Page last updated: 2024-12-05

nordazepam

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2997
CHEMBL ID523
CHEBI ID111762
SCHEMBL ID78453
MeSH IDM0005804

Synonyms (116)

Synonym
7-chloro-5-phenyl-1,3-dihydro-[1,4]benzodiazepin-2-one
nsc631619
nsc-631619
7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one
nordiazepam
ro 5-2180
n-deoxydemoxepam
ro 52180
a 101
ndz ,
wln: t67 gmv jn ihj cg kr
n-demethyldiazepam
nsc-46078
2h-1, 7-chloro-1,3-dihydro-5-phenyl-
n-desmethyldiazepam
2h-1, 1,3-dihydro-7-chloro-5-phenyl-
demethyldiazepam
n1-desmethyldiazepam
A101 ,
nsc46078
7-chloro-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one
7-chloro-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one
DIVK1C_000979
KBIO1_000979
7-chlor-2,3-dihydro-5-phenyl-1h-1,4-benzodiazepin-2-on
ccris 9181
1-demethyldiazepam
einecs 214-123-4
nsc 46078
dmdz
n-descyclopropylmethylprazepam
2h-1,4-benzodiazepin-2-one, 7-chloro-1,3-dihydro-5-phenyl-
demadar
sopax
7-chloro-1,3-dihydro-5-phenyl-2h-1,4-benzodiazepin-2-one
nordazepamum [inn-latin]
n-deoxydemoxapam
2h-1,4-benzodiazepin-2-one, 1,3-dihydro-7-chloro-5-phenyl-
dea no. 2838
lomax
brn 0751823
calmday
madar
stilny
vegesan
norprazepam
nordazepam [inn]
IDI1_000979
ndd ,
CHEMDIV1_028362
nordazepam
C07486
1088-11-5
7-chloro-1,3-dihydro-5-phenyl-(2h)-1,4-benzodiazepin-2-one
desmethyldiazepam
5-phenyl-7-chloro-1,4-benzodiazepin-2-one
OPREA1_578139
MIXCOM6_000554
NINDS_000979
NCGC00168263-01
MLS001173623
smr000238153
nordazepamum
CHEBI:111762 ,
CHEMBL523 ,
praxadium
desoxydemoxepam
nordazepam civ
nordazepam (inn)
D08283
calmday (tn)
HMS503C19
HMS667J04
AKOS000636746
7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one( am)
7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one(desmethyldiazepam)
bdbm50027835
7-chloro-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one(nordiazepam)
7-chloro-5-phenyl-1h-benzo[e][1,4]diazepin-2(3h)-one
A801929
AKOS005486646
nordaz
67220mcm01 ,
5-24-04-00291 (beilstein handbook reference)
unii-67220mcm01
tox21_113493
cas-1088-11-5
dtxcid3028926
dtxsid2049000 ,
STK560158
7-chloro-5-phenyl-3h-1,4-benzodiazepin-2-ol
7-chloro-5-phenyl-3h-1,4-benzodiazepin-2-one
HMS2272B05
dipotassium clorazepate impurity b [ep impurity]
nordazepam [who-dd]
diazepam impurity a [ep impurity]
nordazepam [mart.]
nordazepam [mi]
nordazepam civ [usp-rs]
SCHEMBL78453
7-chloro-5-phenyl-2-oxo-2,3-dihydro-1h-benzo[f]-1,4-diazepine
7-chloro-1,3 -dihydro-5-phenyl-2h-1,4-benzodiazepine-2-one
7-chloro-2,3-dihydro-5-phenyl-1h-1,4-benzodiazepin-2-one
7-chloro-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one #
desmethyldiazepam, analytical standard
diazepam-m n-desmethyl
nordazepam (nordiazepam) 1.0 mg/ml in methanol
nordazepam (nordiazepam) 0.1 mg/ml in methanol
7-chloro-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one (nordazepam)
Q3180288
DB14028
diazepam ep impurity a
nordazepam; desmethyl amino diazepam; 7-chloro-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one
(z)-7-chloro-5-phenyl-1h-benzo[e][1,4]diazepin-2(3h)-one
desmethyldiazepam (nordazepam)
desmethyldiazepam (nordazepam), 1mg/ml in methanol

Research Excerpts

Actions

ExcerptReferenceRelevance
"Nordazepam with a lower solubility in milk fat showed M/P ratios which could be best explained by considering protein and fat concentrations together."( Studies on the excretion of diazepam and nordazepam into milk for the prediction of milk-to-plasma drug concentration ratios.
Guentert, TW; Stebler, T, 1992
)
1.27

Pharmacokinetics

ExcerptReferenceRelevance
" The method is applicable to pharmacokinetic studies of clorazepate, a benzodiazepine derivative transformed to desmethyldiazepam prior to absorption."( Determination of desmethyldiazepam in plasma by electron-capture GLC: application to pharmacokinetic studies of clorazepate.
Greenblatt, DJ, 1978
)
0.26
" While the normal half-life (T1/2(beta)) varies between 1 and 2 days, it can be increased to up to 80--100 h in subjects over 60 years of age."( [Clinical pharmacokinetics of diazepam and its biologically active metabolites (author's transl)].
Klotz, U, 1978
)
0.26
"35 ml/min/kg in man, whereas T1/2(alpha), the half-life of distribution, varied only approximately 3-fold (0."( Pharmacokinetics and plasma binding of diazepam in man, dog, rabbit, guinea pig and rat.
Antonin, KH; Bieck, PR; Klotz, U, 1976
)
0.26
" 4 Compared with diazepam the tested drug has a longer plasma apparent half-life and a lower relative clearance."( Pharmacokinetics of N-demethyldiazepam in patients suffering from insomnia and treated with nortriptyline.
