
8.28
Ki
=
5.2
nM
Action on Target
Target
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all)
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
binding activity
Patent: US6426343 B1, ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gamma-aminobutyric acid receptor subunit alpha-5:Wild
binding activity
Patent: US6426343 B1, ...
Title/Abstract Full Text Show Details
Radioligand (/ligand)
Gamma-aminobutyric acid receptor subunit gamma-2:Wild + Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gamma-aminobutyric acid receptor subunit alpha-6:Wild
binding activity
Patent: US6426343 B1, ...
Title/Abstract Full Text Show Details
Inhibitor
Protein kinase C epsilon type:Wild
inhibitory activity
Patent: WO2016/3450 A1...
Title/Abstract Full Text Show Details
Gerard Raphael Dawson
Patent: US6426343 B1, 2002 ; Title/Abstract Full Text Show Details
8.68
Ki
=
2.11
nM
Gerard Raphael Dawson
Patent: US6426343 B1, 2002 ; Title/Abstract Full Text Show Details
8
Ki
>
10
nM
Gerard Raphael Dawson
Patent: US6426343 B1, 2002 ; Title/Abstract Full Text Show Details
6.82
EC50
=
150
nM
HEK293 cell line
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; MESSING, Robert Owen; PLEISS, Michael A.; LEVINE, Jon A.
Patent: WO2016/3450 A1, 2016 ; Title/Abstract Full Text Show Details
1
Ki
>
10000
nM
Radioligand (/ligand)
Translocator protein:Wild
C6
Bioorganic and Medicinal...
Title/Abstract Full Text View citing articles Show Details
Li, Jun; Schulte, Michael L.; Nickels, Michael L.; Manning, H. Charles
Bioorganic and Medicinal Chemistry Letters, 2016 , vol. 26, # 15 p. 3472 - 3477 Title/Abstract Full Text View citing articles Show Details
% Efficacy
17
%
cerebellum
granule cell
0.1
Journal of Molecular Neu...
μM
Title/Abstract Full Text View citing articles Show Details
Gatta, Elena; Cupello, Aroldo; Di Braccio, Mario; Grossi, Giancarlo; Robello, Mauro; Scicchitano, Francesca; Russo, Emilio; De Sarro, Giovambattista
Journal of Molecular Neuroscience, 2016 , vol. 60, # 4 p. 539 - 547 Title/Abstract Full Text View citing articles Show Details
% Increase
Active
Agonist
GABA-A receptor [Sprague Dawley rat]:Wild
brain
Synaptosomal cell
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cappelli, Andrea; Anzini, Maurizio; Castriconi, Federica; Grisci, Giorgio; Paolino, Marco; Braile, Carlo; Valenti, Salvatore; Giuliani, Germano; Vomero, Salvatore; Di Capua, Angela; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Frosini, Maria; Ricci, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2016 , vol. 59, # 7 p. 3353 - 3372 Title/Abstract Full Text View citing articles Show Details
8.28
Ki
5.2
nM
Inhibitor
GABA-A receptor [taurine cattle]:Wild
brain cortex
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cappelli, Andrea; Anzini, Maurizio; Castriconi, Federica; Grisci, Giorgio; Paolino, Marco; Braile, Carlo; Valenti, Salvatore; Giuliani, Germano; Vomero, Salvatore; Di Capua, Angela; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Frosini, Maria; Ricci, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2016 , vol. 59, # 7 p. 3353 - 3372 Title/Abstract Full Text View citing articles Show Details
8.19
Ki
6.4
nM
Inhibitor
GABA-A receptor [human]:Wild
brain cortex
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Cappelli, Andrea; Anzini, Maurizio; Castriconi, Federica; Grisci, Giorgio; Paolino, Marco; Braile, Carlo; Valenti, Salvatore; Giuliani, Germano; Vomero, Salvatore; Di Capua, Angela; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Frosini, Maria; Ricci, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2016 , vol. 59, # 7 p. 3353 - 3372 Title/Abstract Full Text View citing articles Show Details
Qualitative Information 1 of 99
2 of 99
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Biological material
Xenopus laevis oocyte
Assay Description
Effect : chloride channel modulator Bioassay : I recorded with two-electrode voltage-clamp (-60 mV; 20 deg C); title comp. effect on GABA-induced I studied cells injected with cRNA of wild-type Drosophila melanogaster GABA-receptor RDL subunit; perfused with saline; membrane currents (I) induced by 10μM GABA; title comp. added to perfusate
Citation
Hosie, Alastair M.; Sattelle, David B.
British Journal of Pharmacology, 1996 , vol. 117, # 6 p. 1229 - 1237 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : ion transport Target : brain from Sprague-Dawley rat Bioassay : (36)Cl(-) uptake determined by radioactivity measurement; title comp. effect on M-induced (36)Cl(-) uptake in Co, Ce for NO and SE rats studied adult male rats (12 h light/dark cycle; normal <NO> or in pilocarpin-induced status epilepticus <SE>) sacrificed; cortical (Co) and cerebellar (Ce) synaptoneurosomes prep.; incub. with title comp.+(36)Cl(-)+muscimol (M) in assay buffer (34 deg C; 5 min)
Results
ca. 10 percent increase of stimulated (36)Cl(-) influx; similar for Co, Ce in NO, SE
Citation
Banerjee, Pradeep K.; Olsen, Richard W.; Snead III, O. Carter
Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 291, # 1 p. 361 - 366 Title/Abstract Full Text View citing articles Show Details
Results
central nervous system depressant, action verified by recording the bioelectrical activity of the precentral cortex (in rabbits)
Citation
Stumpf Ch.; Viernstein
Journal of Pharmaceutical Sciences, 1990 , vol. 79, # 12 p. 1062 - 1064 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : Sprague-Dawley rat cortical synaptoneurosomes Bioassay : radioactivity quantitation using liquid scintillation spectrometry rats (4-5 wk); purified cerebrocortical membranes were incubated with 5 nmol/l <35S>-TBPS in the presence of title comp. at 22
deg C for 90 min
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9 of 99
10 of 99
Results
title comp. exhibited biphasic effect on <35S>-TBPS binding to cortical synaptoneurosomes: at conc. < 1 μmol/l - increased and at conc. > 1 μmol/l - inhibited (diagram)
Citation
Masonis; McCarthy
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 1 p. 186 - 193 Title/Abstract Full Text Show Details
Results
reduction of the increase of HVA induced by chlorpromazine (male mice, 1 mg/kg, i.p.)
Citation
Pieri; Schaffner; Scherschlicht; Polc; Sepinwall; Davidson; Moehler; Cumin; Da Prada; Burkard; Keller; Mueller; Gerold; Cook; Haefely
Arzneimittel-Forschung/Drug Research, 1981 , vol. 31, # 12 a p. 2180 - 2201 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |pharmacokinetics Target : human liver microsomes Bioassay : CLint: intrinsic clearance CLint determined for both oxidative pathways and summed to give CLint
Results
CLint: 5.9 μL/min/mg protein
Citation
Hakooz, Nancy; Ito, Kiyomi; Rawden, Helen; Gill, Helen; Lemmers, Lynn; Boobis, Alan R.; Edwards, Robert J.; Carlile, David J.; Lake, Brian G.; Houston, J. Brian
Pharmaceutical Research, 2006 , vol. 23, # 3 p. 533 - 539 Title/Abstract Full Text View citing articles Show Details
Target
endothelin receptor [human]:Wild
Assay Description
Effect : |receptor blocking agent Bioassay : SPA=scintillation proximity assay in vitro; SPA kit with endothelin preparation from human placental membrane was used; binding of 125I-endothelin (2,000 Ci/mmol) measured
Citation
Raffa, Robert B.; Schupsky, James J.; Lee, David K. H.; Jacoby, Henry I.
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 1 - 7 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : Wistar rat brain sections Bioassay : number of brain areas from mesencephalon, cerebral cortex, hippocampus, and cerebellum; Tris-HCl, pH 7.4; 4 deg C; incubated for 40 min; characterization of BZ2 carried out directly by coincubation with 1 μmol/l zolpidem (specifically binds to BZ1) in vitro; autoradiographical saturation kinetic study of overall benzodiazepine (BZ) binding sites as well as of benzodiazepine binding site subtype 1 (BZ1) and subtype 2 (BZ2); <3H>labelled title comp.
Results
KD, equilibrium association constant KDs as well as receptor densities Bmax (32-328 fmol/mg protein) for several brain areas presented; statistically significant differences in affinities of BZ2 with respect to BZ and BZ1 binding sites were mainly found in cortical 1.1 - 4.8 nmol/l
Citation
Soria, Carlos; Revilla, Victoria; Candelas, Maria Adoracion; Calvo, Pedro; Fernandez-Lopez, Arsenio
Biochemical Pharmacology, 1995 , vol. 50, # 10 p. 1619 - 1625 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : Trachemys scripta, freshwater turtle Bioassay : turtles (0.75-1.3 kg) subjected to a 100 percent N2 atmosphere for up to 24 h; after exposure, cerebral cortex dissected out, and saturation binding assay for GABA/benzodiazepine receptors performed using <3H>labelled title comp.
Results
no signif. change in dissociation constant over 24 h of anoxia; signif. increase in receptor density after 12 h of anoxia
Citation
Lutz; Leone-Kabler
American Journal of Physiology - Regulatory Integrative and Comparative Physiology, 1995 , vol. 268, # 5 37-5 p. R1332-R1335 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus granule cell
Assay Description
Effect : effect on extracellular acidification rate
Bioassay : 30 min washout to remove GABA, followed by 30 min exposure to title comp.; 15 min washout performed between each GABA concentration; measurement of CGC extracellular acidification rate in cytosensor microphysiometer primary CGC prepared from 8-day-post-natal rats; cells (9-12E5 cells/transwell cup) at 8 days in vitro assessed for response to increasing concentrations of GABA (0.010-1000 μmol/l, 25 deg C, 33 s stimulation) in presence of title comp.
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Results
title comp. significantly potentiated GABA-stimulated increase in the extracellular acidification rate at low GABA concentration (0.010-1 μmol/l); graphical representation; title comp. had no effect in the absence of GABA
Citation
Brown, Maria J.; Wood, Martyn D.; Coldwell, Martyn C.; Bristow, David R.
British Journal of Pharmacology, 1997 , vol. 121, # 1 p. 71 - 76 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : binding affinity; inhibition of Target : rat brain cortex membranes Bioassay : ref.: rolipram (IC50: 0.058 μmol/l) membranes treated with <3H>-rolipram; title comp. added; displacement of <3H>-rolipram by title comp. determined by binding assay
Results
percent inhibition of binding affinity by title comp. was 14.7 percent; table
Citation
Collado, M. Carmen; Beleta, Jorge; Martinez, Ester; Miralpeix, Montse; Domenech, Teresa; Palacios, Jose Maria; Hernandez, Jesus
British Journal of Pharmacology, 1998 , vol. 123, # 6 p. 1047 - 1054 Title/Abstract Full Text View citing articles Show Details
Target
cGMP-specific 3',5'-cGMP phosphodiesterase 3:Wild
Biological material
guinea pig
Assay Description
Effect : |enzyme; inhib. of Bioassay : control: vehicle; ref.: rolipram (IC50: 242 μmol/l) enzyme treated with title comp.; cyclic nucleotide phosphodiesterase activities measured by phosphodiesterase assay
Results
percent inhibition of enzyme by title comp. was 35 percent; table
Citation
Collado, M. Carmen; Beleta, Jorge; Martinez, Ester; Miralpeix, Montse; Domenech, Teresa; Palacios, Jose Maria; Hernandez, Jesus
British Journal of Pharmacology, 1998 , vol. 123, # 6 p. 1047 - 1054 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : brain membranes from bovine brain Bioassay : membranes prepared from cerebral cortex or cerebellum by known method; radioligand labelling; binding place determined after hydroxylamine cleavage
Results
photoaffinity labelling in receptor population occurs within residues 1-103 of the α1 sequence
Citation
Duncalfe; Dunn
European Journal of Pharmacology, 1996 , vol. 298, # 3 p. 313 - 319 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cerebral cortical neurones from 15-d-old fetus of ddY mouse Bioassay : neurones cultured with 1 μM β-CCE at 37 deg C for 12 h or not (control); the extensively washed membrane fractions from neurones then incubated with various concns. of (3H)-title comp. at 2 deg C for 60 min; Scatchard analysis neopallium free of meninges dissected from a 15-day-old fetus, minced, trypsinized and centrifuged, cultured at 37 deg C for 3 ds; <95 percent of the cells confirmed to be neurons by immunohistochemical approch
Results
high affinity binding site for (3H)-title comp. Bmax 1.51 pmol/mg protein (absence of β-CCE); Bmax 1.06 pmol/mg protein (presence of β-CCE) decrease after 3 h exposure to β-CCE; Kd 12.0 nM (control) 11.2
Citation
Katsura, Masashi; Ohkuma, Seitaro; Jun, Xu; Kuriyama, Kinya
European Journal of Pharmacology, 1996 , vol. 298, # 1 p. 71 - 77 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : modulation of GABA currents Target : Xenopus laevis oocytes injected with α1β1γ2s Bioassay : adult Xenopus laevis stage V and VI oocytes nuclei inj. with recombinant human GABAA receptors; title compound effect examined using two-electrode voltage-clamp method; on control GABA EC20 responses with a preapplication time of 30 sec
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Results
ca. 125 percent modulation of control GABA EC20 (fig. given)
Citation
Wafford; Thompson; Thomas; Sikela; Wilcox; Whiting
Molecular Pharmacology, 1996 , vol. 50, # 3 p. 670 - 678 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : modulation of GABA currents Target : Xenopus laevis oocytes injected with α4β1γ2s Bioassay : adult Xenopus laevis stage V and VI oocytes nuclei inj. with recombinant human GABAA receptors; title compound effect examined using two-electrode voltage-clamp method; on control GABA EC20 responses with a preapplication time of 30 sec
Citation
Wafford; Thompson; Thomas; Sikela; Wilcox; Whiting
Molecular Pharmacology, 1996 , vol. 50, # 3 p. 670 - 678 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : modulation of GABA currents Target : Xenopus laevis oocytes injected with α6β1γ2s Bioassay : adult Xenopus laevis stage V and VI oocytes nuclei inj. with recombinant human GABAA receptors; title compound effect examined using two-electrode voltage-clamp method; on control GABA EC20 responses with a preapplication time of 30 sec
Citation
Wafford; Thompson; Thomas; Sikela; Wilcox; Whiting
Molecular Pharmacology, 1996 , vol. 50, # 3 p. 670 - 678 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |metabolic Target : Harlan Spraque-Dawley rat Bioassay : coronal sections of the freezed brain, thickness 12 μ; incubation with 1nM 3H radiolabelled flunitrazepam for various time and temperatures (4 and 22 Celsius degrees); the sections were then exposed for 2 weeks
Results
incubation 90 min in -4 Celsius degrees: the best results; in pentobarbital-tolerant rats: the activity observed in most regions of the brain; in pentobarbital-dependent rats: the binding sites increased in relatively large number of brain regions
Citation
Suzuki, Toshihito; Ito, Takehiko; Wellman, Susan E.; Ho, Ing Kang
European Journal of Pharmacology, 1996 , vol. 295, # 2-3 p. 169 - 179 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cerebellar membranes from Sprague-Dawley rats Bioassay : membrane homogenates of cerebellum from rats prepared according to Endo and Olsen (J.Neurochem. 59,1444 (1993)); supernatant or pellet suspension incubated with ligand; radioligand assay
Results
binding activities of immunoprecipitates in Fig.
Citation
Huh, Kyung-Hye; Endo, Shuichi; Olsen, Richard W.
European Journal of Pharmacology, 1996 , vol. 310, # 2-3 p. 225 - 233 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |agonist Target : Sprague-Dawley rat cortical wedge Bioassay : further study: influence of ethanol and Ro 15-1788 on title comp. effect; GABA: γ-aminobutyric acid wedges were superfused for 20 min with superfusion buffer containing title comp.; GABA/gaboxadol EC20 applied with title comp.; number of spikes during last 12 min counted; relative frequency calculated
Results
% potentiation of GABA/gaboxadol EC20 response by title comp. were 18.6/60, resp.; ethanol not potentiated GABA/gaboxadol EC20 response; Ro 15-1788 partially antagonised title comp. effect for GABA, completely abolished for gaboxadol EC20; fig., table
Citation
Storustovu, Signe i; Ebert, Bjarke
European Journal of Pharmacology, 2003 , vol. 467, # 1-3 p. 49 - 56 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |agonist Target : Xenopus laevis oocytes expressing human GABA receptors
A
Bioassay : test system comprising GABAA (γ-aminobutyric acid type A) receptors are composed of Α1β3Γ2S subunits; further study: influence of ethanol and Ro 15-1788 on title comp. effect oocytes superfused with solution containing title comp.; after 60 s, gaboxadol EC20 and title comp. were co-applied; potentiation of gaboxadol EC20 responses by title comp. was investigated
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27 of 99
Results
title comp. potentiated gaboxadol EC20 responses by 124%; ethanol was not able to bring further potentiation for title comp.; Ro 15-1788 increased gaboxadol EC20 response by 10%; fig.
