Page last updated: 2024-12-07

sr 95531

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

Cross-References

ID SourceID
PubMed CID107896
CHEMBL ID32503
CHEBI ID34968
SCHEMBL ID5529434
MeSH IDM0142644

Synonyms (55)

Synonym
BRD-K79905821-001-01-6
sr95531
PRESTWICK2_000443 ,
PDSP2_001588
gabazine
tocris-1262
NCGC00025088-01
PDSP1_001604
BIOMOL-NT_000259
BPBIO1_000771
NCGC00025088-02
sr 95531
C13796 ,
PRESTWICK0_000443 ,
PRESTWICK1_000443 ,
SPBIO_002425
CHEMBL32503 ,
chebi:34968 ,
FT-0668923
(gabazine)4-[6-imino-3-(4-methoxy-phenyl)-6h-pyridazin-1-yl]-butyric acid
4-[6-imino-3-(4-methoxy-phenyl)-6h-pyridazin-1-yl]-butyric acid(gabazine)
4-(6-imino-3-(4-methoxyphenyl)pyridazin-1(6h)-yl)butanoic acid
bdbm50001572
4-[6-imino-3-(4-methoxy-phenyl)-6h-pyridazin-1-yl]-butyric acid (gabazine or sr-95331)
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid
NCGC00025088-03
105538-73-6
2-(3-carboxypropyl)-3-amino-6-(4-methoxyphenyl)pyridazinium
gtpl4197
[3h]gabazine
4-[6-imino-3-(4-methoxyphenyl)-1,6-dihydropyridazin-1-yl]butanoic acid
gtpl4083
SCHEMBL5529434
gabazine free base
L45297DIU1 ,
1,6-dihydro-6-imino-3-(4-methoxyphenyl)-1-pyridazinebutanoic acid
1(6h)-pyridazinebutanoic acid, 6-imino-3-(4-methoxyphenyl)-
6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinebutanoic acid
4-(6-imino-3-(4-methoxyphenyl)pyridazin-1-yl)butanoic acid
j331.170h ,
4-(6-imino-3-(4-methoxyphenyl)-1(6h)-pyridazinyl)butanoic acid
unii-l45297diu1
zinc02559949
J-001443
DTXSID20276043
6-imino-3-(4-methoxyphenyl)-1(6h )-pyridazinebutanoic acid
AKOS030254307
ACVGNKYJVGNLIL-UHFFFAOYSA-N
Q27894364
4-[6-imino-3-(4-methoxy-phenyl)-6h-pyridazin-1-yl]-butyric acid
BCP33110
sr95531; sr 95531; sr-95531
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid.
G-215
4-(6-imino-3-(4-methoxyphenyl)pyridazin-1(6h)-yl)butanoicacid

Research Excerpts

Effects

ExcerptReferenceRelevance
"SR 95531 has been shown to be a potent, selective, reversible and competitive GABAA antagonist. "( Specific binding of a phenyl-pyridazinium derivative endowed with GABAA receptor antagonist activity to rat brain.
Biziere, K; Chambon, JP; Heaulme, M; Leyris, R; Wermuth, CG, 1986
)
1.71

Actions

ExcerptReferenceRelevance
"The SR 95531-induced increase in DA was blocked by coadministration of GABA."( Tonic inhibition of striatal dopamine transmission: effects of benzodiazepine and GABAA receptor antagonists on extracellular dopamine levels.
Coale, A; Friedhoff, AJ; Gruen, RJ; Moghaddam, B, 1992
)
0.76