Alberti, GG; De Maio, D; Franciosi, P; Gomeni, R; Scieghi, G; Tognoni, G, 1975
)
0.25
" The plasma half-life of diazepam in the poor metabolizers was longer than that in the extensive metabolizers (mean +/- SEM, 91."( Incidence of S-mephenytoin hydroxylation deficiency in a Korean population and the interphenotypic differences in diazepam pharmacokinetics.
Chiba, K; Ishizaki, T; Jang, IJ; Kusaka, M; Shin, JG; Shin, SG; Sohn, DR, 1992
)
0.28
" Diazepam plasma concentrations and pharmacokinetic parameters were not affected by the concomitant medication with felodipine."( The effects of felodipine on the pharmacokinetics of diazepam.
de la Rey, N; Hundt, HK; Luus, HG; Meyer, BH; Müller, FO; Röthig, HJ, 1992
)
0.28
" These results, when compared with human pharmacokinetic studies, allow a means of extrapolating effective monkey anticonvulsant doses to humans on a pharmacokinetic basis."( Pharmacokinetics of diazepam intramuscularly administered to rhesus monkeys.
Corcoran, KD; Lukey, BJ; Solana, RP, 1991
)
0.28
" On this day, subjects began taking diazepam (10 mg) orally for one week, with pharmacokinetic studies performed at day 8, when steady state levels of diazepam were reached."( Effect of orally administered misoprostol and cimetidine on the steady state pharmacokinetics of diazepam and nordiazepam in human volunteers.
Andrade, GN; Lima, DR; Santos, RM; Werneck, E,
)
0.13
" Pharmacokinetic analysis were carried out by two ways; according to compartmental pharmacokinetic models and by statistic moments."( Pharmacokinetic profiles of prazepam and 14C-prazepam in rat.
Dios-Vieitez, MC; Fos, D; Renedo, MJ, 1991
)
0.28
" Suitability of the method was assessed in a preliminary pharmacokinetic study in which three subjects were given a single 20-mg oral dose of halazepam following an overnight fast."( Liquid chromatographic assay and pharmacokinetics of halazepam and its metabolite in humans.
Ellinwood, EH; Gupta, SK, 1990
)
0.28
" The mean elimination half-life of diazepam fell within the range observed in healthy persons after the ingestion of therapeutic doses (5), or it was only moderately prolonged (t1/2 49."( Diazepam loading in alcohol withdrawal: clinical pharmacokinetics.
Heikkinen, H; Heinälä, P; Piepponen, T, 1990
)
0.28
" However, the distributions of elimination half-life (44."( A large-sample study of diazepam pharmacokinetics.
Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Shader, RI, 1989
)
0.28
" DZ and synthesized NDDZ had the same pharmacodynamic characteristics, but the main metabolic product of DZ (metabolite NDDZ) showed a different pharmacokinetic profile."( Determination of pharmacodynamics of diazepam by quantitative pharmaco-EEG.
Iwaya, N; Miyoshi, K; Morita, Y, 1989
)
0.28
"The pharmacokinetic profiles of oral and sublingual administrations of prazepam 20 mg to 5 normal volunteers were compared in order to explain the clinical observation that sublingual prazepam appears to exhibit sedative properties when compared to the same dose of oral prazepam."( Comparison of sublingual and oral prazepam in normal subjects. II. Pharmacokinetic and pharmacodynamic data.
Ansseau, M; Jacqmin, P, 1988
)
0.27
" Mean kinetic variables were volume of distribution (Vd), 90 liters; elimination half-life (t1/2), 93 hours; and clearance, 12."( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam.
Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988
)
0.27
" It is concluded that acute tolerance to diazepam in mice may not be attributed to changes in pharmacokinetic factors."( Acute tolerance to diazepam in mice: pharmacokinetic considerations.
Gwee, MC; Lee, HS; Wong, PT; Yoong, YL, 1986
)
0.27
" Plasma levels declined with a biphasic pattern, and the elimination phase had a half-life of 82."( Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans.
Bareggi, SR; Leva, S; Pirola, R; Zecca, L,
)
0.13
" Pharmacokinetic parameters were derived assuming a two compartment model, distribution phase less than 6 h, and 100% oral systemic availability."( Differences in diazepam pharmacokinetics in Chinese and white Caucasians--relation to body lipid stores.
Chan, M; Ko, W; Kumana, CR; Lauder, IJ; Lin, HJ, 1987
)
0.27
"To determine the effect of fluoxetine on diazepam's pharmacokinetic and psychomotor responses, single oral doses of 10 mg diazepam were administered to six normal subjects on three occasions, either alone or in combination with 60 mg fluoxetine."( The effect of fluoxetine on the pharmacokinetics and psychomotor responses of diazepam.
Bergstrom, RF; Bosomworth, JC; Lemberger, L; Rowe, H; Tenbarge, JB, 1988
)
0.27
" We also report results on using this assay in a pharmacokinetic study of high doses of diazepam used to treat chronic schizophrenic patients."( Liquid-chromatographic assay of diazepam and its major metabolites in serum, and application to pharmacokinetic study of high doses of diazepam in schizophrenics.
Moroji, T; Motomura, H; Noguchi, T; Sekiguchi, R; Tada, K, 1985
)
0.27
"The elimination half-life of chlordiazepoxide and diazepam increases with age, and this may cause prolongation of action after a single dose and delayed accumulation on multiple dosing in elderly patients."( [Pharmacokinetic of benzodiazepines in old age].
Vozeh, S, 1981
)
0.26
" Newborns and premature infants can metabolize and eliminate diazepam, although the parent drug has a longer half-life and decreased rate of biotransformation to its primary metabolites than in older children and adults."( Pharmacokinetics of benzodiazepines and psychostimulants in children.