Citation
Storustovu, Signe i; Ebert, Bjarke
European Journal of Pharmacology, 2003 , vol. 467, # 1-3 p. 49 - 56 Title/Abstract Full Text View citing articles Show Details
Results
ligand affinities for calmodulin and tropinon C and effect on calmodulin dependent stimulation of cyclic nucleotide phosphodiesterase
Citation
Tkachuk; Baldenkov; Feoktistov; Men'shikov; Quast; Herzig
Arzneimittel-Forschung/Drug Research, 1987 , vol. 37, # 9 p. 1013 - 1017 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : receptor photoaffinity labeling Target : R-3327 Dunning prostatic tumor Bioassay : tumor sublines AT-1, H, G; mitochondrial and microsomal fractions; peripheral benzodiazepine receptor; <N-methyl-3H>title comp.; preincubation (dark, 15 min); 60 min. UV irradiation; 10 μmol/l of unlabeled title comp.; electrophoresis
Citation
Alenfall, Jan; Batra, Satish
Biochemical Pharmacology, 1996 , vol. 51, # 8 p. 1009 - 1013 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : GABAA receptors, recombinant, cloned on HEK 293 cells Bioassay : HEK: human embryonic kidney cells transfected with cDNAs for α1-, β3-, γ2 subunits of GABAA receptors and their combinations; incubated in Tris-citrate buffer, 90 min, 4 deg C, with <3H>labeled title comp.; non-specific binding in pres. diazepam; scintillation
Results
high affinity binding only to membranes from cells transfected with α1γ2- and α1β3γ2-subunits, low affinity binding also to non-transfected cells; diagram
Citation
Zezula; Slany; Sieghart
European Journal of Pharmacology, 1996 , vol. 301, # 1-3 p. 207 - 214 Title/Abstract Full Text Show Details
Biological material
human HEK293-EBNA cell line
Assay Description
Effect : |receptor; binding activity Bioassay : filtered, filters were subjected to scintillation counting cells were cultured and transfected with cDNA encoding for α1, β3 or γ2 subunits of GABAA receptors, membranes extracted, frozen membranes thawed, centrifuged, incubated in buffer with 3H-radiolabeled title comp. at 4 degC for 90 min
Results
high affinity binding sites observed in membranes from cells cotransfected with α1, β3, and γ2 subunits while no binding sites were formed from cells transfected with these subunits
Citation
Slany; Zezula; Tretter; Sieghart
Molecular Pharmacology, 1995 , vol. 48, # 3 p. 385 - 391 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : Wistar rat cerebral synaptic membranes Bioassay : nonspecific binding determined by parallel incubations with 1E-5 M diazepam rat weighing 180-220 g; incubation of membrane preparations with <3H> labelled title comp. together with 1E-9 1E-3 M S-adenosyl-L-homocysteine, S-adenosylmethionine and 5'-methylthioadenosine, resp. for 1 h at 4 deg C; liquid scintillation
Results
inhibition of title comp. binding with Ki value of 7.9 μM and 15.8 μM, resp. by S-adenosylhomocysteine and 5'-methylthioadenosine; no effect of S-adenosylmethionine
Citation
Tsvetnitsky; Campbell; Gibbons
European Journal of Pharmacology, 1995 , vol. 282, # 1-3 p. 255 - 258 Title/Abstract Full Text Show Details
Assay Description
Effect : gaba-A, Benzodiazepine (Central) receptor binding
Target : Receptor source - bovine cortical membranes Bioassay : [00100] Experiment 6-Bioactivity of Infused Agents-Pharmacology Activity Test [00101] It was demonstrated that introduced drugs and drug-like agents can maintain their pharmacological activity during their residence in the biological materials. The following procedures were employed and the following
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Results
Flunitrazepam, a hypnotic, demonstrated specific binding in the benzodiazepine central assay
Citation
American Moxie LLC
Patent: US6660310 B2, 2003 ; Title/Abstract Full Text Show Details
Assay Description
Effect : |receptor; binding activity Target : embryos from 14-day-old C57B1/6CR mouse Bioassay : non specific binding was detn. in presence of 10 μM Ro15-1788 coverslips contg. cortical cultured neurons pretreated with pentobarbital (200 μM, 5-days), or not (control) removed from the tissue culture medium rinsed at room temp. in HEPES-buffered saline, incubated with (3H)title comp. for 30 min at 24 deg C
Results
specific binding: control 141 fmol/mg protein; in cells pretreated with 200 μM pentobarbital for 5 days 154 fmol/mg protein; chronic pretreatment with pentobarbital did not change basal title comp. binding to intact cortical neurons
Citation
Yu; Ticku
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 275, # 3 p. 1442 - 1446 Title/Abstract Full Text View citing articles Show Details
Biological material
Xenopus laevis oocyte
Assay Description
Effect : |receptor; binding activity Bioassay : oocytes expressing human α3, β1 and γ2L GABAA receptor subunits; effect of title comp. on pentobarbitone-, 5α-pregnan-3α-ol-20-one-, and propofol-evoked currents mediated by the recombinant receptors in vitro; oocytes voltage-clamped at -60 mV; two-electrode voltage-clamp mode; continuously superfused (7-10 ml/min) with frog Ringer soln.; title comp., pentobarbitone, 5αpregnan-3α-ol-20-one, and propofol applied by the superfusion system
Results
title comp. enhanced responses to pentobarbitone, propofol, and 5α-pregnan-3α-ol-20-one
Citation
Belelli, Delia; Callachan, Helen; Hill-Venning, Claire; Peters, John A.; Lambert, Jeremy J.
British Journal of Pharmacology, 1996 , vol. 118, # 3 p. 563 - 576 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cell membranes expressing human α1β3γ2 GABAA receptor Bioassay : membranes preincubated with 50 nmol/l des-methyl flunitrazepam for 30 min at 4 deg C and exposed to UV light (365 nm, 50-60 Hz, 200-220 V) for 1 h at 4 deg C; GABA: γ-aminobutyric acid; BZ: benzodiazepine binding of <3H>title comp. to BZ binding site of GABAA receptor after photoincorporation of des-methyl flunitrazepam studied by saturation assay; incubation for 30 min at 20 deg C; radioactivity measured by scintillation counting
Results
Bmax = 22.1 percent, Kd not detected (table)
Citation
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cell membranes expressing human α1β3γ2 GABAA receptor Bioassay : membranes preincubated with 50 nmol/l Ro 15-4513 (partial inverse agonist) for 30 min at 4 deg C and exposed to UV light (365 nm, 50-60 Hz, 200-220 V) for 1 h at 4 deg C; GABA: γaminobutyric acid; BZ: benzodiazepine binding of <3H>title comp. to BZ binding site of GABAA receptor before and after photoincorporation of Ro 15-4513 studied by saturation assay; incubation for 30 min at 20 deg C; radioactivity measured by scintillation
Results
binding of <3H>title comp. was reduced after photoincorporation of Ro 15-4513 by > 68 percent (Kd: 5.33 and 2.93 nmol/l, Bmax: 95.1 and 12.9 percent before and after photoincorporation, resp.) (figure, table)
Citation
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cell membranes expressing human α1β3γ2 GABAA receptor
Bioassay : membranes preincubated with 50 nmol/l title comp. for 30 min at 4 deg C and exposed to UV light (365 nm, 50-60 Hz, 200-220 V) for 1 h at 4 deg C; GABA: γ-aminobutyric acid; BZ: benzodiazepine affinity of title comp. to BZ binding site of GABAA receptor before and after photoincorporation of title comp. studied by competition assay using <3H>Ro 15-1788 as radioligand
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Results
Ki: 4.2 and 230.0 nmol/l before and after title comp. photoincorporation, resp. (table)
Citation
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cell membranes expressing human α1β3γ2 GABAA receptor Bioassay : membranes preincubated with 50 nmol/l title comp. for 30 min at 4 deg C and exposed to UV light (365 nm, 50-60 Hz, 200-220 V) for 1 h at 4 deg C; GABA: γ-aminobutyric acid; BZ: benzodiazepine binding of <3H>title comp. to BZ binding site of GABAA receptor before and after photoincorporation of title comp. studied in presence of GABA (1 mmol/l)
Results
binding of <3H>title comp. in presence of GABA: 156.3 percent before and no binding after title comp. photoincorporation resp. (table)
Citation
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : cell membranes expressing human α1β3γ2 GABAA receptor Bioassay : membranes preincubated with 50 nmol/l title comp. (full agonist) for 30 min at 4 deg C and exposed to UV light (365 nm, 50-60 Hz, 200-220 V) for 1 h at 4 deg C; GABA: γ-aminobutyric acid; BZ: benzodiazepine binding of <3H>title comp. to BZ binding site of GABAA receptor before and after photoincorporation of title comp. studied by saturation assay; incubation for 30 min at 20 deg C; radioactivity measured by scintillation counting
Results
binding of <3H>title comp. was reduced after photoincorporation of title comp. by 84.1 percent (Kd: 5.33 and 6.06 nmol/l, Bmax: 95.1 and 9.4 percent before and after photoincorporation, resp.) (figure, table)
Citation
McKernan, Ruth M.; Farrar, Sophie; Collins, Ian; Emms, Frances; Asuni, Ayodeji; Quirk, Kathleen; Broughton, Howard
Molecular Pharmacology, 1998 , vol. 54, # 1 p. 33 - 43 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor blocking agent Target : Xenopus laevis oocyte, transfected Bioassay : oocyte expressed GABAA receptors composed of α1, β2, γ1 subunits; GABA conc. (3-8 μmol/l) corresponded to conc. eliciting 5-10 percent of maximal current amplitude (EC5-10); control: sol. contained GABA without title comp. chamber with oocyte perfused with sol. contained GABA (3-8 μmol/l or 1 mmol/l) and title comp. by fast perfusion system; GABA-induced chloride currents (IGABA) measured by two-electrode voltage-clamp
Results
title comp. inhibited IGABA (11 percent at 1 μmol/l); at GABA conc. 1 mmol/l title comp. did not affect IGABA
Citation
Khom; Baburin; Timin; Hohaus; Sieghart; Hering
Molecular Pharmacology, 2006 , vol. 69, # 2 p. 640 - 649 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor blocking agent Target : Xenopus laevis oocyte, transfected Bioassay : oocyte expressed GABAA receptors composed of α1, β2 subunits; GABA conc. (3-8 μmol/l) corresponded to conc. eliciting 5-10 percent of maximal current amplitude (EC5-10); control: sol. contained GABA without title comp. chamber with oocyte perfused with sol. contained GABA (3-8 μmol/l) and title comp. by fast perfusion system; GABA-induced chloride currents (IGABA) measured by two-electrode voltage-clamp method at holding potential
Results
title comp. did not inhibit IGABA statistically significant (9 percent)
Citation
Khom; Baburin; Timin; Hohaus; Sieghart; Hering
Molecular Pharmacology, 2006 , vol. 69, # 2 p. 640 - 649 Title/Abstract Full Text View citing articles Show Details
Biological material
human
Assay Description
Effect : |drug dependence Bioassay : simple experimental epidemiologic survey of prescription forgeries in community pharmacies (1253 pharmacies) in the Midi-Pyrenees area (southwest France)
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Results
17 percent of the all forged prescription was made to obtain title compound
Citation
Lapeyre-Mestre; Damase-Michel; Adams; Michaud; Montastruc
European Journal of Clinical Pharmacology, 1997 , vol. 52, # 1 p. 37 - 39 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : receptor binding affinity Target : astrocytoma A172 cell membranes Bioassay : membrane fragments immobilized on IAM chromatographic phase
Results
molecular target: γ-aminobutyric acid receptor
Citation
Kitabatake; Moaddel; Cole; Gandhari; Frazier; Hartenstein; Rosenberg; Bernier; Wainer
Analytical Chemistry, 2008 , vol. 80, # 22 p. 8673 - 8680 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : receptor binding affinity Target : astrocytoma 1321N1 cell membranes of human Bioassay : membrane fragments immobilized on IAM chromatographic phase
Results
molecular target: γ-aminobutyric acid receptor
Citation
Kitabatake; Moaddel; Cole; Gandhari; Frazier; Hartenstein; Rosenberg; Bernier; Wainer
Analytical Chemistry, 2008 , vol. 80, # 22 p. 8673 - 8680 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : formula Ia metabolite formation; effect on Target : liver cytosol of human Bioassay : Inhibition Studies with AKR Competitors Inhibition studies were also conducted using some of the AKR competitors listed in Table 2.; Note that AKR1C2/3 inhibitor 5beta-cholanic acid 3alpha, 7-alpha-diol, a bile acid displayed IC50s of 0.21 um and 74.4 uM for AKR1C2 and AKR1C3, respectively, using tibolone
Results
title compound at 60&micro;M inhibited metabolism of 14C-radiolabelled compound of Formula Ia by 51%
Citation
Ghosal, Anima; Kishnani, Narendra S.; Alton, Kevin B.; White, Ronald E.
Patent: US2006/276404 A1, 2006 ; Title/Abstract Full Text Show Details
Target
Serum albumin [human]:Wild
Assay Description
Effect : human serum albumin; binding of Bioassay : TRANSIL&reg; technology
Results
LogHSA -3.046 no_unit
Citation
Bayer Technology Services GmbH
Patent: US2005/137807 A1, 2005 ; Title/Abstract Full Text Show Details
Results
inhibitory influence on respiration in anesthetized cats (chloralose/urethane and pentobarbital anesthesia), 0.005-3.325 mg/kg i.v. administration
Citation
Danneberg
Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 3 A p. 610 - 615 Title/Abstract Full Text View citing articles Show Details
Results
in vitro central nervous system receptors binding affinities: <3H>flunitrazepam (benzodiazepine receptor) pIC50= 8.30 in male rat cerebral cortices
Citation
Nicholls, Ian A.; Alewood, Paul F.; Brinkworth, Ross I.; Morrison, Stuart F.; Andrews, Peter R.
Journal of Chemical Research, Miniprint, 1993 , # 10 p. 2811 - 2826 Title/Abstract Full Text Show Details
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Results
effect of cumulative concentrations on peripheral neuromuscular function (in-vitro rat phrenic nerve-hemidiaphragm preparation)
Citation
Driessen; Vree; Booij; et al.
Journal of Pharmacy and Pharmacology, 1984 , vol. 36, # 4 p. 244 - 247 Title/Abstract Full Text View citing articles Show Details
Results
inhibition of specific 3H-flunitrazepam binding in in vitro preparations of rat cerebral cortex memranes at O deg C; IC50 3.0 nM
Citation
Dodd, Robert H.; Doisy, Xavier; Potier, Pierre; Potier, Marie-Claude; Rossier, Jean
Heterocycles, 1989 , vol. 28, # 2 p. 1101 - 1113 Title/Abstract Full Text View citing articles Show Details
Effect
Psychotropic
Assay Description
Effect : (3)H-flunitrazepam binding Target : Wistar rat synaptosomes Bioassay : amount of (3)H-flunitrazepam receptors (Bmax); dissociation constant (Kd) of ligand-receptor complex synaptosomes isol. from brain of male Wistar rats weighing 150-200 g; label. test comp.; in the pres. and abs. of TMD; 22 deg C; radioact. meas. on a Beat-1 liquid. scint. counter
Results
Bmax: 30.0-31.5 fM/mg protein in the pres. and abs. of TMD; Kd: 2.27-7.14 pM/mg protein in the pres. and abs. of TMD; IC50 of (3)H-imipramine in the pres. of TMD 0.53 mM
Citation
Stradomskii; Klimontova; Ryabukhin
Pharmaceutical Chemistry Journal, 1997 , vol. 31, # 1 p. 7 - 8 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |agonist Target : Xenopus laevis oocytes expressing human GABAA receptor Bioassay : GABA: γ-aminobutyric acid; 5α3α: 5α-pregnan-3α-ol-20-one electrical recordings made from oocytes expressing human α1β1γ2L GABAA receptors; oocytes voltage-clamped at -60 mV in twoelectrode voltage clamp mode; current induced by propofol, sodium pentobarbitone, 5α3α and trichloroethanol
Results
title comp. potentiated propofol-, pentobarbitone- and 5α3α-induced inward currents
Citation
Pistis, Marco; Belelli, Delia; Peters, John A.; Lambert, Jeremy J.
British Journal of Pharmacology, 1997 , vol. 122, # 8 p. 1707 - 1719 Title/Abstract Full Text View citing articles Show Details
Results
effect on human plasma protein binding of digoxin at 1 and 3 μg ml-1 (in-vitro)
Citation
Castillo Ferrando; Carrasco Prieto; De La Torre Brasas
Journal of Pharmacy and Pharmacology, 1983 , vol. 35, # 7 p. 462 - 463 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : Ltk- cells expressing human GABAA α6β3γ2 receptor
Bioassay : affinity measured by competition for <3H>Ro15-1788, incubation at 4 deg C in phosphate buffer (pH=7.4), radioactivity detected by liquid scintillation counting
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Results
not active up to a concentration of 1 μM
Citation
Huang, Qi; Zhang, Weijiang; Liu, Ruiyan; McKernan, Ruth M.; Cook, James M.
