Page last updated: 2024-08-05 15:32:17

GABAA receptor antagonist

null

ChEBI ID: 145515

Members (1)

MemberDefinitionClass
bicucullineA benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.bicuculline

Research

Studies (6,041)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901,588 (26.29)18.7374
1990's1,847 (30.57)18.2507
2000's1,705 (28.22)29.6817
2010's816 (13.51)24.3611
2020's85 (1.41)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials3 (0.05%)5.53%
Reviews65 (1.04%)6.00%
Case Studies1 (0.02%)4.05%
Observational0 (0.00%)0.25%
Other6,184 (98.90%)84.16%

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
chromobox protein homolog 1Homo sapiens (human)Potency79.432811
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency25.118911
gemininHomo sapiens (human)Potency2.310911
importin subunit beta-1 isoform 1Homo sapiens (human)Potency70.794611
snurportin-1Homo sapiens (human)Potency70.794611
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.794611

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-4Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-5Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit deltaHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit epsilonHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-1Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit gamma-3Homo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit piHomo sapiens (human)IC5015.000011
Gamma-aminobutyric acid receptor subunit thetaHomo sapiens (human)IC5015.000011