Coffey, B; Greenblatt, DJ; Shader, RI, 1983
)
0.27
"Large differences exist among the various benzodiazepines with regard to their pharmacokinetic properties and metabolism in man."( Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles.
Breimer, DD; Jochemsen, R, 1984
)
0.27
"03) the elimination of desmethyldiazepam, as shown prolongation of its elimination half-life from 51."( Influence of cimetidine on the pharmacokinetics of desmethyldiazepam and oxazepam.
Klotz, U; Reimann, I, 1980
)
0.26
" The elimination half-life was significantly shorter and the plasma clearance significantly higher in the patients than in the normal volunteers."( Pharmacokinetics of diazepam in epileptic patients and normal volunteers following intravenous administration.
Dhillon, S; Richens, A, 1981
)
0.26
"015) and elimination half-life tended to be prolonged (38."( Clearance of diazepam can be impaired by its major metabolite desmethyldiazepam.
Klotz, U; Reimann, I, 1981
)
0.26
" In the control state, antipyrine half-life was longer in elderly than in young subjects (16."( Cimetidine impairs clearance of antipyrine and desmethyldiazepam in the elderly.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI, 1982
)
0.26
" administration the kinetics of total chlordesmethyldiazepam in patients with liver disease differed from those in controls: elimination half-life was almost twice that in controls (395 and 204 h), as a consequence of a marked reduction in total clearance (0."( Effects of liver disease on the pharmacokinetics of intravenous and oral chlordesmethyldiazepam.
Bareggi, SR; Devis, G; Pirola, R; Potvin, P, 1995
)
0.29
" The elimination half-life of desmethyldiazepam was longer in the Riv:TOX(M) (from the National Institute of Public Health and Environmental Protection) and in the Cpb:WU strain than in the Crl:(WI)BR strain."( Pharmacokinetic differences of desmethyldiazepam in three outbred Wistar strains related to differences in liver enzyme activities.
de Groot, G; Noordhoek, J; van der Laan, JW; Wortelboer, H, 1993
)
0.29
" ND and parent OX have similar pharmacokinetic profiles."( Pharmacokinetics of nordiazepam in physical dependence and precipitated abstinence in dogs.
Martin, WR; Sloan, JW; Wala, EP, 1993
)
0.29
" There was evidence for pharmacokinetic changes when probe doses of diazepam were given after 7, 14 or 21 recovery days."( Evidence against oppositional and pharmacokinetic mechanisms of tolerance to diazepam's sedative effects.
Berry, D; Fernandes, C; File, SE, 1996
)
0.29
" The pharmacokinetic analyses were based on data from 20 individuals."( Effect of sertraline on the pharmacokinetics and protein binding of diazepam in healthy volunteers.
Baris, BA; Gardner, MJ; Preskorn, SH; Wilner, KD, 1997
)
0.3
"To evaluate changes in the pharmacokinetic disposition of diazepam in foals from 4 to 84 days of age."( Age-related changes in the pharmacokinetic disposition of diazepam in foals.
Court, MH; Greenblatt, DJ; Norman, WM, 1997
)
0.3
"Factors likely to affect the pharmacokinetic disposition of diazepam in foals, such as body composition and hepatic enzyme activity, are in transition during the first 21 days of life."( Age-related changes in the pharmacokinetic disposition of diazepam in foals.
Court, MH; Greenblatt, DJ; Norman, WM, 1997
)
0.3
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"This was a phase I, randomized, open-label, two-part, single-dose, crossover, single-centre pharmacokinetic study in 48 healthy young adult (aged 18-40 years) male and female subjects."( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study.
Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011
)
0.37
" The brain concentration-time profiles of diazepam that correspond to these effects are unknown, but can be estimated with physiologically based pharmacokinetic (PBPK) modeling."( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points.
Burkat, PM, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" Also alcohol alone, and all the drugs in combination with alcohol retarded learning acquisition."( Effects on learning and memory of 2-week treatments with chlordiazepoxide lactam, N-desmethyldiazepam, oxazepam and methyloxazepam, alone or in combination with alcohol.
Liljequist, R; Linnoila, M; Palva, E, 1979
)
0.26
"Effects of alprazolam, alone and in combination with ethanol, on psychomotor and cognitive performance were studied in healthy male volunteers and compared to effects of diazepam."( Effects of single doses of alprazolam and diazepam, alone and in combination with ethanol, on psychomotor and cognitive performance and on autonomic nervous system reactivity in healthy volunteers.
Eckardt, MJ; Granger, A; Lane, E; Linnoila, M; Lister, R; Moss, H; Stapleton, JM, 1990
)
0.28
" The plasma pharmacokinetics of melagatran, diclofenac, diazepam, N-desmethyl-diazepam and nifedipine were determined when administered alone and in combination with ximelagatran."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.32
"No inhibition, or only minor inhibition, of CYP enzymes by ximelagatran, the intermediates or melagatran was shown in the in vitro studies, suggesting that ximelagatran would not cause CYP-mediated drug-drug interactions in vivo."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.32
" Together, the in vitro and in vivo studies indicate that metabolic drug-drug interactions involving the major human CYP enzymes should not be expected with ximelagatran."( Ximelagatran, an oral direct thrombin inhibitor, has a low potential for cytochrome P450-mediated drug-drug interactions.
Andersson, TB; Bredberg, E; Eriksson, UG; Eriksson-Lepkowska, M; Frison, L; Johansson, S; Larsson, M; Thuresson, A, 2003
)
0.32

Bioavailability

ExcerptReferenceRelevance
" Bioavailability was 77% for tablets and 79% for drops."( Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans.
Bareggi, SR; Leva, S; Pirola, R; Smirne, S; Truci, G; Zecca, L, 1988
)
0.27
" The bioavailability of desmethyldiazepam from tablets and from drops was practically the same."( Preliminary study of the pharmacokinetics of desmethyldiazepam administered as drops or tablets.