Medicinal Chemistry Research, 1996 , vol. 6, # 6 p. 384 - 391 Title/Abstract Full Text View citing articles Show Details
Results
parameters of binding to serum proteins at pH 7.4, obtained from the fluorescence method
Citation
Maruyama; Furuie; Hibino; Otagiri
Journal of Pharmaceutical Sciences, 1992 , vol. 81, # 1 p. 16 - 20 Title/Abstract Full Text View citing articles Show Details
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Biological material
Rattus norvegicus
Assay Description
Effect : |receptor; binding activity Bioassay : binding parameters (KD, nM; Bmax, fmol/mg protein) determined by Scatchard analysis membranes from cerebellum of adult rats incub. in buffer (pH 7.4; 90 min; 4 deg C) with <3H>labeled title comp. +/- 10 μM diazepam; binding determined with liquid scintillation
Results
KD: 2.8; Bmax: 1332
Citation
Slany; Zezula; Fuchs; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 2 p. 99 - 105 Title/Abstract Full Text View citing articles Show Details
Biological material
human HEK293 cell line
Assay Description
Effect : |receptor; binding activity Bioassay : binding parameters (KD, nM; Bmax, fmol/mg protein) determined by Scatchard analysis HEK cells, native or transfected with cDNAs for rat GABAA receptor α1β3γ2- or α1γ2-subunits incub. in buffer (pH 7.4; 90 min; 4 deg C) with <3H>labeled title comp. +/- 10 μM diazepam; binding determined with liquid scintillation
Results
increased binding in transfected cells (fmol/mg protein, native: 20; α1γ2: 46, KD: 10.9; Bmax: 240; α1β3γ2: 246, KD: 3.53; Bmax: 705)
Citation
Slany; Zezula; Fuchs; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 291, # 2 p. 99 - 105 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : PA3 cells Bioassay : effect on (GABA)A receptor function; Kd, Bmax, GABA shift cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 10 μM title comp. and 50 μM GABA
Results
Kd = 5.72 nM, Bmax = 141 percent of control, GABA shift: 1.35
Citation
Klein; Mascia; Harkness; Hadingham; Whiting; Harris
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1484 - 1492 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : PA3 cells Bioassay : effect on (GABA)A receptor subunit α1, β1 protein cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 100 μM title comp. and 50 μM GABA; Western blot analysis
Citation
Klein; Mascia; Harkness; Hadingham; Whiting; Harris
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1484 - 1492 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : PA3 cells Bioassay : effect on (GABA)A receptor subunit mRNAs: α1, β1, γ2L cells cultured in Dulbecco's modified Eagle's medium; induction with 1 μM dexamethasone; after 2 d 100 μM title comp. and 50 μM GABA; Northern blot analysis
Citation
Klein; Mascia; Harkness; Hadingham; Whiting; Harris
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 274, # 3 p. 1484 - 1492 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |receptor; binding activity Bioassay : elution front and plateau obtained binding on multiple-receptor stationary phase (MR-SP) studied; MR-SP prepared from homogenized brains and IAM-PC packing material; filled into
chromatographic coloumn; mobile phase: Tris*HCl pH 7.4 containing title comp.
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Results
dissociation constant on GABAA receptor determined by frontal chromatography: 1.3 nmol/l
Citation
Moaddel; Cloix; Ertem; Wainer
Pharmaceutical Research, 2002 , vol. 19, # 1 p. 104 - 107 Title/Abstract Full Text View citing articles Show Details
Results
free fraction (percent unbound = 22.5) of normal human plasma is concentration independent at conc. of the drug ranging from 10 to 10000 ng ml-1 (dialysis for 20 h at 37 deg C and pH 7.4)
Citation
Moschitto; Greenblatt
Journal of Pharmacy and Pharmacology, 1983 , vol. 35, # 3 p. 179 - 180 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : drug interaction Target : human GABAA receptors expressed in Xenopus oocytes Bioassay : oocytes placed in bath with modified Barth's medium and impaled with two 1-3 Mο containing 2M KCl; voltage-clamp; title comp. preapplied 30 s before GABA; concetration-response curves α6β2γ2S and α1β2γ2S receptors (α6 and α1); effect of title comp. on γ-aminobutyric acid (GABA) currents in oocytes
Results
title comp. potentiated effect of GABA in α1; no effect in α6
Citation
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : human GABAA receptors in human embryonic kidney 293 cells Bioassay : cells transiently transfected with α6β1γ2S receptors; affinities of title comp. determined by inhibition of <3H>Ro 15-4513 binding in membranes
Results
had a biphasic curve with low (IC50=380 nM) and high affinity (IC50=14 nM)
Citation
Hadingham, Karen L.; Garrett, Elizabeth M.; Wafford, Keith A.; Bain, Corinna; Heavens, Robert P.; Sirinathsinghji, Dalip J. S.; Whiting, Paul J.
Molecular Pharmacology, 1996 , vol. 49, # 2 p. 253 - 259 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : neural network activity; reduction of Target : hippocampal neuron culture of Sprague-Dawley rat Bioassay : 00235] Example 6 : Mg++ and GABAB Agonists Increase Synaptic Plasticiy on a Long Term Basis ; Various Other Agents that Reduce Ca++ Flux Increase Synaptic Plasticity on a Short Term Basis. [00236] We sought to assess the ability of various treatments to increase synaptic plasticity. In functional neural
Results
pre-treatment with title compound at 5 &micro;mol/l for 48 hours inhibited global neuronal network activity; but no effect on synaptic plasticity was observed (figures are given)
Citation
MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Patent: WO2005/37215 A2, 2005 ; Title/Abstract Full Text Show Details
Assay Description
Effect : plasticity of presynaptic terminals; enhancing of Target : hippocampal neuron culture of Sprague-Dawley rat Bioassay : 00235] Example 6 : Mg++ and GABAB Agonists Increase Synaptic Plasticiy on a Long Term Basis ; Various Other Agents that Reduce Ca++ Flux Increase Synaptic Plasticity on a Short Term Basis. [00236] We sought to assess the ability of various treatments to increase synaptic plasticity. In functional neural
Results
pre-treatment with title compound at 5 &micro;mol/l for 4-6 hours led to enhancing of inhibitory synaptic transmission and corresponding reduction in overall activity of neural network, resulting in formation of a highly plastic network (increase in
Citation
MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Patent: WO2005/37215 A2, 2005 ; Title/Abstract Full Text Show Details
Results
no effect on the response to GABA (field-stimulated guinea-pig vas deferens preparation; dose: 1E-5 M)
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Citation
Doble; Turnbull
Journal of Pharmacy and Pharmacology, 1981 , vol. 33, # 4 p. 267 - 268 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : drug interaction Bioassay : determination of I/Ic ( GABA-induced peak current in the presence of the drug/ control GABA-induced peak current); I/Imax (Imax: maximal current) in vitro; cells from 6-d-old Wistar rats; electrophysiological recording γ-aminobutyric acid (GABA)-induced membrane currents; add. of γ-aminobutyric acid (GABA, 3 μM) and bicuculline (BIC,100 μM)
Results
title comp. potentiated GABA-induced currents
Citation
Feigenspan; Bormann
European Journal of Pharmacology - Molecular Pharmacology Section, 1994 , vol. 288, # 1 p. 97 - 104 Title/Abstract Full Text Show Details
Assay Description
Effect : |receptor; binding activity Target : different brain regions of Harlan Sprague-Dawley rat Bioassay : region sepcific changes in benzodiazepine binding site labeled by <3H>-title compound in discrete brain regions of rats made tolerant and dependent upon pentobarbital the brain sections of rats (rendered tolerant by intracerebroventricular infusion with pentobarbital (300 μg/10μl/h for 6 d)) incubated with 1 nM <3H>-labeled title compound for 90 min at 4 deg C, pH 7.1; autoradiograms generated
Results
in tolerant rats: significant increase in <3H>-title compound binding sites in frontal cortex and olfactory bulb; in dependent rats: increase in frontal cortex, caudate-putamen, olfactory tubercle, olfactory bulb, globus pallidus and ventral pallidum
Citation
Suzuki; Ito; Wellman; Ho Ing Kang
Life Sciences, 1995 , vol. 57, # 5 p. 63 - 69 Title/Abstract Full Text Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |pharmacokinetics Bioassay : drugs were administered into femoral vein, blood samples taken from the carotid artery of the womb; pharmacokinetic parameters of the transplacental passage were determined
Results
half-life of elimination phase: t1/2λ2=83.49 min; foetomaternal conc ratio at equilibrium: FMCReq=0.324; time to reach equilibrium: teq=37.67 min
Citation
Staud; Fendrich; Kopecka; Palicka; Laznicek
Pharmaceutical Sciences, 1996 , vol. 2, # 4 p. 195 - 198 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |receptor; binding activity Bioassay : Wistar rats, membranes prepared from the cerebral cortex, cerebellum and spinal cord, enriched with cholesterol, incubated with phosphatidylcholine liposomes, experiments were performed to determine the binding effects in the presence of pregnanolone
Results
the potency of pregnanolone was reduced by a factor of 3.2 in cerebral cortex while increased by a factor of 8.4 in spinal cord by title comp. following cholesterol enrichment, little overall change in cerebellum in pregnanolon potency by title comp.
Citation
Bennett; Simmonds
British Journal of Pharmacology, 1996 , vol. 117, # 1 p. 87 - 92 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |receptor; binding activity Bioassay : Wistar rats, membranes prepared from the whole brain, enriched with cholesterol, incubated with phosphatidylcholine liposomes, experiments were performed to determine the binding effects in the presence of pregnanolone, propofol, muscimol
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Results
cholesterol enrichment did not affected the binding of title comp., however, the enhancement of binding by pregnanolone was affected; that of by propofol was reduced in cholesterol-enriched membranes, muscimol was a potentiator of title comp. binding
Citation
Bennett; Simmonds
British Journal of Pharmacology, 1996 , vol. 117, # 1 p. 87 - 92 Title/Abstract Full Text View citing articles Show Details
Results
significant deterioration of the individual optimal quotient in the driver-vehicle-road system and of steering ability, the increase of the number of errors in technical handling; 2 mg; male and female; orally
Citation
Schmidt; Brendemuhl; Dellen; Meurer-Kruell; Helm
Arzneimittel-Forschung/Drug Research, 1985 , vol. 35, # 8 p. 1336 - 1340 Title/Abstract Full Text View citing articles Show Details
Results
impairement of motor coordination - ED 50: 0.23 mg/kg p.o., induce of muscle relaxation - ED 50: 0.15 mg/kg p.o., 0.5 h, female mice; inhibition of in vitro tritiated flunitrazepam binding, Ki = 4.4 nmol/l, rats
Citation
Chambon; Perio; Demarne; et al.
Arzneimittel-Forschung/Drug Research, 1985 , vol. 35, # 10 p. 1572 - 1577 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus granule cell
Assay Description
Effect : potentiation of GABA-gated currents Bioassay : cells prepared from 8-d-old pups; whole-cell recordings of inward currents obtained from granule neurons maintained for 8 d in vitro without flumazenil pretreatment then cells treated with 0.3 μM GABA and various concentrations of flumazenil
Results
in presence of title comp. + 0.3 μM GABA potentiation of GABA-gated currents were 112 percent, 111 percent, 50 percent and 24 percent without flumazenil, in presence of 20 nM, 1 μM and 10 μM flumazenil, resp.
Citation
Zheng; Caruncho; Wei Jian Zhu; Vicini; Ikonomovic; Grayson; Costa
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 277, # 1 p. 525 - 533 Title/Abstract Full Text View citing articles Show Details
Results
loss of palpebral reflex (in 77 s), apnea onset (in 91 s), duration of apnea 114 s, percent of apnea onset 80, no changes in PaO2, increase of PaCO2 and pH, decrease of BE, fall in SAP, DAP, MAP (5 min), decrease of HR (human, 0.03 mg/kg)
Citation
Morel; Forster; Gardaz; Suter; Gemperle
Arzneimittel-Forschung/Drug Research, 1981 , vol. 31, # 12 a p. 2264 - 2267 Title/Abstract Full Text View citing articles Show Details
Results
immediate fall and then slow increase of BP (hypertonic human, 0.015 mg/kg, i.v. + 1 mg/kg of ketamine)
Citation
Langrehr; Erdmann
Arzneimittel-Forschung/Drug Research, 1981 , vol. 31, # 12 a p. 2269 - 2273 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : human embryonic kidney cell line 293 (HEK 293) Bioassay : membranes from HEK cells in Tris-citrate buffer (pH 7.4) incubated with various concns. of (3H)-title comp. for 90 min at 4 deg C in absence or presence of 100 μM diazepam; radioactivity measured after rapid filtration
Results
binding of (3H)-title comp. increased with increasing concn.; Kd for specific binding above 100 nM; high values for non specific binding
Citation
Fuchs; Zezula; Slany; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 289, # 1 p. 87 - 95 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : transfected human embryonic kidney (HEK) cell line 293
Bioassay : transfected cells, with various combinations of plasmids encoding for GABAA receptor subunits, incubated with (3H)-title comp. in presence or absence of 100 μM GABA for 120 min at 4 deg C; results expressed as percent of the experiments without GABA HEK cells transfected with cDNA encoding for rat brain α1-, β3- and γ2-subunits of GABAA receptors; polymerase chain reaction (PCR) used for estimation of
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Results
binding of (3)H-title comp. to cells transfected with α1,β3,γ2 GABAA subunits in presence of GABA 191 percent; not detected in case of α1β3 and β3γ2;
Citation
Fuchs; Zezula; Slany; Sieghart
European Journal of Pharmacology - Molecular Pharmacology Section, 1995 , vol. 289, # 1 p. 87 - 95 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : binding Target : brain of Sprague-Dawley rat Bioassay : autoradiographic anal. of dried slices; ASO - antisense oligodeoxynuclide rats (250-300 g) cannulated, injection of vehicle or gamma-2 ASO (18 μg, every 12 h 3 days) into right i.c.v. space; 6 h after last i.c.v. injection rats killing, brain slices prepn.; preincubation (30 min); incubation with 3H-labeled title compd.
Results
specific binding in various brain tissue areas (dependence on gamma-2 ASO pretreatment) evaluated (diagram)
Citation
Zhao, Tai-Jun; Li, Ming; Chiu, Ted H.; Rosenberg, Howard C.
Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 287, # 2 p. 752 - 759 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : expression of α1 subunit protein of GABAA receptor Target : primary cerebellar granule cells from Sprague-Dawley rats Bioassay : Western blotting; optical density readings in vitro; cells isolated from post-natal day 8 Sprague-Dawley rats, culture density 6-7E6 cells per 25 cm2, treated with the title comp. at day 8 in vitro, 37 deg C, 2 days, enhanced chemiluminescence used to detect GABAA receptor subunit proteins
Results
the level of GABAA receptor α1 subunit protein is significantly reduced (-25+/-4 percent , -58+/-18 percent, -41+/-3 percent for doses 1 nM, 10 nM, 1μM, respectively
Citation
Brown, Maria J.; Bristow, David R.
British Journal of Pharmacology, 1996 , vol. 118, # 5 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : expression of the GABAA α6 subunit protein Target : cerebellar granule cells from Sprague-Dawley rats Bioassay : BME=basal modified Eagle`s medium, ECL=enhanced cheminiluminescence in vitro; 6-7E6 cells per 25 cm2, at day 8 media replaced with supplemented BME with 10 μM cytosine arabinoside and the title comp., 37 deg C, 12 days, cells harvested for protein, western blotting, ECL detection GABAA receptor subunit proteins
Results
expression of GABAA receptor α6 subunit protein is not altered by exposure to 1 μM flunitrazepam treatment over a 12 day treatment period
Citation
Brown, Maria J.; Bristow, David R.
British Journal of Pharmacology, 1996 , vol. 118, # 5 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : pancreas of pig Bioassay : radioactivity counted after filtration; PK-11195: 1-(2-chlorophenyl-N-methyl-1-methyl-propyl)-3-isoquinolinecarboxamide (benzodiazepine receptor ligand) pure islets of Langerhans prepared from the market-age pigs; membrane prepared and 0.05 mg of proteins incubated at 0 deg C with <3H>PK-11195 (0.4 nmol/l) in the presence of 5 to 8 different concentrations of the title comp.
Results
title comp. displaced PK-11195; Ki = 3400 nmol/l (table)
Citation
Marchetti, Piero; Trincavelli, Letizia; Giannarelli, Rosa; Giusti, Laura; Coppelli, Alberto; Martini, Claudia; Navalesi, Renzo; Lucacchini, Antonio
Biochemical Pharmacology, 1996 , vol. 51, # 11 p. 1437 - 1442 Title/Abstract Full Text View citing articles Show Details
Assay Description
Effect : |receptor; binding activity Target : P2 cortical membranes Bioassay : CBR tested; nonspecific binding determined in the presence of clonazepam; CBR: central-type benzodiazepine receptor in vitro; saturation binding study; <3H>title comp. as radioligand; incubated at 4 deg C for 30 min under 760 μM O2; liquid scintillation counting
Results
graphical representation
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Citation
Courtiere; Molard; Reybaud
Biochemical Pharmacology, 1995 , vol. 50, # 11 p. 1815 - 1822 Title/Abstract Full Text Show Details
Assay Description
Effect : receptor subunit protein expression; inhibition of Target : rat primary cerebellar granule cells Bioassay : further investigations on mechanism of action using bisindolylmaleimide and H-89 cells incubated with title comp. at 37 deg C for 10 min or 1 h; cells lysed in denaturating buffer, GABAA receptor α1 and β2/3 subunit protein detected in whole cell extracts measuring protein immunoreactivity in grey-scale units by densitometry
Results
reduction of α1 and β2/3 subunit protein levels by 22 and 21 percent, respectively, via protein kinase C-dependent mechanism (diagram)
Citation
Johnston, Jonathan D.; Price, Sally A.; Bristow, David R.