Dosage Studied

ExcerptRelevanceReference
"We have investigated the effects of an aryl-aminopyridazine derivative of GABA (SR 95531) on dose-response curves of GABA-induced depolarizations from dorsal root ganglion neurones recorded intracellularly."( Quantitative evaluation of the properties of a pyridazinyl GABA derivative (SR 95531) as a GABAA competitive antagonist. An electrophysiological approach.
Bader, MF; Desarmenien, M; Desaulles, E; Feltz, P; Hamann, M, 1988
)
0.73
" The GABA antagonists 2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride (SR 95103) and 3-alpha-hydroxy-16-imino-5 beta-17-aza-androstan-11-one (R 5135) shifted and suppressed the dose-response curve of GABA on diazepam binding."( GABAA receptor populations bind agonists and antagonists differentially and with opposite affinities.
Maksay, G, 1988
)
0.27
", with a U-shape dose-response relationship."( Inhibition by levetiracetam of a non-GABAA receptor-associated epileptiform effect of bicuculline in rat hippocampus.
Margineanu, DG; Wülfert, E, 1997
)
0.3
" Bilateral VLPO lesions attenuated the sedative response to dexmedetomidine, and the dose-response curve to dexmedetomidine was shifted right by gabazine administered systemically or directly into the TMN."( The alpha2-adrenoceptor agonist dexmedetomidine converges on an endogenous sleep-promoting pathway to exert its sedative effects.
Franks, NP; Guo, T; Lu, J; Maze, M; Nelson, LE; Saper, CB, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
methoxybenzenesAny aromatic ether that consists of a benzene skeleton substituted with one or more methoxy groups.
[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 (31)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
15-lipoxygenase, partialHomo sapiens (human)Potency15.84890.012610.691788.5700AID887
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency3.98110.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.15850.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency3.16230.00636.904339.8107AID883
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.58930.020010.786931.6228AID912
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency3.16230.00638.235039.8107AID883
[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 receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)IC50 (µMol)0.27630.00011.14948.0000AID1638734; AID604340; AID765274
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.24000.00000.21085.6234AID260169
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)IC50 (µMol)0.27630.00011.29158.0000AID1638734; AID604340; AID765274
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.24000.00000.18819.0000AID260169
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.505710.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki5.38270.00020.561410.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.497310.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki5.38270.00020.635210.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki5.38270.00020.621710.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.498810.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki5.38270.00020.675810.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.504610.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki5.38270.00020.646910.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit beta-3Homo sapiens (human)Ki0.24000.00010.20769.0000AID260169
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki5.38270.00020.671210.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)IC50 (µMol)0.27630.00010.93746.0000AID1638734; AID604340; AID765274
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.506510.0000AID71975
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki5.38270.00020.557710.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.505710.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki5.38270.00020.640310.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki5.38270.00020.570810.0000AID1638732; AID1638733; AID72135
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
GABA theta subunitRattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)0.24000.00010.507510.0000AID71975
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki5.38270.00020.656110.0000AID1638732; AID1638733; AID72135
[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)
Gamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)Kb35.00001.50005.750010.0000AID71407
Gamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)Kb35.00000.80003.033310.0000AID71407
Gamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)Kb35.00001.50005.750010.0000AID71407
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-3Homo 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)
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)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
modulation of chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-1Homo 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)
signal transductionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
visual perceptionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit rho-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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
GABA-A receptor activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-3Homo 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-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 rho-1Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
identical protein bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
protein-containing complex bindingGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-1Homo 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)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
protein domain specific bindingGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit rho-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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
cellular_componentGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-3Homo 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)
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 gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
presynaptic membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
glutamatergic synapseGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-1Homo 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)
plasma membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit rho-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit rho-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-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1638747Displacement of [3H]NCS382 from high-affinity GHB binding site of alpha4betadelta receptor in mouse brain membranes2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID71407Agonist activity against Gamma-aminobutyric acid C (GABA-C) receptor derived from bovine retinal RNA expressed in Xenopus oocytes2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.
AID71975Inhibition of Gamma-aminobutyric acid A (GABA-A) receptor in vitro by whole-cell patch-clamp recording in cultured cerebral cortical neurones2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
AID72155Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
AID604341Ratio of IC50 for compound to IC50 for gabazine for human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
AID765274Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins by FLIPR membrane potential blue assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.
AID72135In vitro inhibition of [3H]muscimol to rat brain synaptic membranes2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
AID765275Displacement of [3H] muscimol from rat GABA A receptor2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.
AID72153Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
AID260169Binding affinity at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by voltage-clamp electrophysiology2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
AID1638732Displacement of [3H]muscimol from orthosteric binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID773897Displacement of [3H]-3-hydroxycyclopent-1-enecarboxylic acid from GHB binding site in Sprague-Dawley rat cerebral cortex at 100 uM after 1 hr by scintillation counting analysis2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.
AID260168Displacement of [3H]muscimol from GABAA alpha-1-beta-3-gamma-2S in rat brain membrane2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
AID1638733Displacement of [3H]NCS-382 from high-affinity GHB binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID1638734Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane potential after 16 to 24 hrs by FMP-blue assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
AID604340Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (595)

TimeframeStudies, This Drug (%)All Drugs %
pre-199016 (2.69)18.7374
1990's99 (16.64)18.2507
2000's231 (38.82)29.6817
2010's235 (39.50)24.3611
2020's14 (2.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.17

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.17 (24.57)
Research Supply Index6.42 (2.92)
Research Growth Index5.29 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (0.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other608 (99.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]