Laufen, H; Leitold, M; Räder, K; Yeates, RA, 1986
)
0.27
"The pharmacokinetics and bioavailability of desmethyldiazepam (DMDZ), formed from its precursor clorazepate (CZP) dipotassium, were assessed in a series of 17 healthy volunteers aged 21--66 years."( Desmethyldiazepam kinetics after intravenous, intramuscular, and oral administration of clorazepate dipotassium.
Greenblatt, DJ; Knüchel, M; Locniskar, A; Ochs, HR; Steinhaus, E, 1982
)
0.26
" The bioavailability was almost 100% after IM administration."( Pharmacokinetics of chlorazepate after intravenous and intramuscular administration.
Bertler, A; Lindgren, S; Magnusson, JO; Malmgren, H, 1983
)
0.27
" Thus, differences in absorption rate of orally administered benzodiazepines can lead to differences in the intensity of single-dose effects, despite administration of doses that are equivalent in terms of long-term anxiolytic efficacy."( Plasma concentrations and clinical effects after single oral doses of prazepam, clorazepate, and diazepam.
Allison, S; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Pary, RJ; Shader, RI, 1984
)
0.27
"The onset and duration of action of benzodiazepines after single oral doses depend largely on absorption rate and the rate and extent of distribution."( [Benzodiazepines: significance of kinetics for therapy].
Ochs, HR, 1983
)
0.27
"The bioavailability of diazepam (I) in uncoated tablets in beagles was tested using tablets tested previously in humans."( Correlation of the bioavailability of diazepam from uncoated tablets in beagle dogs with its dissolution rate and bioavailability in humans.
Aoyagi, N; Ejima, A; Kaniwa, N; Koibuchi, M; Nishida, Y; Ogata, H; Ogawa, Y; Shibazaki, T; Shimamoto, T; Uda, Y; Yashiki, T, 1982
)
0.26
"The lymphatic bioavailability (FL) of diazepam (DZ) and its major metabolite desmethyldiazepam (DDZ) was studied."( Lymphatic bioavailability of diazepam and desmethyldiazepam in the rat.
Jindrová, O; Lamka, J, 1996
)
0.29
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The new methodology may, therefore, be used for fast bioavailability screening of virtual libraries having millions of molecules."( Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
Ertl, P; Rohde, B; Selzer, P, 2000
)
0.31
" The relative bioavailability between both formulations was assessed by calculating individual test/reference ratios for Cmax, AUClast and AUC0-inf."( Quantification of chlordesmethyldiazepam by liquid chromatography-tandem mass spectrometry: application to a cloxazolam bioequivalence study.
Barrientos-Astigarraga, RE; De Nucci, G; Galvinas, PA; Mendes, GD; Oliveira, CH; Oliveira-Silva, D, 2009
)
0.35
" This study evaluated the dose proportionality of the diazepam autoinjector and the consequent diazepam bioavailability relative to an equivalent dose of diazepam administered rectally as a commercial gel."( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study.
Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011
)
0.37
" Part II (n = 24) assessed the relative bioavailability of the diazepam 10 mg autoinjector versus the diazepam 10 mg rectal gel."( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study.
Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011
)
0.37
"21), respectively, indicating that the overall bioavailability of the diazepam autoinjector was approximately 14% higher than that of diazepam rectal gel."( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study.
Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"A specially designed tablet dosage form of the benzodiazepine clorazepate dipotassium (Tranxene) was developed for once-a-day administration."( Steady-state bioavailability of two clorazepate dipotassium dosage forms.
Barker, WM; Carrigan, PJ; Chao, GC; Chun, AH; Hoffman, DJ, 1977
)
0.26
"The effects on active social interaction of acute and chronic dosage with diazepam (1 mg/kg), desmethyldiazepam (2 mg/kg), and chlor-desmethyl-diazepam (0."( Acute and chronic effects of three benzodiazepines in the social interaction anxiety test in mice.
de Angelis, L; File, SE, 1979
)
0.26
" The accumulation of DD after multiple dosage could be explained by the fact that it is formed faster from D than it is eliminated."( Disposition of diazepam and its major metabolite desmethyldiazepam in patients with liver disease.
Antonin, KH; Bieck, PR; Brügel, H; Klotz, U, 1977
)
0.26
" After multiple dosing with diazepam its T1/2(beta) is prolonged, which is caused by a lowered clearance."( [Important factors determining human distribution and elimination of diazepam].
Klotz, U, 1977
)
0.26
" A second peak in plasma diazepam concentration 6--12 h after dosing was observed in 6 children, which may have been due to mobilization of diazepam from the gastrointestinal mucosa produced by feeding 4 h after administration of the drug."( Plasma concentration of diazepam and N-desmethyldiazepam in children after a single rectal or intramuscular dose of diazepam.
Bredesen, JE; Langslet, A; Lunde, PK; Meberg, A, 1978
)
0.26
"Clorazepate dipotassium was administered orally to 8 healthy dogs at a dosage of 2 mg/kg of body weight, q 12 h, for 21 days."( Disposition of clorazepate in dogs after single- and multiple-dose oral administration.
Brown, SA; Forrester, SD; Hartsfield, SM; Lees, GE, 1990
)
0.28
" Blood was collected up to 120 hours after diazepam dosing (still during one-daily omeprazole and placebo administration) for measurement of diazepam and its major metabolite desmethyldiazepam."( Effect of omeprazole treatment on diazepam plasma levels in slow versus normal rapid metabolizers of omeprazole.
Andersson, T; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990
)
0.28
"The effects of steady state dosing with omeprazole and cimetidine on plasma diazepam levels have been studied in 12 healthy males."( Effect of omeprazole and cimetidine on plasma diazepam levels.