British Journal of Pharmacology, 1998 , vol. 124, # 7 p. 1338 - 1340 Title/Abstract Full Text View citing articles Show Details
Target
GABA-A receptor:Wild
Biological material
Rattus norvegicus nerve cell
Assay Description
Effect : GABAA receptor; modulation of Bioassay : GABA: γ-aminobutyric acid; GABA EC50 ratio: GABA EC50 in presence of title comp./GABA EC50 without title comp.; control: not CHL- or ECHL-enriched or CHL-depleted; CHL: cholesterol; ECHL: epicholesterol neurons enriched with CHL, ECHL or depleted, attached to patch electrode for whole-cell patch clamp recording; membrane current recorded from somata of neurons, voltageclamped at -20 mV at ca. 20 deg C; GABA and title comp. added simultaneously
Results
GABA EC50 ratio in CHL-depleted (56 percent control), CHL-enriched (182 percent control) and ECHL-incorporated neurons: 0.397, 0.276 and 0.297, resp. (control: 0.477)
Citation
Sooksawate; Simmonds
British Journal of Pharmacology, 2001 , vol. 134, # 6 p. 1303 - 1311 Title/Abstract Full Text View citing articles Show Details
Target
Gamma-aminobutyric acid receptor subunit delta [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [taurine cattle]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [taurine cattle]:Wild
Substance action on target
Antagonist
Biological material
taurine cattle
Assay Description
Ratio of binding affinity of the compound towards cow Central benzodiazepine receptor from cortical membrane without GABA to that of with 50 uM GABA
Citation
Anzini, Maurizio; Valenti, Salvatore; Braile, Carlo; Cappelli, Andrea; Vomero, Salvatore; Alcaro, Stefano; Ortuso, Francesco; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Daniele, Simona; Martini, Claudia; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5694 - 5711 Title/Abstract Full Text View citing articles Show Details
Target
Gamma-aminobutyric acid receptor subunit delta [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Substance action on target
Antagonist
Biological material
human
Assay Description
Ratio of binding affinity of the compound towards human Central benzodiazepine receptor from cortical membrane without GABA to that of with 50 uM GABA
Citation
Anzini, Maurizio; Valenti, Salvatore; Braile, Carlo; Cappelli, Andrea; Vomero, Salvatore; Alcaro, Stefano; Ortuso, Francesco; Marinelli, Luciana; Limongelli, Vittorio; Novellino, Ettore; Betti, Laura; Giannaccini, Gino; Lucacchini, Antonio; Daniele, Simona; Martini, Claudia; Ghelardini, Carla; Di Cesare Mannelli, Lorenzo; Giorgi, Gianluca; Mascia, Maria Paola; Biggio, Giovanni
Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5694 - 5711 Title/Abstract Full Text View citing articles Show Details
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Target
Gamma-aminobutyric acid receptor subunit delta:Wild + Gamma-aminobutyric acid receptor subunit beta-2:Wild + Gamma-aminobutyric acid receptor subunit alpha-1:Wild
Assay Description
Ratio of inhibition constant against GABAA receptor in C57BL/6J to that of gamma2F77I in mouse brain membrane upon incubation for 90 min at 4 degree C using 50 mM Tris/citrate buffer (pH 7.1) and 5 nM [3H]flunitrazepam radioligand
Citation
Ogris, Waltraud; Poeltl, Angelika; Hauer, Birgit; Ernst, Margot; Oberto, Alessandra; Wulff, Peer; Hoeger, Harald; Wisden, William; Sieghart, Werner
Biochemical Pharmacology, 2004 , vol. 68, # 8 p. 1621 - 1629 Title/Abstract Full Text View citing articles Show Details
Target
Peripheral-type benzodiazepine receptor-associated protein 1:Wild
Substance action on target
Radioligand (/ligand)
Assay Description
Binding affinity of the compound towards benzodiazepine receptor
Citation
Billie K. Koe
Patent: US4320124 A, 1981 ; Title/Abstract Full Text Show Details
Target
Platelet-activating factor receptor:Wild
Substance action on target
Antagonist
Assay Description
Antagonistic activity towards platelet activating factor receptor
Citation
Casals-Stenzel, Jorge, Dr.; Weber, Karl-Heinz, Dr.; Walther, Gerhard, Dr.; Harreus, Albrecht, Dr; Muacevic, Gojki, Dr.
Patent: EP176928 A2, 1986 ; Title/Abstract Full Text Show Details
Target
Peripheral-type benzodiazepine receptor-associated protein 1:Wild
Assay Description
Activity of the compound against Benzodiazepine receptor
Citation
Pfizer Inc.
Patent: US4320124 A, 1982 ; Title/Abstract Full Text Show Details
Target
chloride channel:Wild
Substance action on target
Agonist
Assay Description
Agonistic activity of compound towards chloride channel receptor
Citation
L'Oreal
Patent: US5869068 A, 1999 ; Title/Abstract Full Text Show Details
Target
Dihydropteridine reductase [Escherichia coli]:Wild
Biological material
Escherichia coli
Assay Description
Ratio of catalytic activity to that of michaelis-menten constant towards recombinant escherichia coli nitroreductase NfsB in the presence of NADPH (2 mM) incubated for 2 h under anaerobic conditions using nitroreductase assay
Results
kcat/Km not calculated
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Citation
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
Target
Dihydropteridine reductase [Escherichia coli]:Wild
Biological material
Escherichia coli DH5
Assay Description
Activity of compound (64 uM) towards Escherichia coli DH5 nitroreductase NfsB under anaerobic conditions in presence of NADPH (2 mM) using nitroreductase assay
Results
Activity not calculated
Citation
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
Target
Dihydropteridine reductase [Salmonella enterica serovar Typhimurium]:Wild
Biological material
Salmonella enterica serovar Typhimurium TA 1537
Assay Description
Activity of compound (64 uM) towards Salmonella typhimurium TA1537 nitroreductase NfsB under anaerobic conditions in presence of NADPH (2 mM) using nitroreductase assay
Results
Activity not calculated
Citation
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
Target
Dihydropteridine reductase [Enterobacter cloacae]:Wild
Biological material
Enterobacter cloacae
Assay Description
Activity of compound (64 uM) towards Enterobacter cloacae nitroreductase NfsB under anaerobic conditions in presence of NADPH (2 mM) using nitroreductase assay
Results
Activity not calculated
Citation
LinWu, Shiuan-Woei; Syu, Cheng-Jie; Chen, Yu-Lian; Wang, Andrew H.-J.; Peng, Fu-Chuo
Biochemical Pharmacology, 2009 , vol. 78, # 1 p. 96 - 103 Title/Abstract Full Text View citing articles Show Details
Effect
agonistic activity
Target
GABA-A receptor:Wild
Substance action on target
Agonist
Assay Description
Agonistic activity of the compound towards GABAA receptor
Results
Not Published
Citation
MOSKOWITZ Michael A.
Patent: WO1996/15782 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
binding activity
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Target
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-2 [human]:Wild
Substance action on target
Radioligand (/ligand)
Assay Description
Binding affinity towards gamma-aminobutyric acid (GABA) A receptor, alpha2beta3gamma2 with 10 mM Tris-HCl pH 7.4 using [3H]Ro15-1788 upon incubation for 1 h at RT
Citation
DAWSON Gerard Raphael
Patent: WO1996/25948 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
binding activity
Target
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-5 [human]:Wild
Substance action on target
Radioligand (/ligand)
Assay Description
Binding affinity towards gamma-aminobutyric acid (GABA) A receptor, alpha5beta3gamma2 with 10 mM Tris-HCl pH 7.4 using [3H]Ro15-1788 upon incubation for 1 h at RT
Citation
DAWSON Gerard Raphael
Patent: WO1996/25948 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
binding activity
Target
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-3 [human]:Wild
Substance action on target
Radioligand (/ligand)
Assay Description
Binding affinity towards gamma-aminobutyric acid (GABA) A receptor, alpha3beta3gamma2 using with 10 mM Tris-HCl pH 7.4 [3H]Ro15-1788 upon incubation for 1 h at RT using Tris-HCl as radioligand AT pH 7.5
Citation
DAWSON Gerard Raphael
Patent: WO1996/25948 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
binding activity
Target
Gamma-aminobutyric acid receptor subunit beta-3:Wild + Gamma-aminobutyric acid receptor subunit alpha-6:Wild + GABA-A receptor (Gamma 3):Wild
Substance action on target
Radioligand (/ligand)
Assay Description
Binding affinity towards gamma-aminobutyric acid (GABA) A receptor, alpha6beta3gamma3 using with 10 mM Tris-HCl pH 7.4 [3H]Ro15-1788 upon incubation for 1 h at RT
Citation
DAWSON Gerard Raphael
Patent: WO1996/25948 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
binding activity
Target
Gamma-aminobutyric acid receptor subunit gamma-2 [human]:Wild + Gamma-aminobutyric acid receptor subunit beta-3 [human]:Wild + Gamma-aminobutyric acid receptor subunit alpha-1 [human]:Wild
Substance action on target
Radioligand (/ligand)
99 of 99
Assay Description
Binding affinity towards gamma-aminobutyric acid (GABA) A receptor, alpha1beta3gamma2 with 10 mM Tris-HCl pH 7.4 using [3H]Ro15-1788 as radioligand upon incubation for 1 h at RT
Citation
DAWSON Gerard Raphael
Patent: WO1996/25948 A1, 1996 ; Title/Abstract Full Text Show Details
Effect
inhibitory activity
Target
GABA-A receptor:Wild
Substance action on target
Inhibitor
Assay Description
Inhibitory activity of the compound against GABAA receptor
Results
Not Published
Citation
Moskowitz Michael A.
Patent: EP1839657 A2, 2007 ; Title/Abstract Full Text Show Details
In vivo: Animal Model (143) Quantitative Results pX
Parameter
Value (qual)
Value (quant)
Unit
Action on Target
Animal Model
Biological Species
Route of administration
%
25
%
Sprague Dawley rat
Dose
Dosing regimen
Effect
Reference (expand all/collapse all)
intraperitoneal administration
5 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
10 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
20 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
60 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
5 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
10 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
%
88
%
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
%
100
%
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
%
100
%
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
Number
6.4
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
Number
Pranzatelli
28.7
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
Number
48
Sprague Dawley rat
intraperitoneal administration
20 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
60 mg/kg
Single
Experimental Neurology, ...
Title/Abstract Full Text Show Details
Sprague Dawley rat
intraperitoneal administration
Single
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
Number
47.7
Pranzatelli
Experimental Neurology, 1989 , vol. 104, # 3 p. 241 - 250 Title/Abstract Full Text Show Details
ID50
2.1
mg/kg
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
ID50
2.5
mg/kg
Sprague Dawley rat
intraperitoneal administration
Single
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
ID50
2.6
mg/kg
Sprague Dawley rat
intraperitoneal administration
Single
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
ID50
2.8
mg/kg
Sprague Dawley rat
intraperitoneal administration
Single
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
ID50
3.5
mg/kg
Sprague Dawley rat
intraperitoneal administration
Single
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Benavides; Peny; Durand; Arbilla; Scatton
Journal of Pharmacology and Experimental Therapeutics, 1992 , vol. 263, # 2 p. 884 - 896 Title/Abstract Full Text View citing articles Show Details
ED50
4.63
mg/kg
Rattus norvegicus
intraperitoneal administration
0.160000 mg/kg
Behavioural Symptoms
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Voss, Jeppe; Sanchez, Connie; Michelsen, Signe; Ebert, Bjarke
European Journal of Pharmacology, 2003 , vol. 482, # 1-3 p. 215 - 222 Title/Abstract Full Text View citing articles Show Details
ID50
0.22
µmol/kg
experimental convulsion
DBA 2 mouse
intraperitoneal administration
Single
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
ID50
0.18
µmol/kg
experimental convulsion
DBA 2 mouse
intraperitoneal administration
Single
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
ID50
0.29
µmol/kg
experimental convulsion
Swiss Webster mouse
intraperitoneal administration
Single
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
ED50
8.7
µmol/kg
Swiss Webster mouse
intraperitoneal administration
Single
Pharmacology Biochemistr...
Title/Abstract Full Text View citing articles Show Details
De Sarro, Giovambattista; Carotti, Angelo; Campagna, Francesco; McKernan, Ruth; Rizzo, Milena; Falconi, Umberto; Palluotto, Fausta; Giusti, Pietro; Rettore, Cristina; De Sarro, Angela
Pharmacology Biochemistry and Behavior, 2000 , vol. 65, # 3 p. 475 - 487 Title/Abstract Full Text View citing articles Show Details
Number
56
C57BL 6 mouse
intraperitoneal administration
5 mg/kg
Single
Sedative
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Dose
Dosing regimen
Effect
Reference (expand all/collapse all)
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Harris, Danni L.; Delorey, Timothy M.; He, Xiaohui; Cook, James M.; Loew, Gilda H.
European Journal of Pharmacology, 2000 , vol. 401, # 3 p. 271 - 287 Title/Abstract Full Text View citing articles Show Details
Time
19
minute
Wistar rat
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
pX
Parameter Time
Value (qual)
Value (quant)
Unit
16.9
minute
Action on Target
Animal Model
Biological Species
Route of administration
Wistar rat
oral administration
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
17.2
minute
Wistar rat
oral administration
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
11.5
minute
Wistar rat
oral administration
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
34.6
minute
Wistar rat
oral administration
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
33.6
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
18.6
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
16.2
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
32.5
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
31.6
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
34.3
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.3
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
39.4
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
37.3
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.4
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.8
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
39.6
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.4
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
40.4
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
36.7
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
34.4
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
36.9
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
36.8
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.7
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
33.6
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.2
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
32.9
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
39
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
30.2
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
36.4
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
38.7
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
37.2
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
26.7
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
26.7
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
31.1
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
31.5
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
24.5
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
24.6
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
31.2
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
33.6
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
19.5
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
25.8
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
26.8
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209
Title/Abstract Full Text View citing articles Show Details
Time
28.1
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
24.8
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
25.7
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
20.5
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
24.5
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
21.6
minute
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
18.2
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
23.2
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
24.8
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
23.3
minute
Wistar rat
oral
0.500000
Single
Hypnotic
Psychopharmacology, 2004...
administration
mg/kg
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
28.8
minute
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
29.8
minute
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
31.1
minute
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
43.3
second
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
46.9
second
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
44.4
second
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
43.5
second
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
30.1
second
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
29.5
second
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
32.3
second
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
29.9
second
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
304.3
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
282.8
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
311.1
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
321.5
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
273.5
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
300.1
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
296.3
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
335.1
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
14.4
second
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
14.4
second
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
13
second
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
12.1
second
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
17.3
second
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
17.9
second
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
15.6
second
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Time
14.5
second
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
115
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
126.8
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
112.9
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
91.1
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
49.5
Wistar rat
oral administration
0.500000 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
57.3
Wistar rat
oral administration
1 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
42.8
Wistar rat
oral administration
2 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
Number
65.4
Wistar rat
oral administration
5 mg/kg
Single
Hypnotic
Psychopharmacology, 2004...
Title/Abstract Full Text View citing articles Show Details
Shinomiya, Kazuaki; Shigemoto, Yuki; Omichi, Junji; Utsu, Yoshiaki; Mio, Mitsunobu; Kamei, Chiaki
Psychopharmacology, 2004 , vol. 173, # 1-2 p. 203 - 209 Title/Abstract Full Text View citing articles Show Details
ED50
0.89
mg/kg
Rattus norvegicus
oral administration
0.500000 mg/kg
Anticonvulsant
Pharmacology, 1998 , vo...
Title/Abstract Full Text View citing articles Show Details
Fukinaga, Masafumi; Ishizawa, Keisuke; Kamei, Chiaki
Pharmacology, 1998 , vol. 57, # 5 p. 233 - 241 Title/Abstract Full Text View citing articles Show Details
ID50
0.2 - 0.3
mg/kg
Atack, John R.; Smith, Alison J.; Emms, Frances; McKernan, Ruth M.
Neuropsychopharmacology, 1999 , vol. 20, # 3 p. 255 - 262
Swiss Webster mouse
intraperitoneal administration
Single
Neuropsychopharmacology,...
Title/Abstract Full Text View citing articles Show Details
Title/Abstract Full Text View citing articles Show Details
ID50
1.69
µmol/kg
Mus musculus
intraperitoneal administration
0.300000 nM
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
0.320000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
3.20000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
32 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
0.0318000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
0.318000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
3.18000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
9.55000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Mus musculus
intraperitoneal administration
31.8000 µmol/kg
Single
European Journal of Phar...
Title/Abstract Full Text Show Details
Rattus norvegicus
intravenous administration
10 mg/kg
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
Concentration
0.13
µmol/kg
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
Concentration
1.4
µmol/kg
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
Concentration
6.3
µmol/kg
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
% Inhibition
7
%
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
% Inhibition
12
%
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
% Inhibition
78
%
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
% Inhibition
85
%
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
% Inhibition
92
%
Chang; Snyder
European Journal of Pharmacology, 1978 , vol. 48, # 2 p. 213 - 218 Title/Abstract Full Text Show Details
7.54
Ki
29
nM
Hoogerkamp; Arends; Bomers; Mandema; Voskuyl; Danhof
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 803 - 812 Title/Abstract Full Text View citing articles Show Details
ED50
0.32
µmol/kg
experimental
Mus
Anticonvulsant
Life Sciences, 1978 , v...
convulsion
musculus
Title/Abstract Full Text Show Details
Fighting behaviour
Mus musculus
Anxiolytic
Life Sciences, 1978 , v...
Title/Abstract Full Text Show Details
Mus musculus
subcutaneous administration
Journal of Medicinal Che...
Title/Abstract Full Text Show Details
guinea pig
Patent: EP176928 A2, 1...
Title/Abstract Full Text Show Details
Single
Psychopharmacology, 2014...
Title/Abstract Full Text View citing articles Show Details
Mohler; Okada; Heitz Ph.; Ulrich
Life Sciences, 1978 , vol. 22, # 11 p. 985 - 996 Title/Abstract Full Text Show Details
ED50
2.5
µmol/kg
Mohler; Okada; Heitz Ph.; Ulrich
Life Sciences, 1978 , vol. 22, # 11 p. 985 - 996 Title/Abstract Full Text Show Details
ED50
=
2.41
mg/kg
Blair; Webb
Journal of Medicinal Chemistry, 1977 , vol. 20, # 9 p. 1206 - 1210 Title/Abstract Full Text Show Details
4.34
IC50
=
46
µM
Inhibitor
Casals-Stenzel, Jorge, Dr.; Weber, Karl-Heinz, Dr.; Walther, Gerhard, Dr.; Harreus, Albrecht, Dr; Muacevic, Gojki, Dr.
Patent: EP176928 A2, 1986 ; Title/Abstract Full Text Show Details
ED50
0.11
mg/kg
drug discrimination test
rhesus monkey
experimental epilepsy
DBA 2 mouse
subcutaneous administration
Gerak, Lisa R.; France, Charles P.
Psychopharmacology, 2014 , vol. 231, # 1 p. 181 - 190 Title/Abstract Full Text View citing articles Show Details
ED50
0.22
μmol/kg
intraperitoneal administration
0.11 0.41 μmol/kg
Anticonvulsant
Journal of Molecular Neu...
Title/Abstract Full Text View citing articles Show Details
Gatta, Elena; Cupello, Aroldo; Di Braccio, Mario; Grossi, Giancarlo; Robello, Mauro; Scicchitano, Francesca; Russo, Emilio; De Sarro, Giovambattista
Journal of Molecular Neuroscience, 2016 , vol. 60, # 4 p. 539 - 547 Title/Abstract Full Text View citing articles Show Details
ED50
0.18
μmol/kg
experimental epilepsy
DBA 2 mouse
intraperitoneal administration
0.09 0.36 μmol/kg
Anticonvulsant
Journal of Molecular Neu...
Title/Abstract Full Text View citing articles Show Details
Gatta, Elena; Cupello, Aroldo; Di Braccio, Mario; Grossi, Giancarlo; Robello, Mauro; Scicchitano, Francesca; Russo, Emilio; De Sarro, Giovambattista
Journal of Molecular Neuroscience, 2016 , vol. 60, # 4 p. 539 - 547 Title/Abstract Full Text View citing articles Show Details
Qualitative Information 1 of 17
Effect Assay Description
2 of 17
Analgesic
Target : Crl:CD-1(ICR)BR mice Bioassay : percent = 100 * number of nonresponders / number in group in vivo; Crl:CD-1(ICR)BR mice (18-25 g) grouphoused (5-15/cage); title comp. was given 30 min before i.p. injection of endothelin-1 (0.1 mg/kg); single abdominal constriction response recorded
Results
less than 50 percent antagonism at the maximum dose (10 mg/kg) applied
Citation
Raffa, Robert B.; Schupsky, James J.; Lee, David K. H.; Jacoby, Henry I.
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 278, # 1 p. 1 - 7 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |pharmacokinetics Bioassay : control: vehicle; PK/PD: pharmacokinetic - pharmacodynamic model; PK/PD model converged yielding estimates of both in vivo receptor affinity (K ) and in vivo intrinsic efficacy (e
) conc.-
PD
PD
effect relationships; arterial blood samples taken in time points after title comp. injection; plasma conc. of title comp. determined by HPLC with UV detection; pharmacodynamics estimated by recording EEG (electroencephalogram) parameters
3 of 17
4 of 17
Results
title comp. PK/PD modeling revealed monophasic concentration-EEG effect relationships with potency (EC50) 35.5 ng/ml and intrinsic activity 9.3 μV; KPD = 9.5 ng/ml and ePD = 0.50
Citation
Visser; Wolters; Gubbens-Stibbe; Tukker; Van Der Graaf; Peletier; Danhof, Meindert
Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 88 - 101 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |drug interaction Bioassay : opioids: morphine sulfate, buprenorphine hydrochloride, methadone hydrochloride; MLD: median lethal dose randomized blind MLD studies; up-and-down method performed in quadruplicate; four series; rats pretreated with title comp., 30 min thereafter treated with opioids; animals examined repeatedly during first 4 h after injection, then daily for mortality
Results
MLDs decreased signif. by pretreatm. with title comp. in case of buprenorphine and methadone; no signif. effects on MLD of morphine; admin. of title comp. signif. prolonged time to death in buprenorphine-treated rats; no signif. effects in other cases
Citation
Borron; Monier; Risede; Baud
Human and Experimental Toxicology, 2002 , vol. 21, # 11 p. 599 - 605 Title/Abstract Full Text View citing articles Show Details
Effect
Hypnogenic
Biological material
human
Assay Description
5 of 17
6 of 17
Bioassay : polysomnographic recordings were made at selected nights (1, 2, 3, 4, 7, 10, 12, 14); delta as 0.3-3.0 Hz sigma as 10.0-15.0 Hz and beta as 20.0-28.0 Hz were defined five healthy young volunteers (age 19-22); experiment performed on a fourteen day schedule in a double blind design; from the fourth to the tenth night title comp. administered before bedtime; otherwise placebo was administered at that time
Results
alteration of delta, sigma and beta EEG induced by title comp. for 7 consecutive nights; sleep EEG subjected to fast Fourier transform analysis; sigma was enhanced without regard to delta amount, but beta only during epochs contng. low delta
Citation
Uchida, Sunao; Okudaira, Nobuyuki; Nishihara, Kyoko; Iguchi, Yoshinobu; Tan, Xin
Life Sciences, 1996 , vol. 59, # 9 p. PL117-PL120 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : respiration; inhibition of Bioassay : BUP: buprenorphine catheters placed to anesthetized rats 22 h before test; title comp. admin. alone or in combination with 30 mg/kg of BUP; arterial blood samples collected before and at 1.5120 min after title comp. admin.; blood gases measured
Results
title comp. with BUP caused respiratory depression; no effect on respiration of title comp. alone; decrease in arterial PaO2, blood pH and increase in PaCO2 after dose of title comp. and BUP; conc. of PaO2, PaCO2, HCO3 and pH values vs time; figures
Citation
Megarbane, Bruno; Pirnay, Stephane; Borron, Stephen W.; Trout, Herve; Monier, Claire; Risede, Patricia; Boschi, Gabrielle; Baud, Frederic J.
Toxicology Letters, 2005 , vol. 157, # 3 p. 211 - 219 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |drug interaction Bioassay : rats trained for 3 d; 24 h after rats treated with title comp. for 45 min and with gaboxadol (Ca 1-10 mg/kg, s.c.) for 30 min; rotarod motor coordination test performed
Results
no synergistic interaction between title comp. and gaboxadol observed
Citation
Voss, Jeppe; Sanchez, Connie; Michelsen, Signe; Ebert, Bjarke
European Journal of Pharmacology, 2003 , vol. 482, # 1-3 p. 215 - 222 Title/Abstract Full Text View citing articles Show Details
7 of 17
8 of 17
Biological material
Rattus norvegicus
Assay Description
Effect : |drug interaction Bioassay : 24 h before title comp. administration rats trained for 3 d; treatment with ethanol (1.0 g/kg, i.p.) for 15 min and with title comp. for 45 min; rotarod motor coordination test performed
Results
supra-additive effect of title comp. at dose of 0.63 mg/kg and ethanol observed
Citation
Voss, Jeppe; Sanchez, Connie; Michelsen, Signe; Ebert, Bjarke
European Journal of Pharmacology, 2003 , vol. 482, # 1-3 p. 215 - 222 Title/Abstract Full Text View citing articles Show Details
Effect
Hypnogenic
Biological material
human
Assay Description
9 of 17
Results
during non rapid eye movement (NREM) sleep of 4DN and 7DN sigma band activity was similarly enhanced in every S; in rapid eye movement sleep of 4DN and 7DN the beta band was enhanced with larger variations among Ss (table, diagram)
Citation
Uchida, Sunao; Okudaira, Nobuyuki; Nishihara, Kyoko; Iguchi, Yoshinobu
Life Sciences, 1996 , vol. 58, # 10 p. PL199-PL205 Title/Abstract Full Text View citing articles Show Details
Effect
Behavioural Symptoms
Assay Description
10 of 17
11 of 17
Bioassay : high intra-individual consistency of relative EEG power patterns on 4DN and 7DN was observed; double blind design 5 healthy volunteers (Ss, 19 - 22 yrs); title comp. administered for seven consecutive nights 30 min before bed time; sleep EEG from baseline night, the initial title comp. night the fourth (4DN) and the seventh (7DN) nights analysed
Target : Long-Evans rat Bioassay : GHB: γ-hydroxybutyrate title comp. was administered 1 week before, during (1000 mg/kg i.p. for 1 week) and 2 weeks after GHB treatment; motor performance (latency to fall) was recorded at both low (8 rpm) and high (32 rpm) speeds; rotorod assay
Results
title comp. dose-dependently decreased motor performance at both speeds, but was 4.6-15 fold more potent at high speed; GHB treatment did not alter potency of title comp.
Citation
Smith, Mark A.; Gergans, Samantha R.; Lyle, Megan A.
European Journal of Pharmacology, 2006 , vol. 552, # 1-3 p. 83 - 89 Title/Abstract Full Text View citing articles Show Details
Biological material
human
Assay Description
Effect : exposure Bioassay : accordance between data sources, reliability 1136 subjects age >65 years: 318 cases (hip fractures), 818 control; 276 men (mean age 79 years), 860 women (81); data sources: patient questionnaire, medical records, plasma samples (HPLC)
Results
concordance between questionnaires or medical records and plasma samples (table)
Citation
Moore; Pierfitte; Pehourcq; Lagnaoui; Begaud
Clinical Pharmacology and Therapeutics, 2001 , vol. 69, # 6 p. 445 - 450 Title/Abstract Full Text View citing articles Show Details
Biological material
Rattus norvegicus
Assay Description
Effect : |pharmacokinetics Bioassay : clearance ranged (CL), volume of distribution at steady-state (Vdss) and free fraction in plasma (fu) were calculated title comp. was infused into right jugular vein of rats (173-200 g) for 1 min;
blood samples (100 μl) were collecteed from a small incision in the tail; title comp. conc. in blood were determined by HPLC-UV
12 of 17
Results
CL 75.1 +/- 4.6 ml/min*kg; Vdss 5.3 +/- 0.6 l/kg; fu 11.1 +/- 0.2 percent (table)
Citation
Hoogerkamp; Arends; Bomers; Mandema; Voskuyl; Danhof
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 803 - 812 Title/Abstract Full Text View citing articles Show Details
Effect
Anticonvulsant
Biological material
Rattus norvegicus
Assay Description
13 of 17
14 of 17
15 of 17
Bioassay : TLS: threshold for localized seizure activity; EC250 value was defined as the concentration needed to increase the TLS by 250 μA for the total plasma conc. (EC250) and the free conc. (EC250,u) direct cortical stimulation model; title comp. was infused into right jugular vein for 1 min; anticonvulsant effect was expressed as elevation over the averadge base-line TLS and determined during the 30min period preceding title comp. administration
Results
title comp. rapidly increased TLS by 300 to 500 μA immediately after administration; the effect slowly declined back to base-line in parallel with the decrease in blood concentration; EC250 = 1.2 +/- 0.3 mg/l; EC250,u = 0.21
Citation
Hoogerkamp; Arends; Bomers; Mandema; Voskuyl; Danhof
Journal of Pharmacology and Experimental Therapeutics, 1996 , vol. 279, # 2 p. 803 - 812 Title/Abstract Full Text View citing articles Show Details
Effect
Behavioural Symptoms
Biological material
rhesus monkey
Assay Description
Effect : discriminative stimulus effects Bioassay : DR: drug responding ( percent responding on flumazenil lever); control response rate represents average of five saline sessions immediately preceding a test; flumazenil 0.32 mg/kg for three monkeys or 0.1 mg/kg for two monkeys diazepam-treated flumazenil discriminating monkeys (training cycles) injected with title comp. during first minute of first test cycle followed by cumulative doses of flumazenil during subsequent cycles; percent DR and response rate ( percent of control) calculated
Results
title comp. occasioned primarily vehicle-lever responding and attenuated the flumazenil discriminative stimulus, shifted flumazenil dose-effect curve to right, and did not substantially modify response rate
Citation
McMahon, Lance R.; France, Charles P.
Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details
Effect
Behavioural Symptoms
Biological material
rhesus monkey
Assay Description
Effect : discriminative stimulus effects Bioassay : DR: drug responding ( percent responding on midazolam lever); control response rate represents average of five saline sessions immediately preceding a test; substitution for midazolam was defined as >= 80 percent responding on midazolam-appropriate lever midazolam discriminating monkeys (midazolam training cycles) injected with title comp. during first minute of first test cycle followed by saline or sham injection on subsequent cycles; percent DR and response rate ( percent of control) calculated
Results
single dose of title comp. (0.032 and 0.1 mg/kg) increased midazolam-lever responding across cycles in a time-related manner (substitution for midazolam was observed within 30 min) and did not substantially modify response rate
Citation
McMahon, Lance R.; France, Charles P.
Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 304, # 1 p. 109 - 120 Title/Abstract Full Text View citing articles Show Details
Biological material
Mus musculus
Assay Description
Effect : |antagonist Bioassay : chronic treatment: inhalation of title compd. (120 mg/10 l air per min), pyrazole (1.0 mmol/kg/day, i.p.) and title compd. injections mice (30 g) chronically treated (inhalation) with ethanol and title compd. (8 days), withdrawal (8 h); mice decapitated, lysate from cerebral cortex anal. (Northern blot anal., radioimmunoassay)
16 of 17
17 of 17
Results
complete abolishment of increase of diazepam binding inhibitor mRNA level in ethanol treated/withdrawn mice (diagram)
Citation
Katsura; Ohkuma; Tsujimura; Kuriyama
Journal of Pharmacology and Experimental Therapeutics, 1995 , vol. 273, # 3 p. 1529 - 1533 Title/Abstract Full Text View citing articles Show Details
Biological material
human
Assay Description
Effect : |pharmacokinetics Bioassay : Cmax: maximum plasma conc.; AUC0-inf: area under conc.-time curve from 0 to infinity; Vdβ: volume of distribution; CL: plasma clearance title comp. given to 31 neonates and infants (0-438 days) as single 0.2-mg/kg dose (SD, n=28) or multiple doses (MD, 0.2 mg/kg followed by 2-6 doses 0.1 mg/kg, n=3); plasma title comp. conc. measured by GC-MS up to 72 h; pharmacokinetic analysis
Results
Cmax of title comp. after SD an MD 243 and 161 μg/l, AUC0-inf 2105 and 1454 μg*h/l, Vdβ 4.6 and 2.1 l/kg, CL 0.15 and 0.17 l/h/kg, resp.; CL and Vdβ sign. increased with postnatal age
Citation
Pariente-Khayat, Ann; Treluyer, Jean-Marc; Rey, Elisabeth; Mokhtari, Mostafa; Werner, Evelyne; Jouvet, Philippe; D'Athis, Philippe; Wood, Chantal; Hubert, Philippe; Hotellier, Francoise; Olive, Georges; Pons, Gerard
Clinical Pharmacology and Therapeutics, 1999 , vol. 66, # 2 p. 136 - 139 Title/Abstract Full Text View citing articles Show Details
Effect
Hypotensive
Biological material
human
Assay Description
Bioassay : plasma title comp. conc. measured by GC-MS title comp. given to neonates and infants (0-438 days) as single 0.2-mg/kg dose (n=28) or multiple doses (0.2 mg/kg followed by 2-6 doses 0.1 mg/kg, n=3); systolic and diastolic blood pressure (SBP and DBP) and heart rate (HR) recorded up to 72 h
Results
DBP (not SBP and HR) was sign. decreased with increasing title comp. plasma conc.
Citation
Pariente-Khayat, Ann; Treluyer, Jean-Marc; Rey, Elisabeth; Mokhtari, Mostafa; Werner, Evelyne; Jouvet, Philippe; D'Athis, Philippe; Wood, Chantal; Hubert, Philippe; Hotellier, Francoise; Olive, Georges; Pons, Gerard
Clinical Pharmacology and Therapeutics, 1999 , vol. 66, # 2 p. 136 - 139 Title/Abstract Full Text View citing articles Show Details
Metabolism (231) Quantitative Results pX
Parameter
1
% Inhibition
Value (qual)
Value (quant)
Unit
Action on Target
18
%
Target
Tissue/Organ
Cell
Cell fraction
Substrate /Carried Molecule
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
Buprenorphine
Dose
Reference (expand all/collapse all)
100 nM
European Journal of Clin...
Title/Abstract Full Text View citing articles Show Details
Chang, Yan; Moody, David E.
European Journal of Clinical Pharmacology, 2005 , vol. 60, # 12 p. 875 - 881 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
14
%
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
Buprenorphine
100 nM
European Journal of Clin...
Title/Abstract Full Text View citing articles Show Details
Chang, Yan; Moody, David E.
European Journal of Clinical Pharmacology, 2005 , vol. 60, # 12 p. 875 - 881 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
14
%
Cytochrome P450 3A4 [human]:Wild
Chang, Yan; Moody, David E.
European Journal of Clinical Pharmacology, 2005 , vol. 60, # 12 p. 875 - 881 Title/Abstract Full Text View citing articles Show Details
liver
Microsome
Buprenorphine
100 nM
European Journal of Clin...
Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
9
%
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
Buprenorphine
100 nM
European Journal of Clin...
Title/Abstract Full Text View citing articles Show Details
Chang, Yan; Moody, David E.