Andersson, T; Andrén, K; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990
)
0.28
" The dosage remained the same for all patients during the 28 days of the experiment."( [Efficacy and kinetics of chlorazepate administered to anxious patients in a single daily dose].
Adamkiewicz, L; Duguay, R; Le Lorier, J; Messier, R; Rochefort, JG; Viguié, F, 1985
)
0.27
"The disposition of diazepam (D) after a single oral dose of 10 mg was evaluated in nine healthy male volunteers under the following conditions (randomized, double-blind, crossover design): D + comedication of placebo and D + nocturnal dosing with 300 mg ranitidine or 300 mg nizatidine."( Nocturnal doses of ranitidine and nizatidine do not affect the disposition of diazepam.
Dammann, HG; Gottlieb, W; Keohane, PP; Klotz, U, 1987
)
0.27
" After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100%."( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam.
Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988
)
0.27
"The dose-response relationships of diazepam and several of its metabolites were determined in rats trained to discriminate diazepam (3 mg/kg) from saline in a two-lever operant choice task."( Potencies of diazepam metabolites in rats trained to discriminate diazepam.
Brase, DA; Dewey, WL; Glennon, RA; Young, R, 1986
)
0.27
" Dosage modification of either fluoxetine or diazepam is unlikely to be necessary."( The effect of fluoxetine on the pharmacokinetics and psychomotor responses of diazepam.
Bergstrom, RF; Bosomworth, JC; Lemberger, L; Rowe, H; Tenbarge, JB, 1988
)
0.27
" Flumazenil caused dose-related increases in the NPAS scores of both diazepam- and nordiazepam-dependent dogs; the slopes of the two dose-response lines were not different."( Precipitation of abstinence in nordiazepam- and diazepam-dependent dogs.
Martin, WR; McNicholas, LF; Sloan, JW; Wala, E, 1988
)
0.27
"Dogs, surgically implanted with a chronic gastric fistula, were chronically dosed with N-desmethyldiazepam (32 mg/kg/day) in four divided doses to attain N-desmethyldiazepam plasma levels comparable to those observed in dogs dependent on diazepam (60 mg/kg/day)."( N-desmethyldiazepam physical dependence in dogs.
Martin, WR; McNicholas, LF; Pruitt, TA, 1985
)
0.27
"The elimination half-life of chlordiazepoxide and diazepam increases with age, and this may cause prolongation of action after a single dose and delayed accumulation on multiple dosing in elderly patients."( [Pharmacokinetic of benzodiazepines in old age].
Vozeh, S, 1981
)
0.26
" Such differences may be very important clinically because pharmacokinetic data will help to optimize drug therapy with respect to the choice of the proper drug and drug preparation, as well as with the choice of a proper dose and dosage regimen."( Pharmacokinetics of benzodiazepines: metabolic pathways and plasma level profiles.
Breimer, DD; Jochemsen, R, 1984
)
0.27
" administration of pure ND in two dogs, has shown that ND declines biexponentially with a t1/2 beta similar to the one estimated after CZP dosing in control animals."( Cimetidine interaction with dipotassium clorazepate disposition in the anesthetized dog.
Colin, P; Lelorier, J; Sirois, G, 1984
)
0.27
" Serum nordiazepam is a more consistent index of dosage after chronic therapy than serum diazepam because it has a longer elimination half-time."( Value of serum diazepam and nordiazepam measurements in anxious patients.
Dawling, S; Flanagan, RJ; Moreton, K; Riley, P; Treasaden, I; Tyrer, P, 1984
)
0.27
" Plasma concentrations of DZ and its major metabolite desmethyldiazepam (DMDZ) were measured daily during the period of dosing and in the 7-day washout period that followed."( Repeated diazepam dosing in cirrhotic patients: cumulation and sedation.
Eckardt, B; Greenblatt, DJ; Harmatz, JS; Ochs, HR; Shader, RI, 1983
)
0.27
" The rate and extent of accumulation during multiple dosage depend on elimination half-life and clearance."( [Benzodiazepines: significance of kinetics for therapy].
Ochs, HR, 1983
)
0.27
" Determination of diazepam and desmethyldiazepam plasma concentrations during the dosing period and for a withdrawal period indicated that accumulation half-life for both diazepam (7."( Prolonged accumulation of diazepam in obesity.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI,
)
0.13
" We studied the clinical importance of this effect in 10 patients, who were receiving long-term treatment with diazepam for anxiety, tension, or difficulty in sleeping, in an eight-week double-blind controlled study during which the diazepam dosage remained constant."( Clinical importance of the interaction of diazepam and cimetidine.
Abernethy, DR; Greenblatt, DJ; Harmatz, JS; Morse, DS; Shader, RI, 1984
)
0.27
" Significant relationships were found between the clinical effect and the plasma concentrations of D and DD, respectively; a curvilinear relationship resulted if the dosage was disregarded, but within the individual dosage groups the relationship was found to be linear."( Diazepam and desmethyldiazepam plasma concentrations in chronic anxious outpatients.
Case, WG; Dixon, R; Downing, RW; Fridman, R; Rickels, K, 1984
)
0.27
" Psychomotor and cognitive functions showed consistent dose-response effects, while for subjective evaluations, the only effect of dose level was in the duration of sedation."( Dose-response analysis of the behavioral effects of diazepam: II. Psychomotor performance, cognition and mood.
Ghoneim, MM; Hinrichs, JV; Mewaldt, SP, 1984
)
0.27
"It is important to understand both the kinetic and the dynamic implications of dosing TCAs and BZs in the elderly, for whom these drugs are frequently prescribed."( Implications of dosing tricyclic antidepressants and benzodiazepines in geriatrics.
Cutler, NR; Narang, PK, 1984
)
0.27
" It was found to vary markedly in an acute dosage study."( Diazepam and N-desmethyldiazepam concentrations in saliva, plasma and CSF.