European Journal of Clinical Pharmacology, 2005 , vol. 60, # 12 p. 875 - 881 Title/Abstract Full Text View citing articles Show Details
3.2
IC50
635
µM
Cytochrome P450 2C19 [human]:Wild
liver
Microsome
Omeprazole
25 µM
Clinical pharmacology an...
Title/Abstract Full Text Show Details
Cytochrome P450 2E1 [human]:Wild
liver
Microsome
p-Nitrophenol
1000 µM
Xenobiotica, 1998 , vol...
Title/Abstract Full Text View citing articles Show Details
Cytochrome P450 2E1 [human]:Wild
liver
Cytochrome P450 2C19 [human]:Wild
LOCK RE, JONES BC, SMITH DA and HAWKSWORTH GM
Clinical pharmacology and therapeutics, 1997 , vol. 45 Title/Abstract Full Text Show Details
1
% Inhibition
10
%
Tassaneeyakul; Birkett; Miners
Xenobiotica, 1998 , vol. 28, # 3 p. 293 - 301 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
<
10
%
Microsome
p-Nitrophenol
250 µM
Xenobiotica, 1998 , vol...
Title/Abstract Full Text View citing articles Show Details
Tassaneeyakul; Birkett; Miners
Xenobiotica, 1998 , vol. 28, # 3 p. 293 - 301 Title/Abstract Full Text View citing articles Show Details
Clint
8.559
µL/min/mg protein
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Clint
1.341
µL/min/mg protein
Cytochrome P450 2C19 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Clint
1.494
µL/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Clint
1.762
µL/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Clint
1.036
µL/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Clint
1.586
µL/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.095
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
4.95
Km
11.1
µM
Cytochrome P450 2C19 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
1.27
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
3.97
Km
108
µM
Cytochrome P450 3A4 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.861
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
3.19
Km
642
µM
Cytochrome P450 2C19 [human]:Wild
BTITn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.42
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
BTITn5B1-4 cell line
Microsome
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
pX
Parameter
4.47
Km
Value (qual)
Value (quant)
Unit
34
µM
Action on Target
Target
Tissue/Organ
Cytochrome P450 3A4 [human]:Wild
Cell BTI-Tn5B1-4 cell line
Cell fraction
Substrate /Carried Molecule
Dose
Reference (expand all/collapse all)
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.13
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.074
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
4.38
Km
42
µM
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
4.06
Km
87
µM
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.171
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
Vmax
0.46
nmol/min/mg protein
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
3.78
Km
165
µM
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
3.54
Km
290
µM
Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465
Title/Abstract Full Text View citing articles Show Details
1
Rate
NA
Cytochrome P450 2D6 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
1
Rate
NA
Cytochrome P450 2E1 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kilicarslan, Tansel; Haining, Robert L.; Rettie, Allan E.; Busto, Usanda; Tyndale, Rachel F.; Sellers, Edward M.
Drug Metabolism and Disposition, 2001 , vol. 29, # 4 I p. 460 - 465 Title/Abstract Full Text View citing articles Show Details
nH
2
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
nH
2.7
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
nH
1.8
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
nH
2.6
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
S50
249
µM
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
S50
286
µM
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Vmax
5.9
nmol/h/mg protein
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
Cytochrome P450 1A2 [human]:Wild + Cytochrome P450 2C19 [human]:Wild + Cytochrome P450 3A4 [human]:Wild
liver
1.25000 mg/kg
Psychopharmacology, 1987...
Title/Abstract Full Text Show Details
1.25000 mg/kg
Psychopharmacology, 1987...
Title/Abstract Full Text Show Details
plasma
5
Molecular Pharmacology, ...
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
Vmax
42.4
nmol/h/mg protein
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
S50
313
µM
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
S50
201
µM
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
Vmax
21.8
nmol/h/mg protein
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
Vmax
101
nmol/h/mg protein
Microsome
25 µM
Xenobiotica, 1999 , vol...
Title/Abstract Full Text View citing articles Show Details
Coller; Somogyi; Bochner
Xenobiotica, 1999 , vol. 29, # 10 p. 973 - 986 Title/Abstract Full Text View citing articles Show Details
BB ratio
1.15
Arendt; Greenblatt; Liebisch; Luu; Paul
Psychopharmacology, 1987 , vol. 93, # 1 p. 72 - 76 Title/Abstract Full Text Show Details
fu
0.193
Arendt; Greenblatt; Liebisch; Luu; Paul
Psychopharmacology, 1987 , vol. 93, # 1 p. 72 - 76 Title/Abstract Full Text Show Details
fu
0.166
µg/mL
Title/Abstract Full Text View citing articles Show Details
Lucek; Coutinho
Molecular Pharmacology, 1976 , vol. 12, # 4 p. 612 - 619 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
<
10
%
Cytochrome P450 3A [human]:Wild
liver
Microsome
Midazolam
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Zimmerlin, Alfred; Trunzer, Markus; Faller, Bernard
Drug Metabolism and Disposition, 2011 , vol. 39, # 6 p. 1039 - 1046 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
<
20
%
Cytochrome P450 [human]:Wild
liver
Cytosol
Naltrexone hydrochloride+Naltrexone hydrochloride
100 µM
0 µM
British Journal of Clini...
Title/Abstract Full Text View citing articles Show Details
Porter; Somogyi; White
British Journal of Clinical Pharmacology, 2000 , vol. 50, # 5 p. 465 - 471 Title/Abstract Full Text View citing articles Show Details
2.72
Km
1920.5
µM
Cytochrome P450 2A6 [human]:Wild
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
3.53
Km
297.5
µM
Cytochrome P450 2A6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
0.13
pmol/min/pmol target
Cytochrome P450 2A6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
1
pmol/min/pmol target
Cytochrome P450 2A6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
0.44
nL/min/pmol target
Cytochrome P450 2A6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
0.52
nL/min/pmol target
Cytochrome P450 2A6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
3.81
Km
154.6
µM
Cytochrome P450 3A4 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
3.54
Km
285.7
µM
Cytochrome P450 3A4 [human]:Wild
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
1.54
pmol/min/pmol target
Cytochrome P450 3A4 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
15.7
pmol/min/pmol target
Cytochrome P450 3A4 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
54.95
nL/min/pmol target
Cytochrome P450 3A4 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
9.96
nL/min/pmol target
Cytochrome P450 3A4 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
4
Km
100.7
µM
Cytochrome P450 2B6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
0.27
pmol/min/pmol target
Cytochrome P450 2B6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
2.68
nL/min/pmol target
Cytochrome P450 2B6 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
4.22
Km
59.6
µM
Cytochrome P450 2C19 [human]:Wild
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Vmax
0.83
pmol/min/pmol target
Cytochrome P450 2C19 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
13.93
nL/min/pmol target
Cytochrome P450 2C19 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
4.3
Km
50.2
µM
Cytochrome P450 2C9 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
0.38
pmol/min/pmol target
Cytochrome P450 2C9 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
7.57
nL/min/pmol target
Cytochrome P450 2C9 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
3.59
Km
256.8
µM
Cytochrome P450 3A4 [human]:Wild
liver
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
3.68
Km
207.6
µM
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
3671.9
pmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
478.9
pmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
2.56
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Clint
13.69
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
nH
1.4
Cytochrome P450 3A4 [human]:Wild
AHH-1 TK+/cell line
Microsome
AHH-1 TK+/cell line
Microsome
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
nH
2.7
Cytochrome P450 2C9 [human]:Wild
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
nH
1.2
Cytochrome P450 3A4 [human]:Wild
liver
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
nH
1.7
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
0 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hesse, Leah M.; Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Shader, Richard I.; Greenblatt, David J.
Drug Metabolism and Disposition, 2001 , vol. 29, # 2 p. 133 - 140 Title/Abstract Full Text View citing articles Show Details
Vmax
0.019
nmol/min/1e6 cells
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858 Title/Abstract Full Text View citing articles Show Details
Vmax
0.14
nmol/min/1e6 cells
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858 Title/Abstract Full Text View citing articles Show Details
S50
66
µM
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858 Title/Abstract Full Text View citing articles Show Details
nH
2.1
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858
Title/Abstract Full Text View citing articles Show Details
4.37
Km
43
µM
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858 Title/Abstract Full Text View citing articles Show Details
Clint
0.442
µL/min/1e6 cells
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Rawden, Helen C.; Hakooz, Nancy; Houston, J. Brian
Drug Metabolism and Disposition, 2005 , vol. 33, # 12 p. 1852 - 1858 Title/Abstract Full Text View citing articles Show Details
3.72
Ki
0.19
mM
UDPglucuronosyltransferase [human]:Wild
liver
Microsome
Zidovudine
0 mM
Biochemical Pharmacology...
Title/Abstract Full Text Show Details
plasma
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Macleod; Eagling; Sim; Back
Biochemical Pharmacology, 1992 , vol. 43, # 2 p. 382 - 386 Title/Abstract Full Text Show Details
fu
0.21
Votano, Joseph R.; Parham, Marc; Hall, L. Mark; Hall, Lowell H.; Kier, Lemont B.; Oloff, Scott; Tropsha, Alexander
Journal of Medicinal Chemistry, 2006 , vol. 49, # 24 p. 7169 - 7181 Title/Abstract Full Text View citing articles Show Details
4.28
Ki
52
µM
UDPglucuronosyltransferase 2B7*2 [human]:Wild
HEK293 cell line
Membrane
4-Hydroxy-Estrone
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.21
Ki
61
µM
UDPglucuronosyltransferase 2B7*2 [human]:Wild
HEK293 cell line
Membrane
4-Hydroxyestradiol
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.33
Ki
47
µM
UDPglucuronosyltransferase 2B7*2 [human]:Wild
HEK293 cell line
Membrane
Nalorphine
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.03
Ki
93
µM
UDPglucuronosyltransferase 2B7*2 [human]:Wild
HEK293 cell line
Membrane
Buprenorphine
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
3.69
Ki
206
µM
UDPglucuronosyltransferase 1-1 [human]:Wild
HEK293 cell line
Membrane
Buprenorphine
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
3.09
Ki
808
µM
UDPglucuronosyltransferase
HEK293 cell line
Membrane
2-Hydroxy-Estrone
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
1-1 [human]:Wild
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
3.4
Ki
402
µM
UDPglucuronosyltransferase 1-1 [human]:Wild
HEK293 cell line
Membrane
2-Hydroxyestradiol
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
1
Ki
NA
UDPglucuronosyltransferase 1-3 [human]:Wild
HEK293 cell line
Homogenate
Buprenorphine
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.66
Ki
22
µM
UDPglucuronosyltransferase 1-3 [human]:Wild
HEK293 cell line
Homogenate
2-Hydroxy-Estrone
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.52
Ki
30
µM
UDPglucuronosyltransferase 1-3 [human]:Wild
HEK293 cell line
Homogenate
2-Hydroxyestradiol
Toxicological Sciences, ...
Title/Abstract Full Text View citing articles Show Details
Cheng, Ziqiang; Rios, Gladys R.; King, Christopher D.; Coffman, Birgit L.; Green, Mitchell D.; Mojarrabi, Behnaz; Mackenzie, Peter I.; Tephly, Thomas R.
Toxicological Sciences, 1998 , vol. 45, # 1 p. 52 - 57 Title/Abstract Full Text View citing articles Show Details
4.6
Ki
25
µM
UDPglucuronosyltransferase 2B7 [human]:Wild
HEK293 cell line
Membrane
Morphine
Drug metabolism and disp...
Title/Abstract Full Text Show Details
HEK293 cell line
Membrane
[14C]-Zidovudine
Drug metabolism and disp...
Title/Abstract Full Text Show Details
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Rios, Gladys R; Tephly, Thomas R
Drug metabolism and disposition: the biological fate of chemicals, 2002 , vol. 30, # 12 p. 1364 - 1367 Title/Abstract Full Text Show Details
4.51
Ki
31
µM
UDPglucuronosyltransferase 2B7 [human]:Wild
Rios, Gladys R; Tephly, Thomas R
Drug metabolism and disposition: the biological fate of chemicals, 2002 , vol. 30, # 12 p. 1364 - 1367 Title/Abstract Full Text Show Details
Blood/Plasma ratio
0.78
blood
Brown, Hayley S.; Griffin, Michael; Houston, J. Brian
Drug Metabolism and Disposition, 2007 , vol. 35, # 2 p. 293 - 301 Title/Abstract Full Text View citing articles Show Details
Vmax
0.2
pmol/min/pmol target
Cytochrome P450 3A4 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Vmax
1.29
pmol/min/pmol target
Cytochrome P450 3A4 [human]:Wild
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
S50
694
mM
Cytochrome P450 3A4 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4
Microsome
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
S50
224
mM
Cytochrome P450 3A4 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clmax
0.9
mL/min/nmol target
Cytochrome P450 3A4 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clmax
5.7
mL/min/nmol target
Cytochrome P450 3A4 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Alpha
0.03
Cytochrome P450 3A4 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Alpha
0.36
Cytochrome P450 3A4 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Vmax
0.14
pmol/min/pmol target
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Vmax
2.38
pmol/min/pmol target
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
S50
337
mM
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clmax
13.4
mL/min/nmol target
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
cell line
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Km
128
mM
Cytochrome P450 3A5 [human]:Wild
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
BTI-Tn5B1-4 cell line
Microsome
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clint
1.09
mL/min/nmol target
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Alpha
0.07
Cytochrome P450 3A5 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Vmax
0.064
pmol/min/pmol target
Cytochrome P450 2C19 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Vmax
0.5
pmol/min/pmol target
Cytochrome P450 2C19 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clint
0.72
mL/min/nmol target
Cytochrome P450 2C19 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Clint
1.7
mL/min/nmol target
Cytochrome P450 2C19 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
Beta
0.28
Cytochrome P450 2C19 [human]:Wild
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
1.05
Km
89
mM
Cytochrome P450 2C19 [human]:Wild
Galetin, Aleksandra; Brown, Caroline; Hallifax, David; Ito, Kiyomi; Houston, J. Brian
10 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1411 - 1420 Title/Abstract Full Text View citing articles Show Details
4.22
% Inhibition
62.6
%
UDPglucuronosyltransferase 1-3 [human]:Wild + UDPglucuronosyltransferase 2B15 [human]:Wild + UDPglucuronosyltransferase 1-1 [human]:Wild
liver
Microsome
[14C]-Ezetimibe
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
4.49
% Inhibition
86.1
%
UDPglucuronosyltransferase 1-3 [human]:Wild + UDPglucuronosyltransferase 2B15 [human]:Wild + UDPglucuronosyltransferase 1-1 [human]:Wild
liver
Microsome
[14C]-Ezetimibe
200 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
3.74
% Inhibition
35.7
%
UDPglucuronosyltransferase 1-3 [human]:Wild + UDPglucuronosyltransferase 2B15 [human]:Wild + UDPglucuronosyltransferase 1-1 [human]:Wild
jejunum
Microsome
[14C]-Ezetimibe
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
3.74
% Inhibition
52.6
%
UDPglucuronosyltransferase 1-3 [human]:Wild + UDPglucuronosyltransferase 2B15 [human]:Wild + UDPglucuronosyltransferase 1-1 [human]:Wild
jejunum
Microsome
[14C]-Ezetimibe
200 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
1
% Inhibition
21.3
%
UDPglucuronosyltransferase 2B7 [human]:Wild
jejunum
Microsome
[14C]-Ezetimibe
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
3.6
% Inhibition
44.2
%
UDPglucuronosyltransferase 2B7 [human]:Wild
jejunum
Microsome
[14C]-Ezetimibe
200 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
4.38
% Inhibition
82.8
%
UDPglucuronosyltransferase 2B7 [human]:Wild
cells
Microsome
[14C]-Ezetimibe
200 µM
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
4.98
% Inhibition
96.9
%
UDPglucuronosyltransferase 2B15 [human]:Wild
cells
Microsome
[14C]-Ezetimibe
200 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Ghosal, Anima; Hapangama, Neil; Yuan, Yuan; Achanfuo-Yeboah, Joana; Iannucci, Robert; Chowdhury, Swapan; Alton, Kevin; Patrick, James E.; Zbaida, Shmuel
Drug Metabolism and Disposition, 2004 , vol. 32, # 3 p. 314 - 320 Title/Abstract Full Text View citing articles Show Details
4.28
% Inhibition
49
%
Aldehyde oxidase [human]:Wild
liver
Cytosol
Phthlazine
50 µM
Journal of Clinical Phar...
Title/Abstract Full Text View citing articles Show Details
Obach, R. Scott; Huynh, Phuong; Allen, Mary C.; Beedham, Christine
Journal of Clinical Pharmacology, 2004 , vol. 44, # 1 p. 7 - 19 Title/Abstract Full Text View citing articles Show Details
Fold-increase
1.41
Cytochrome P450 3A4 [human]:Wild
7-Benzyloxy-4trifluoromethylcoumarin
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kumar, Santosh; Qiu, Huan; Oezguen, Numan; Herlyn, Holger; Halpert, James R.; Wojnowski, Leszek
Drug Metabolism and Disposition, 2009 , vol. 37, # 6 p. 1328 - 1333 Title/Abstract Full Text View citing articles Show Details
Fold-increase
1.55
Cytochrome P450 3A4 [chimpanzee]:Wild
7-Benzyloxy-4trifluoromethylcoumarin
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Kumar, Santosh; Qiu, Huan; Oezguen, Numan; Herlyn, Holger; Halpert, James R.; Wojnowski, Leszek
Drug Metabolism and Disposition, 2009 , vol. 37, # 6 p. 1328 - 1333 Title/Abstract Full Text View citing articles Show Details
Vmax
0.4
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Vmax
7.1
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
S50
300
µM
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
S50
174
µM
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
1.4
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
12
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
0.08
µL/min/pmol target
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
0.1
µL/min/nmol target
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Vmax
0.007
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Vmax
0.17
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
S50
458
µM
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
S50
293
µM
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
0.01
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
0.19
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Clmax
0.004
µL/min/pmol target
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229
Title/Abstract Full Text View citing articles Show Details
Clmax
0.012
µL/min/pmol target
Cytochrome P450 3A4 [human]:Wild
intestine
Microsome
1 µM
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
Vmax
64
pmol/min/1e6 cells
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
Vmax
11
pmol/min/1e6 cells
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
nH
1.4
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
fu
0.94
intestine
Microsome
Journal of Pharmacology ...
Title/Abstract Full Text View citing articles Show Details
Galetin, Aleksandra; Houston, J. Brian
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 3 p. 1220 - 1229 Title/Abstract Full Text View citing articles Show Details
nH
1.7
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
S50
76
µM
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
S50
130
µM
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
% Pathway
>
75
%
Cytochrome P450 3A4 [human]:Wild
liver
liver cell
1 µM
Xenobiotica, 2008 , vol...
Title/Abstract Full Text View citing articles Show Details
Hallifax; Galetin; Houston
Xenobiotica, 2008 , vol. 38, # 4 p. 353 - 367 Title/Abstract Full Text View citing articles Show Details
Vmax
0.29
nmol/min/mg
Cytochrome P450 3A4
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
protein
[human]:Wild
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
Vmax
3.2
nmol/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
3.61
Km
248
µM
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
3.68
Km
208
µM
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
nH
1.9
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
nH
1.6
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
Clmax
0.71
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
Clmax
5.3
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
Clint
1.394
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
Clint
12.9
µL/min/mg protein
Cytochrome P450 3A4 [human]:Wild
liver
Microsome
10 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
fu
0.94
liver
Microsome
1 µM
Xenobiotica, 2005 , vol...
Title/Abstract Full Text View citing articles Show Details
Rawden; Carlile; Tindall; Hallifax; Galetin; Ito; Houston
Xenobiotica, 2005 , vol. 35, # 6 p. 603 - 625 Title/Abstract Full Text View citing articles Show Details
5.24
EC50
=
5.7
µM
Cytochrome P450 2B2 [Rattus norvegicus]:Wild
Cytochrome P450 3A5:Wild
liver cell
Biochemical Pharmacology...
Title/Abstract Full Text View citing articles Show Details
Roberge, Christian; Beaudet, Marie-Josee; Anderson, Alan
Biochemical Pharmacology, 2004 , vol. 68, # 7 p. 1383 - 1389 Title/Abstract Full Text View citing articles Show Details
Ratio
1.8
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Clint
0.9
µL/min/nmol P450 all
Cytochrome P450 3A4:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Activity
0.32
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Lin, Jiunn H.
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 46 - 59 Title/Abstract Full Text View citing articles Show Details
Clint
5.7
µL/min/nmol P450 all
Cytochrome P450 3A4:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
3.47
Km
=
337
µM
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Clint
1.09
µL/min/nmol P450 all
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Ratio
0.7
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Ratio
1.2
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Clint
13.4
µL/min/nmol P450 all
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
3.89
Km
=
128
µM
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
3.65
Km
=
224
µM
Cytochrome P450 3A4:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Ratio
0.57
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Ratio
0.49
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Ratio
2.4
Cytochrome P450 3A5:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
3.16
Km
=
694
µM
Cytochrome P450 3A4:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
4.36
Km
43.8
µM
Cytochrome P450 3A5 [human]:Wild
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
4.45
Km
35.6
µM
Cytochrome P450 3A4 [human]:Wild
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
3.97
Km
106
µM
Cytochrome P450 3A4 [human]:Wild
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
4.31
Km
49.3
µM
Cytochrome P450 3A5 [human]:Wild
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
t1/2 el
25.5
hour
Clarke's Analysis of Dru...
Full Text Show Details
%
Clarke's Analysis of Dru...
Full Text Show Details
hour
Clarke's Analysis of Dru...
Full Text Show Details
Clarke's Analysis of Dru...
Full Text Show Details
L/kg
Clarke's Analysis of Dru...
Full Text Show Details
mL/min/kg
Archives of Pharmacal Re...
Title/Abstract Full Text View citing articles Show Details
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Protein binding (%)
78.5
Clarke's Analysis of Drugs and Poisons Full Text Show Details
t1/2 el
3
Clarke's Analysis of Drugs and Poisons Full Text Show Details
F(%)
@
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Vd
4.5
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Cl
=
7.18
Lee, Soyoung; Kim, Dongsup
Archives of Pharmacal Research, 2007 , vol. 30, # 2 p. 182 - 190 Title/Abstract Full Text View citing articles Show Details
Cl
=
79.17
mL/min/kg
Archives of Pharmacal Re...
Title/Abstract Full Text View citing articles Show Details
Lee, Soyoung; Kim, Dongsup
Archives of Pharmacal Research, 2007 , vol. 30, # 2 p. 182 - 190 Title/Abstract Full Text View citing articles Show Details
Cl
=
70.59
mL/min/kg
Archives of Pharmacal Re...
Title/Abstract Full Text View citing articles Show Details
Lee, Soyoung; Kim, Dongsup
Archives of Pharmacal Research, 2007 , vol. 30, # 2 p. 182 - 190 Title/Abstract Full Text View citing articles Show Details
Cl
=
4.03
mL/min/kg
Archives of Pharmacal Re...
Title/Abstract Full Text View citing articles Show Details
Lee, Soyoung; Kim, Dongsup
Archives of Pharmacal Research, 2007 , vol. 30, # 2 p. 182 - 190 Title/Abstract Full Text View citing articles Show Details
Clint
=
12.7
mL/min/kg
liver cell
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Turlizzi, Elisa; Zanelli, Ugo; Houston, J. Brian
European Journal of Pharmaceutical Sciences, 2012 , vol. 45, # 5 p. 570 - 574 Title/Abstract Full Text View citing articles Show Details
Papp (transport)
=
8.55E06
cm/s
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Turlizzi, Elisa; Zanelli, Ugo; Houston, J. Brian
European Journal of Pharmaceutical Sciences, 2012 , vol. 45, # 5 p. 570 - 574 Title/Abstract Full Text View citing articles Show Details
Clint
=
4.5
mL/min/kg
liver cell
European Journal of Phar...
Title/Abstract Full Text View citing articles Show Details
Hallifax, David; Turlizzi, Elisa; Zanelli, Ugo; Houston, J. Brian
European Journal of Pharmaceutical Sciences, 2012 , vol. 45, # 5 p. 570 - 574 Title/Abstract Full Text View citing articles Show Details
Protein binding (%)
78
%
Goodman & Gilman's The P...
Full Text Show Details
Goodman & Gilman's The P...
Full Text Show Details
Current Medicinal Chemis...
Title/Abstract Full Text View citing articles Show Details
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
t1/2 el
15
hour
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
%
10 - 15
%
Cytochrome P450 2C9 [human]:Wild
He; Zhou; Li
Current Medicinal Chemistry, 2011 , vol. 18, # 5 p. 667 - 713 Title/Abstract Full Text View citing articles Show Details
Cl
=
3.5
mL/min/g
Mini reviews in medicina...
Title/Abstract Full Text View citing articles Show Details
Quinones-Torrelo; Martin-Biosca; Martinez-Pla; Sagrado; Villanueva-Camanas; Medina-Hernandez
Mini reviews in medicinal chemistry, 2002 , vol. 2, # 2 p. 145 - 161 Title/Abstract Full Text View citing articles Show Details
Vd
=
3.3
L/kg
Mini reviews in medicina...
Title/Abstract Full Text View citing articles Show Details
Quinones-Torrelo; Martin-Biosca; Martinez-Pla; Sagrado; Villanueva-Camanas; Medina-Hernandez
Mini reviews in medicinal chemistry, 2002 , vol. 2, # 2 p. 145 - 161 Title/Abstract Full Text View citing articles Show Details
%
=
0
%
Mini reviews in medicina...
Title/Abstract Full Text View citing articles Show Details
Quinones-Torrelo; Martin-Biosca; Martinez-Pla; Sagrado; Villanueva-Camanas; Medina-Hernandez
Mini reviews in medicinal chemistry, 2002 , vol. 2, # 2 p. 145 - 161 Title/Abstract Full Text View citing articles Show Details
Log BB
0.06
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Platts, James A.; Abraham, Michael H.; Zhao, Yuan H.; Hersey, Anne; Ijaz, Luke; Butina, Darko
European Journal of Medicinal Chemistry, 2001 , vol. 36, # 9 p. 719 - 730 Title/Abstract Full Text View citing articles Show Details
Cl
=
47.04
mL/min/kg
plasma cell
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Wan, Hong; Bold, Peter; Larsson, Lars-Olof; Ulander, Johan; Peters, Sheila; Loefberg, Boel; Ungell, Anna-Lena; Nagard, Mats; Llinas, Antonio
Current Drug Metabolism, 2010 , vol. 11, # 7 p. 583 - 594 Title/Abstract Full Text View citing articles Show Details
Activity
1
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Wan, Hong; Bold, Peter; Larsson, Lars-Olof; Ulander, Johan; Peters, Sheila; Loefberg, Boel; Ungell, Anna-Lena; Nagard, Mats; Llinas, Antonio
Current Drug Metabolism, 2010 , vol. 11, # 7 p. 583 - 594 Title/Abstract Full Text View citing articles Show Details
Clint
=
240
mL/min/kg
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Wan, Hong; Bold, Peter; Larsson, Lars-Olof; Ulander, Johan; Peters, Sheila; Loefberg, Boel; Ungell, Anna-Lena; Nagard, Mats; Llinas, Antonio
Current Drug Metabolism, 2010 , vol. 11, # 7 p. 583 - 594 Title/Abstract Full Text View citing articles Show Details
fu
0.25
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Wan, Hong; Bold, Peter; Larsson, Lars-Olof; Ulander, Johan; Peters, Sheila; Loefberg, Boel; Ungell, Anna-Lena; Nagard, Mats; Llinas, Antonio
Current Drug Metabolism, 2010 , vol. 11, # 7 p. 583 - 594 Title/Abstract Full Text View citing articles Show Details
BB ratio
1.2
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Wan, Hong; Bold, Peter; Larsson, Lars-Olof; Ulander, Johan; Peters, Sheila; Loefberg, Boel; Ungell, Anna-Lena; Nagard, Mats; Llinas, Antonio
Current Drug Metabolism, 2010 , vol. 11, # 7 p. 583 - 594 Title/Abstract Full Text View citing articles Show Details
Ratio
0.54
plasma cell
European Journal of Medi...
Title/Abstract Full Text View citing articles Show Details
Fatemi, Mohammad H.; Ghorbanzad'E, Mehdi
European Journal of Medicinal Chemistry, 2010 , vol. 45, # 11 p. 5051 - 5055 Title/Abstract Full Text View citing articles Show Details
% Inhibition
10 - 15
%
Inhibitor
Cytochrome P450 2C9 [human]:Wild
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Mo, Sui-Lin; Zhou, Zhi-Wei; Yang, Li-Ping; Wei, Ming Qian; Zhou, Shu-Feng
Current Drug Metabolism, 2009 , vol. 10, # 10 p. 1075 - 1126 Title/Abstract Full Text View citing articles Show Details
Vd
=
4.58
L/kg
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Sui, Xiaofan; Sun, Jin; Wu, Xin; Li, Haiyan; Liu, Jianfang; He, Zhonggui
Current Drug Metabolism, 2008 , vol. 9, # 6 p. 574 - 580 Title/Abstract Full Text View citing articles Show Details
Vd
=
13
L/kg
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Sui, Xiaofan; Sun, Jin; Wu, Xin; Li, Haiyan; Liu, Jianfang; He, Zhonggui
Current Drug Metabolism, 2008 , vol. 9, # 6 p. 574 - 580 Title/Abstract Full Text View citing articles Show Details
3.97
% Inhibition
48
%
Carboxylesterase 1 [human]:Wild
Sf21 cell line
4-Nitrophenyl acetate
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Shimizu, Mai; Fukami, Tatsuki; Nakajima, Miki; Yokoi, Tsuyoshi
Drug Metabolism and Disposition, 2014 , vol. 42, # 7 p. 1103 - 1109 Title/Abstract Full Text View citing articles Show Details
3.86
% Inhibition
42
%
Carboxylesterase 2 [human]:Wild
Sf21 cell line
4-Nitrophenyl acetate
100 µM
Drug Metabolism and Disp...
Title/Abstract Full Text View citing articles Show Details
Shimizu, Mai; Fukami, Tatsuki; Nakajima, Miki; Yokoi, Tsuyoshi
Drug Metabolism and Disposition, 2014 , vol. 42, # 7 p. 1103 - 1109 Title/Abstract Full Text View citing articles Show Details
4.82
% Inhibition
92.9
%
Inhibitor
Solute carrier family 22 member 5 [human]:Wild
HEK293 cell line
metformin
200 μM
PLoS ONE, 2015 , vol. 1...
Title/Abstract Full Text View citing articles Show Details
Hacker, Kristina; Maas, Renke; Kornhuber, Johannes; Fromm, Martin F.; Zolk, Oliver
PLoS ONE, 2015 , vol. 10, # 9 art. no. E0136451 Title/Abstract Full Text View citing articles Show Details
5.16
% Inhibition
74.1
%
Inhibitor
Solute carrier family 22 member 5 [human]:Wild
HEK293 cell line
metformin
20 μM
Hacker, Kristina; Maas, Renke; Kornhuber, Johannes; Fromm, Martin F.; Zolk, Oliver
PLoS ONE, 2015 , vol. 10, # 9 art. no. E0136451 Title/Abstract Full Text View citing articles Show Details
Qualitative Information 1 of 12
2 of 12
3 of 12
Target
Cytochrome P450 3A5:Wild
Assay Description
Maximal velocity of the compound for N-Demethylation reaction mediated by Cytochrome P450 3A5 from Baculovirus-infected insect cells
Results
Vmax not calculated
Citation
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A4:Wild
Assay Description
Maximal velocity of the compound for N-Demethylation reaction mediated by Cytochrome P450 3A4 from Baculovirus-infected insect cells
Results
Vmax not calculated
Citation
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A5:Wild
Assay Description
Maximal velocity of the compound for 3-Hydroxylation reaction mediated by Cytochrome P450 3A5 from Baculovirus-infected insect cells
Results
Vmax not calculated
PLoS ONE, 2015 , vol. 1...
Title/Abstract Full Text View citing articles Show Details
4 of 12
5 of 12
6 of 12
7 of 12
8 of 12
Citation
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A4:Wild
Assay Description
Maximal velocity of the compound for 3-Hydroxylation reaction mediated by Cytochrome P450 3A4 from Baculovirus-infected insect cells
Results
Vmax not calculated
Citation
Niwa, Toshiro; Murayama, Norie; Emoto, Chie; Yamazaki, Hiroshi
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 20 - 33 Title/Abstract Full Text View citing articles Show Details
Assay Description
Distribution coefficient of the compound at PH 7.4 (LOG D7.4)
Citation
Benet, Leslie Z.; Broccatelli, Fabio; Oprea, Tudor I.
AAPS Journal, 2011 , vol. 13, # 4 p. 519 - 547 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A4 [human]:Wild
Biological material
human
Assay Description
Maximum velocity for CYP3A4 catalyzed 3-hydroxyflunitrazepam formation in human liver microsomes
Results
19.3
Citation
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A5 [human]:Wild
Biological material
human
Assay Description
Maximum velocity for CYP3A5 catalyzed 3-hydroxyflunitrazepam formation in human liver microsomes
Results
3.85
Citation
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
Target
Cytochrome P450 3A4 [human]:Wild
Biological material
human
Assay Description
Maximum velocity for CYP3A4 catalyzed N-desmethylflunitrazepam formation in human liver microsomes
Results
0.550
Citation
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
9 of 12
10 of 12
11 of 12
12 of 12
Target
Cytochrome P450 3A5 [human]:Wild
Biological material
human
Assay Description
Maximum velocity for CYP3A5 catalyzed N-desmethylflunitrazepam formation in human liver microsomes
Results
0.217
Citation
Huang, Weili; Lin, Yvonne S.; McConn II, Donavon J.; Calamia, Justina C.; Totah, Rheem A.; Isoherranen, Nina; Glodowski, Mary; Thummel, Kenneth E.