Hallstrom, C; Lader, MH, 1980
)
0.26
" However, concurrent ingestion of diazepam together with other central depressant drugs (such as ethanol, barbiturates, analgesics, or tricyclic antidepressants) produced serious intoxication in 5 of the remaining 14 patients, regardless of the diazepam dosage or plasma concentration."( Benzodiazepine overdosage: plasma concentrations and clinical outcome.
Divoll, M; Greenblatt, DJ; Lacasse, Y; Shader, RI, 1981
)
0.26
" The findings of modest diazepam dose and plasma concentration (mean=324 ng/ml) and of a trend toward a positive correlation between anxiety level and both dose and plasma level suggest inadequate dosage as a more likely explanation for the subjects' continued anxiety."( Chronic diazepam treatment in psychiatric outpatients.
Battey, YW; Greenblatt, DJ; Laughren, TP, 1982
)
0.26
" These results suggest that sertraline at the maximum recommended dosage under steady-state conditions, and demethylsertraline, the principal metabolite of sertraline, are unlikely to exert significant inhibitory effects on the CYP2C19 and CYP3A3/4 hepatic isoenzymes responsible for the metabolism of diazepam."( Effect of sertraline on the pharmacokinetics and protein binding of diazepam in healthy volunteers.
Baris, BA; Gardner, MJ; Preskorn, SH; Wilner, KD, 1997
)
0.3
"Repeat dosing of DZP leads to substantial accumulation, and high, persistent serum and CSF concentrations, which may explain the toxic effects of repeat DZP dosing."( Comparison of single- and repeated-dose pharmacokinetics of diazepam.
Brown, S; Patsalos, PN; Shorvon, SD; Tong, X; Walker, MC, 1998
)
0.3
"To determine whether the gene dosage of CYP2C19 affects the metabolism of diazepam and desmethyldiazepam in healthy Chinese subjects."( Effect of the gene dosage of CgammaP2C19 on diazepam metabolism in Chinese subjects.
He, N; Huang, SL; Ou-Yang, DS; Qin, XP; Wang, W; Wang, YJ; Xie, HG; Xu, ZH; Zhou, HH, 1999
)
0.3
" Each subject completed screening up to 30 days prior to three (Part I) or two (Part II) dosing periods."( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study.
Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011
)
0.37
" Causing concern for safety is the lack of dosage information resulting in users self-medicating, often leading to unintended overdoses, coma or death at higher doses."( Validation of an LC-MS/MS Method for the Quantification of 13 Designer Benzodiazepines in Blood.
Concheiro, M; Cooper, G; Mei, V; Pardi, J, 2019
)
0.51
"1 nM at equilibrium with this diazepam dosing schedule."( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points.
Burkat, PM, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
GABA modulatorA substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor-ionophore complex. GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of gamma-aminobutyric acid-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act.
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
anticonvulsantA drug used to prevent seizures or reduce their severity.
sedativeA central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
1,4-benzodiazepinone
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency19.55870.000221.22318,912.5098AID743035; AID743063
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency23.91450.000214.376460.0339AID720692
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency21.75780.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency0.20600.004611.374133.4983AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)106,414.00000.00011.14948.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-6Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC50 (µMol)106,414.00000.00011.03936.0000AID40995
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)106,414.00000.00011.29158.0000AID40995
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki73.00000.00010.739610.0000AID42169
Gamma-aminobutyric acid receptor subunit gamma-2Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit deltaMus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit alpha-2Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit alpha-3Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit gamma-3Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC50 (µMol)106,414.00000.00011.30188.0000AID40995
Translocator proteinHomo sapiens (human)IC50 (µMol)106,414.00000.00030.13020.4900AID40987
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC50 (µMol)106,414.00000.00010.98006.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)106,414.00000.00011.19936.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)106,414.00000.00010.93746.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)106,414.00000.00011.01936.0000AID40995
Gamma-aminobutyric acid receptor subunit beta-1Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit alpha-1Mus musculus (house mouse)IC50 (µMol)0.00000.00000.03690.0740AID42161
Gamma-aminobutyric acid receptor subunit beta-3Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-5Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit piMus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
Gamma-aminobutyric acid receptor subunit alpha-4Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit thetaMus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit gamma-1Mus musculus (house mouse)IC50 (µMol)0.00000.00000.00030.0005AID42161
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC50 (µMol)106,414.00000.00011.02016.0000AID40995
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1-acid glycoprotein 1Homo sapiens (human)Activity9.00009.00009.500010.0000AID288810
AlbuminHomo sapiens (human)Activity17.00001.30004.65008.0000AID288811
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
chloride transmembrane transportGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
regulation of immune system processAlpha-1-acid glycoprotein 1Homo sapiens (human)
acute-phase responseAlpha-1-acid glycoprotein 1Homo sapiens (human)
inflammatory responseAlpha-1-acid glycoprotein 1Homo sapiens (human)
negative regulation of interleukin-6 productionAlpha-1-acid glycoprotein 1Homo sapiens (human)
negative regulation of tumor necrosis factor productionAlpha-1-acid glycoprotein 1Homo sapiens (human)
positive regulation of interleukin-1 beta productionAlpha-1-acid glycoprotein 1Homo sapiens (human)
positive regulation of interleukin-1 productionAlpha-1-acid glycoprotein 1Homo sapiens (human)
positive regulation of tumor necrosis factor productionAlpha-1-acid glycoprotein 1Homo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
monoatomic ion transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to toxic substanceGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
central nervous system neuron developmentGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
response to progesteroneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ovulation cycleGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
roof of mouth developmentGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
protein targeting to mitochondrionTranslocator proteinHomo sapiens (human)
C21-steroid hormone biosynthetic processTranslocator proteinHomo sapiens (human)
heme biosynthetic processTranslocator proteinHomo sapiens (human)
monoatomic anion transportTranslocator proteinHomo sapiens (human)
chloride transportTranslocator proteinHomo sapiens (human)
steroid metabolic processTranslocator proteinHomo sapiens (human)
glial cell migrationTranslocator proteinHomo sapiens (human)
response to xenobiotic stimulusTranslocator proteinHomo sapiens (human)
response to manganese ionTranslocator proteinHomo sapiens (human)
response to vitamin B1Translocator proteinHomo sapiens (human)
peripheral nervous system axon regenerationTranslocator proteinHomo sapiens (human)
sterol transportTranslocator proteinHomo sapiens (human)
adrenal gland developmentTranslocator proteinHomo sapiens (human)
negative regulation of protein ubiquitinationTranslocator proteinHomo sapiens (human)
regulation of cholesterol transportTranslocator proteinHomo sapiens (human)
response to progesteroneTranslocator proteinHomo sapiens (human)
negative regulation of tumor necrosis factor productionTranslocator proteinHomo sapiens (human)
response to testosteroneTranslocator proteinHomo sapiens (human)
regulation of cell population proliferationTranslocator proteinHomo sapiens (human)
cholesterol homeostasisTranslocator proteinHomo sapiens (human)
positive regulation of apoptotic processTranslocator proteinHomo sapiens (human)
negative regulation of nitric oxide biosynthetic processTranslocator proteinHomo sapiens (human)
behavioral response to painTranslocator proteinHomo sapiens (human)
regulation of steroid biosynthetic processTranslocator proteinHomo sapiens (human)
positive regulation of mitochondrial depolarizationTranslocator proteinHomo sapiens (human)
positive regulation of calcium ion transportTranslocator proteinHomo sapiens (human)
contact inhibitionTranslocator proteinHomo sapiens (human)
positive regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
negative regulation of glial cell proliferationTranslocator proteinHomo sapiens (human)
positive regulation of programmed necrotic cell deathTranslocator proteinHomo sapiens (human)
cellular response to lipopolysaccharideTranslocator proteinHomo sapiens (human)
cellular response to zinc ionTranslocator proteinHomo sapiens (human)
cellular hypotonic responseTranslocator proteinHomo sapiens (human)
maintenance of protein location in mitochondrionTranslocator proteinHomo sapiens (human)
negative regulation of mitophagyTranslocator proteinHomo sapiens (human)
negative regulation of ATP metabolic processTranslocator proteinHomo sapiens (human)
response to acetylcholineTranslocator proteinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processTranslocator proteinHomo sapiens (human)
negative regulation of corticosterone secretionTranslocator proteinHomo sapiens (human)
behavioral fear responseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
associative learningGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
negative regulation of chloride transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
response to xenobiotic stimulusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neurotransmitter transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
GABA-A receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
protein bindingAlpha-1-acid glycoprotein 1Homo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
androgen bindingTranslocator proteinHomo sapiens (human)
protein bindingTranslocator proteinHomo sapiens (human)
benzodiazepine receptor activityTranslocator proteinHomo sapiens (human)
cholesterol bindingTranslocator proteinHomo sapiens (human)
transmembrane transporter bindingTranslocator proteinHomo sapiens (human)
cholesterol transfer activityTranslocator proteinHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
signaling receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA receptor bindingGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane signaling receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter transmembrane transporter activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (48)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
apical plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit piHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
axonGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)
extracellular regionAlpha-1-acid glycoprotein 1Homo sapiens (human)
extracellular spaceAlpha-1-acid glycoprotein 1Homo sapiens (human)
platelet alpha granule lumenAlpha-1-acid glycoprotein 1Homo sapiens (human)
specific granule lumenAlpha-1-acid glycoprotein 1Homo sapiens (human)
collagen-containing extracellular matrixAlpha-1-acid glycoprotein 1Homo sapiens (human)
extracellular exosomeAlpha-1-acid glycoprotein 1Homo sapiens (human)
blood microparticleAlpha-1-acid glycoprotein 1Homo sapiens (human)
tertiary granule lumenAlpha-1-acid glycoprotein 1Homo sapiens (human)
extracellular spaceAlpha-1-acid glycoprotein 1Homo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
nuclear envelopeGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
dendriteGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
presynaptic active zone membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)
mitochondrionTranslocator proteinHomo sapiens (human)
mitochondrial outer membraneTranslocator proteinHomo sapiens (human)
cytosolTranslocator proteinHomo sapiens (human)
intracellular membrane-bounded organelleTranslocator proteinHomo sapiens (human)
extracellular exosomeTranslocator proteinHomo sapiens (human)
endoplasmic reticulumTranslocator proteinHomo sapiens (human)
membraneTranslocator proteinHomo sapiens (human)
nucleoplasmGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
cytosolGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuronal cell body membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synaptic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuronal cell bodyGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
inhibitory synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
cerebellar Golgi cell to granule cell synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)
nucleolusGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
microtubule cytoskeletonGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (100)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID42161Inhibition of binding to GABA-A central benzodiazepine receptor at 0.2 mg/kg1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID13305-Log C was determined by performing the foot shock test1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Decomposition of pharmacological activity indices into mutually independent components using principal component analysis.
AID228469Evaluation of inclined screen test.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID39914The compound was tested for binding affinity against PBR(peripheral benzodiazepine receptor) in normal rat brain homogenate1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID55575The compound was tested for cytotoxicity against D341 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID135326BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID200785The compound was tested for cytotoxicity against SF-188 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID237585Tested for fraction of oral dose absorbed orally in humans2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1136394Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of strychnine-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID29844Fraction absorbed after oral administration in humans2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID407142Selectivity index, ratio of CC50 for human Hep G2.2.15 cells to IC50 for HBV e antigen secretion2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
AID15120Percent of the drug absorbed after administration to humans was determined1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Molecular hashkeys: a novel method for molecular characterization and its application for predicting important pharmaceutical properties of molecules.