Drug Metabolism and Disposition, 2004 , vol. 32, # 12 p. 1434 - 1445 Title/Abstract Full Text View citing articles Show Details
Assay Description
Partition Coefficient of the compound was determined
Citation
Alelyunas, Yun W.; Empfield, James R.; McCarthy, Dennis; Spreen, Russell C.; Bui, Khanh; Pelosi-Kilby, Luciana; Shen, Cindy
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7312 - 7316 Title/Abstract Full Text View citing articles Show Details
Assay Description
Partition Coefficient of the compound was determined
Citation
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
Assay Description
Partition Coefficient of the compound was determined
Citation
Dimitra Hadjipavlou-Litina; Corwin Hansch
Chemical reviews, 1994 , vol. 94, # 6 p. 1483 - 1505 Title/Abstract Full Text Show Details
Pharmacokinetic (56) Quantitative Results pX
Parameter
Value (qual)
Value (quant)
Unit
Biological Species
Route of administration
Dose
Dosing regimen
Population
Reference (expand all/collapse all)
Fa(%)
90
%
human
Single
Healthy
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Bergstroem, Christel A. S.; Strafford, Melissa; Lazorova, Lucia; Avdeef, Alex; Luthman, Kristina; Artursson, Per
Journal of Medicinal Chemistry, 2003 , vol. 46, # 4 p. 558 - 570 Title/Abstract Full Text View citing articles Show Details
Cmax
6
ng/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Concentration
0.4
ng/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Tmax
1
hour
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
AUC
57
ng.h/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 el
16
hour
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Cmax
6
ng/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Concentration
0.4
ng/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Tmax
1
hour
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
AUC
57
ng.h/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 el
16
hour
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
AUC i/AUC
1.28
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 el i/t1/2 el
1.56
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122
Title/Abstract Full Text View citing articles Show Details
Cmax i/Cmax
1.17
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Concentration i/Concentration
1.75
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
AUC i/AUC
1.25
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 el i/t1/2 el
2
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Cmax
7
ng/mL
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Concentration
0.7
ng/mL
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
Tmax
2
hour
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
pX
Parameter AUC
Value (qual)
Value (quant)
Unit
Biological Species
Route of administration
Dose
Dosing regimen
Population
Reference (expand all/collapse all)
73
ng.h/mL
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
human
oral administration
1 mg
Single
Non Smoker
Pharmacology and Toxicol...
Title/Abstract Full Text View citing articles Show Details
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 el
25
hour
Luurila, Harri; Olkkola, Klaus T.; Neuvonen, Pertti J.
Pharmacology and Toxicology, 1996 , vol. 78, # 2 p. 117 - 122 Title/Abstract Full Text View citing articles Show Details
t1/2 abs
0.144
hour
Human Caucasian
oral administration
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Repeated
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Repeated
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Repeated
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Repeated
Healthy
Journal of Pharmacokinet...
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Tlag
0.266
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
t1/2 [lambda1]
2.07
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
t1/2 el
13.5
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Cl/F
0.278
L/h/kg
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Vd ss/F
4.44
L/kg
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Blood/Serum ratio
0.75
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
t1/2 abs
1.47
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
t1/2 [lambda1]
1.9
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
t1/2 el
19.2
hour
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Cl/F
0.278
L/h/kg
Human Caucasian
oral administration
Title/Abstract Full Text Show Details
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Vd/F
5.63
L/kg
Human Caucasian
oral administration
2 mg
Repeated
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
2 mg
Single
Healthy
Journal of Pharmacokinet...
Title/Abstract Full Text Show Details
oral administration
2 mg
Single
Healthy
British Journal of Clini...
Title/Abstract Full Text Show Details
oral administration
2 mg
Single
Healthy
British Journal of Clini...
Title/Abstract Full Text Show Details
intravenous administration
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
ClH
0.235
L/h/kg
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
ER
0.154
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
Vd ss
3.76
L/kg
Human Caucasian
oral administration
Boxenbaum; Posmanter; Macasieb; Geitner; Weinfeld; Moore; Darragh; O'Kelly; Weissman; Kaplan
Journal of Pharmacokinetics and Biopharmaceutics, 1978 , vol. 6, # 4 p. 283 - 293 Title/Abstract Full Text Show Details
kel
0.031
h-1
human
Dorow; Seidler; Schneider
British Journal of Clinical Pharmacology, 1982 , vol. 13, # 4 p. 561 - 565 Title/Abstract Full Text Show Details
t1/2 el
23
hour
human
Dorow; Seidler; Schneider
British Journal of Clinical Pharmacology, 1982 , vol. 13, # 4 p. 561 - 565 Title/Abstract Full Text Show Details
CSF/Plasma ratio
0.34
domestic cat
Lin, Jiunn H.
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 46 - 59 Title/Abstract Full Text View citing articles Show Details
Tmax
=
8.3
minute
domestic cat
intravenous administration
Current Drug Metabolism,...
Title/Abstract Full Text View citing articles Show Details
Lin, Jiunn H.
Current Drug Metabolism, 2008 , vol. 9, # 1 p. 46 - 59 Title/Abstract Full Text View citing articles Show Details
Ue (%)
=
0.5
%
human
oral administration
AAPS Journal, 2011 , vo...
Title/Abstract Full Text View citing articles Show Details
Benet, Leslie Z.; Broccatelli, Fabio; Oprea, Tudor I.
AAPS Journal, 2011 , vol. 13, # 4 p. 519 - 547 Title/Abstract Full Text View citing articles Show Details
F(%)
>
80
%
oral administration
Journal of Medicinal Che...
Title/Abstract Full Text View citing articles Show Details
Yoshida, Fumitaka; Topliss, John G.
Journal of Medicinal Chemistry, 2000 , vol. 43, # 13 p. 2575 - 2585 Title/Abstract Full Text View citing articles Show Details
Concentration
0.0015
µg/mL
human
Clarke's Analysis of Dru...
Full Text Show Details
0.002
µg/mL
human
Clarke's Analysis of Dru...
Full Text Show Details
0.0025
µg/mL
human
Clarke's Analysis of Dru...
Full Text Show Details
1
hour
human
oral administration
Clarke's Analysis of Dru...
Full Text Show Details
2
mL/min/kg
human
oral administration
Clarke's Analysis of Dru...
Full Text Show Details
10
%
human
Clarke's Analysis of Dru...
Full Text Show Details
1.2
hour
human
oral administration
Goodman & Gilman's The P...
Full Text Show Details
intravenous administration
Goodman & Gilman's The P...
Full Text Show Details
oral administration
Goodman & Gilman's The P...
Full Text Show Details
oral administration
Goodman & Gilman's The P...
Full Text Show Details
oral administration
Medicinal Research Revie...
Title/Abstract Full Text View citing articles Show Details
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Concentration
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Concentration
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Tmax
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Cl
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Ue (%)
Clarke's Analysis of Drugs and Poisons Full Text Show Details
Tmax
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
Vd
3.3
L/kg
human
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
F(%)
85
%
human
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
Cl
3.5
mL/min/kg
human
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
F(%)
=
85
%
Fecik, Robert A.; Frank, Kristine E.; Gentry, Elmer J.; Menon, Sanjay R.; Mitscher, Lester A.; Telikepalli, Hanumaiah
Medicinal Research Reviews, 1998 , vol. 18, # 3 p. 149 - 185 Title/Abstract Full Text View citing articles Show Details
t1/2 el
=
26
hour
human
intravenous administration
Current drug metabolism,...
Title/Abstract Full Text Show Details
Mandrioli, Roberto; Mercolini, Laura; Raggi, Maria Augusta
Current drug metabolism, 2008 , vol. 9, # 8 p. 827 - 844 Title/Abstract Full Text Show Details
Qualitative Information 1 of 1
Biological material
human
Assay Description
Urinary Excretion
Results
<1
Citation
Goodman & Gilman's The Pharmacological Basis of Therapeutics, 9th ed., 1996, 1996 Full Text Show Details
Toxicity/Safety Pharmacology (18) Quantitative Results pX
Parameter
Value (qual)
Value (quant)
Unit
Action on Target
Target
Tissue/Organ
Cell
Bioassay
Dose
Effect
Reference (expand all/collapse all)
LD50
=
870
mg/kg
Chemical Biology and Dru...
Title/Abstract Full Text View citing articles Show Details
Critical Care Medicine, ...
Title/Abstract Full Text View citing articles Show Details
Kiso to Rinsho Clinical ...
Full Text Show Details
Gekkan Yakuji. Pharmaceu...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Esteki, Mahnaz; Khayamian, Taghi
Chemical Biology and Drug Design, 2008 , vol. 72, # 5 p. 409 - 435 Title/Abstract Full Text View citing articles Show Details
TDLo
3.478
mg/kg
Roald; Dahl
Critical Care Medicine, 1989 , vol. 17, # 12 p. 1355 - 1356 Title/Abstract Full Text View citing articles Show Details
LD50
2.76
mg/kg
Kiso to Rinsho Clinical Report, 1985, 19, 1277, 1985 , vol. 19, p. 1277 Full Text Show Details
TDLo
0.222
mg/kg
Gekkan Yakuji. Pharmaceuticals Monthly.,1996, 38, 2597., 1996 , vol. 38, p. 2597 Full Text Show Details
LD50
2000
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
1060
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
4000
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
2000
mg/kg
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical...
Full Text Show Details
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
1200
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
1050
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
415
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
4000
mg/kg
Kiso to Rinsho. Clinical Report.,1985, 19, 1277., 1985 , vol. 19, p. 1277 Full Text Show Details
LD50
=
415
mg/kg
Kiso to Rinsho, 1985, 19...
Full Text Show Details
mg/kg
Archives of Internal Med...
Title/Abstract Full Text Show Details
Journal of Analytical To...
Title/Abstract Full Text Show Details
Journal of Analytical To...
Title/Abstract Full Text Show Details
Journal of Analytical To...
Title/Abstract Full Text Show Details
Toxic
Journal of Analytical To...
Title/Abstract Full Text Show Details
Kiso to Rinsho, 1985, 19, 1277, 1985 , vol. 19, p. 1277 Full Text Show Details
TDLo
0.127
Hofer; Scollo-Lavizzari
Archives of Internal Medicine, 1985 , vol. 145, # 4 p. 663 - 664 Title/Abstract Full Text Show Details
LDLo
0.007
mg/kg
Heyndrickx
Journal of Analytical Toxicology, 1987 , vol. 11, # 6 p. 278 - 278 Title/Abstract Full Text Show Details
=
430
µg/kg
Heyndrickx
Journal of Analytical Toxicology, 1987 , vol. 11, # 6 p. 278 - 278 Title/Abstract Full Text Show Details
LDLo
0.43
mg/kg
Heyndrickx
Journal of Analytical Toxicology, 1987 , vol. 11, # 6 p. 278 - 278 Title/Abstract Full Text Show Details
TDLo
0.184
mg/kg
Heyndrickx
Journal of Analytical Toxicology, 1987 , vol. 11, # 6 p. 278 - 278 Title/Abstract Full Text Show Details
Identification
Physical Data Spectra Other Data Reaxys Registry Number: 6441871
Type of Substance: heterocyclic Molecular Formula: C16H12FN3O3*H Linear Structure Formula: C16H12FN3O3*H(1+)
no reactions.
Druglikeness
Identification Physical Data (2)
Show Targets
1
Chemical Name: [3H]-flunitrazepam
no reactions.
Druglikeness
Identification
Show Targets
no reactions.
Druglikeness
Identification
Show Targets
1
no reactions.
Druglikeness
Identification Spectra (2)
Show Targets
3
Molecular Weight: 314.296
InChI Key: PPTYJKAXVCCBDU-UHFFFAOYSA-O 3
Synthesize | Show Details Find similar
Reaxys Registry Number: 27883497
Molecular Formula: C16H12FN3O3
Linear Structure Formula: C16H11(3)HFN3O3
4
Molecular Weight: 315.28
InChI Key: PPTYJKAXVCCBDU-CNRUNOGKSA-N
Synthesize | Show Details Find similar Chemical Name: [3H]-flunitrazepam Reaxys Registry Number: 32097874
Molecular Formula: C16H12FN3O3
Linear Structure Formula: C16H11(3)HFN3O3
5
Molecular Weight: 315.28
InChI Key: PPTYJKAXVCCBDU-FIRFLZKJSA-N
Synthesize | Show Details Find similar Chemical Name: flunitrazepam-d7
6
Reaxys Registry Number: 9813319
Type of Substance: heterocyclic Molecular Formula: C16H12FN3O3
Linear Structure Formula: C16H5D7FN3O3
Molecular Weight: 320.232
InChI Key: PPTYJKAXVCCBDU-AAYPNNLASA-N
Synthesize | Show Details Find similar Chemical Name: benzodiazepine flunitrazepam
no reactions.
Druglikeness
Identification
Show Targets
1
no reactions.
Bioactivity
Show Targets
1
Reaxys Registry Number: 32291059
Molecular Formula: C9H8N2*C16H12FN3O3
Linear Structure Formula: C9H8N2*C16H12FN3O3
Molecular Weight: 457.464
InChI Key: ZAXIUWFOWWOOLG-UHFFFAOYSA-N 7
Synthesize | Show Details Find similar
8
Chemical Name: flunitrazepam; poly(ethylene glycol) 200; mixture of
mixture (composition partially given) :
flunitrazepam poly(ethylene glycol) 200
Reaxys Registry Number: 8389175 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms flunitrazepam; poly(ethylene glycol) 200; mixture of Composition
poly(ethylene glycol) 200 (99 weight percent)
flunitrazepam (1 weight percent)
Synthesize
Synthesize
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Find similar
Bioactivity In vivo: Animal Model (1) Qualitative Information 1 of 1
Assay Description
repeated dose toxicity New Zealand/lop ear cross rabbit
Results
no adverse clinical signs of toxicity; no gross pathological findings related to treatment; no microscopic abnormalities in brain; flattening of olfactory epithelium
Citation
Hjortkjaer, Rolf K.; Bechgaard, Erik; Gizurarson, Sveinbjoern; Suzdak, Carol; McDonald; Greenough
Journal of Pharmacy and Pharmacology, 1999 , vol. 51, # 4 p. 377 - 383 Title/Abstract Full Text View citing articles Show Details
9
Chemical Name: flunitrazepam; poly(ethylene glycol) 200; glycofurolum 75; mixture of
mixture (composition partially given) :
flunitrazepam poly(ethylene glycol) 200, 70 percent; glycofurolum 75, 30 percent; mixture of
no reactions.
Bioactivity
Show Targets
1
Reaxys Registry Number: 8389177 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms flunitrazepam; poly(ethylene glycol) 200; glycofurolum 75; mixture of Composition
poly(ethylene glycol) 200, 70 percent; glycofurolum 75, 30 percent; mixture of (99 weight percent)
flunitrazepam (1 weight percent)
Synthesize
Synthesize
Find similar
Find similar
Bioactivity In vivo: Animal Model (1) Qualitative Information 1 of 1
10
Assay Description
repeated dose toxicity New Zealand/lop ear cross rabbit
Results
no adverse clinical signs of toxicity; no gross pathological findings related to treatment; no microscopic abnormalities in brain; inflammatory cells in middle part of nasal cavity; flattening and focal inflammation of olfactory epithelium
Citation
Hjortkjaer, Rolf K.; Bechgaard, Erik; Gizurarson, Sveinbjoern; Suzdak, Carol; McDonald; Greenough
Journal of Pharmacy and Pharmacology, 1999 , vol. 51, # 4 p. 377 - 383 Title/Abstract Full Text View citing articles Show Details
mixture (composition partially given) :
flunitrazepam flumazenil Hide Details
Chemical Name: flunitrazepam; flumazenil; mixture of
no reactions.
Reaxys Registry Number: 8827787 Type of Substance: mixture (composition partially given)
Chemical Names and Synonyms flunitrazepam; flumazenil; mixture of Composition flunitrazepam
flumazenil
Bioactivity
Show Targets
1
Synthesize
Synthesize
Find similar
Find similar
Bioactivity In vitro: Efficacy (1) Qualitative Information 1 of 1
11
Assay Description
expression of α1 subunit protein of GABAA receptor primary cerebellar granule cells from Sprague-Dawley rats Western blotting; optical density readings, ECL=enhanced chemiluminiscence
Results
no change in the expression of the GABAA receptor α1 subunit protein
Citation
Brown, Maria J.; Bristow, David R.
British Journal of Pharmacology, 1996 , vol. 118, # 5 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details
Chemical Name: flunitrazepam; γ-aminobutyric acid; mixture of
mixture (composition partially given) :
flunitrazepam 4-amino-n-butyric acid
no reactions.
Reaxys Registry Number: 8827788 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms flunitrazepam; γ-aminobutyric acid; mixture of Composition
4-amino-n-butyric acid
flunitrazepam
Synthesize
Synthesize
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Bioactivity
Show Targets
1
Bioactivity In vitro: Efficacy (1) Qualitative Information 1 of 1
12
Assay Description
expression of α1 subunit protein of GABAA receptor primary cerebellar granule cells from Sprague-Dawley rats Western blotting; optical density readings, ECL (enhanced chemiluminiscence) detection for GABAamp; receptor protein subunits
Results
decrease in the expression of the GABAA receptor α1 subunit protein, not significantly different from flunitrazepam (1 μM) alone, at a lower doses of flunitrazepam (1 and 10 nM) the downregulation also mirrored the effect of flunitrazepam alone
Citation
Brown, Maria J.; Bristow, David R.
British Journal of Pharmacology, 1996 , vol. 118, # 5 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details
Chemical Name: flunitrazepam; bicuculline; mixture of
mixture (composition partially given) :
bicuculline flunitrazepam
no reactions.
Reaxys Registry Number: 8827790 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms flunitrazepam; bicuculline; mixture of Composition
flunitrazepam
bicuculline
Synthesize
Synthesize
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Bioactivity In vitro: Efficacy (1) Qualitative Information 1 of 1
Assay Description
expression of α1 subunit protein of GABAA receptor primary cerebellar granule cells from Sprague-Dawley rats Western blotting; optical density readings, ECL (enhanced chemiluminescence) used for detection of GABAA receptor subunits proteins
Results
decrease in the expression of the GABAA receptor α1 subunit protein, not significantly different from the effect of flunitrazepam alone
Citation
Brown, Maria J.; Bristow, David R.
British Journal of Pharmacology, 1996 , vol. 118, # 5 p. 1103 - 1110 Title/Abstract Full Text View citing articles Show Details
Bioactivity
Show Targets
1