AID288810Binding affinity to human alpha1-acid glycoprotein at 30 uM2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein.
AID407140Cytotoxicity against human Hep G2.2.15 cells2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
AID288811Binding affinity to 30 uM human serum albumin at 30 uM2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein.
AID1150164Anticonvulsion activity in mouse assessed as protection against pentylenetetrazole-induced convulsion1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID194134Halving of lever pressing in non punished rats, ED50 value reported as log 1/C1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID1136389Effect on motor activity in ip dosed albino CF-1 mouse by dish test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1136388Effect on motor activity in ip dosed albino CF-1 mouse by chimney test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1136390Effect on motor activity in ip dosed albino CF-1 mouse by pedestal test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID130033Evaluated for seizure threshold test at a dose 0.2 mg/kg &MMT is the maximal metrazole threshold to tonic flexion.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID28392Apparent permeability coefficient (Papp) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID679756TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Nordazepam: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID28399Cellular permeability (Pc) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID130035Evaluated for seizure threshold test at a dose 0.2 mg/kg &MST is the metrazole seizure threshold to persistent clonus1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID23479Partition coefficient (logP)1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID1136391Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of nicotine-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1150161Sedative activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID1136397Anxiolytic activity in ip dosed albino CF-1 mouse under hypoxic stress1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1136396Antidepressant activity in ip dosed albino CF-1 mouse assessed as inhibition of ethanol-induced response1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID26380Dissociation constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID407139Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBsAg secretion2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
AID1136395Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of maximal electric shock-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID1150165Muscle relaxant activity in cat suspended by scruff of neck assessed as relaxation of body and hind legs1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID29360Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID13308-Log C was determined by performing the pentylenetetrazole test1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Decomposition of pharmacological activity indices into mutually independent components using principal component analysis.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID227698Evaluation for the Anti-pentylenetetrazole effect.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID1727019Half life in human2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
AID40995Binding affinity towards benzodiazepine/GABA A receptor.1995Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.
AID1150162Muscle relaxant activity in mouse1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1136393Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of thiosemicarbazide-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID131372Effective dose (ED50) was determined in sc Met (pentylenetetrazole) seizure threshold test1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID18847Percent of drug absorbed by human intestine after oral administration2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID42169Binding affinity for umolar GABA-A central benzodiazepine receptor1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID40987Binding affinity of compound towards Benzodiazepine receptor in a competition assay1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors.
AID231333Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID227697Compound was evaluated for the Anti-fighting behavior.1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Neural networks applied to quantitative structure-activity relationship analysis.
AID194131ED50 value was reported as log1/C, which is the concentration required to reduce locomotor activity by 50% in rats1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID55601The compound was tested for cytotoxicity against DAOY (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID136091Compound was determined in rotarod test and expressed as TD501984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID1136392Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced seizures1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID13307-Log C was determined by performing the maximum electroshock test1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Decomposition of pharmacological activity indices into mutually independent components using principal component analysis.
AID166691The compound was tested for cytotoxicity against RG-2 (Rat) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID200783The compound was tested for cytotoxicity against SF-126 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID13306-Log C was determined by performing the incl screen test1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Decomposition of pharmacological activity indices into mutually independent components using principal component analysis.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID407138Antiviral activity against hepatitis B virus infected Hep G2.2.15 cells assessed as inhibition of HBeAg secretion2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
AID13304-Log C was determined by performing the electroshock minimum test1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Decomposition of pharmacological activity indices into mutually independent components using principal component analysis.
AID44482The compound was tested for cytotoxicity against C6 (Rat) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID599144Intrinsic solubility, log 1/S0 of the compound2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Computational aqueous solubility prediction for drug-like compounds in congeneric series.
AID139100Logarithm of effective dose evaluated using the foot-shock test in mice1983Journal of medicinal chemistry, Aug, Volume: 26, Issue:8
Quantitative structure-activity relationships employing independent quantum chemical indices.
AID194132Fourfod increase in lever pressing in punished rats, ED50 value reported as log1/C1980Journal of medicinal chemistry, Feb, Volume: 23, Issue:2
Rm values and structure-activity relationship of benzodiazepines.
AID55444The compound was tested for cytotoxicity against D283 MR (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID55572The compound was tested for cytotoxicity against D341 MR (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID1136387Effect on motor activity in ip dosed albino CF-1 mouse by traction test1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID55598The compound was tested for cytotoxicity against DAOY MR (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID130036Evaluated for seizure threshold test at a dose 1 mg/kg &MMT is the maximal metrazole threshold to tonic flexion.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID1150163Taming activity in mouse assessed as suppression of electrical current-induced aggressive behavior by foot-shock test1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones.
AID407141Selectivity index, ratio of CC50 for human Hep G2.2.15 cells to IC50 for HBV surface antigen secretion2008Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
AID55448The compound was tested for cytotoxicity against D283 (human) Glioma cell lines1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
AID130037Evaluated for seizure threshold test at a dose 1 mg/kg &MST is the metrazole seizure threshold to persistent clonus1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (481)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990274 (56.96)18.7374
1990's96 (19.96)18.2507
2000's46 (9.56)29.6817
2010's49 (10.19)24.3611
2020's16 (3.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.01

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.01 (24.57)
Research Supply Index6.41 (2.92)
Research Growth Index4.35 (4.65)
Search Engine Demand Index76.15 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials80 (15.15%)5.53%
Reviews12 (2.27%)6.00%
Case Studies38 (7.20%)4.05%
Observational1 (0.19%)0.25%
Other397 (75.19%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]