Target Information
Target General Infomation | |||||
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Target ID |
T51452
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Former ID |
TTDR01177
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Target Name |
Gamma-aminobutyric-acid receptor alpha-2 subunit
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Gene Name |
GABRA2
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Synonyms |
GABA(A)Gamma-aminobutyric-acid receptor alpha-2 subunit precursor receptor; GABA-A receptor alpha 2; GABRA2
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Target Type |
Discontinued
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Disease | Alcohol use disorders [ICD9: 303; ICD10: F10.2] | ||||
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0] | |||||
Unspecified [ICD code not available] | |||||
Function |
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
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BioChemical Class |
Neurotransmitter receptor
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Target Validation |
T51452
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UniProt ID | |||||
Sequence |
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM SRIVFPVLFGTFNLVYWATYLNREPVLGVSP |
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Drugs and Mode of Action | |||||
Inhibitor | (2E,4S)-4-ammoniopent-2-enoate | Drug Info | [533514] | ||
(4R)-4-ammoniopentanoate | Drug Info | [533514] | |||
(4S)-4-ammoniopentanoate | Drug Info | [533514] | |||
3-(benzyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-(isopentyloxy)-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-butoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-Ethoxy-9H-beta-carboline | Drug Info | [534660] | |||
3-ethoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-isobutoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
3-propoxy-9H-pyrido[3,4-b]indole | Drug Info | [531188] | |||
5-[(1R)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [533514] | |||
5-[(1S)-1-ammonioethyl]isoxazol-3-olate | Drug Info | [533514] | |||
AMENTOFLAVONE | Drug Info | [526653] | |||
Barbituric acid derivative | Drug Info | [551407] | |||
Beta-Carboline-3-carboxylic acid t-butyl ester | Drug Info | [531188] | |||
CGS-17867A | Drug Info | [527100] | |||
CI-218872 | Drug Info | [531188] | |||
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
GAMMA-AMINO-BUTANOIC ACID | Drug Info | [533580] | |||
L-655708 | Drug Info | [527005] | |||
Ro-151310 | Drug Info | [531044] | |||
Ro-154513 | Drug Info | [534122] | |||
Ro-4938581 | Drug Info | [530391] | |||
RY-066 | Drug Info | [534718] | |||
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | [531188] | |||
Modulator (allosteric modulator) | alpha3IA | Drug Info | [543809] | ||
alpha5IA | Drug Info | [543809] | |||
DMCM | Drug Info | [543809] | |||
tetrahydrodeoxycorticosterone | Drug Info | [543809] | |||
TP003 | Drug Info | [543809] | |||
[11C]flumazenil | Drug Info | [543809] | |||
[18F]fluoroethylflumazenil | Drug Info | [543809] | |||
[3H]CGS8216 | Drug Info | [543809] | |||
Agonist | isonipecotic acid | Drug Info | [543809] | ||
piperidine-4-sulphonic acid | Drug Info | [543809] | |||
[3H]muscimol | Drug Info | [543809] | |||
Modulator | MK-0343 | Drug Info | |||
MRK016 | Drug Info | ||||
PF-4480682 | Drug Info | [550179] | |||
Blocker (channel blocker) | TBPS | Drug Info | [543809] | ||
[35S]TBPS | Drug Info | [543809] | |||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Retrograde endocannabinoid signaling | |||||
GABAergic synapse | |||||
Morphine addiction | |||||
Nicotine addiction | |||||
Reactome | Ligand-gated ion channel transport | ||||
GABA A receptor activation | |||||
WikiPathways | Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell | ||||
Iron uptake and transport | |||||
References | |||||
Ref 526653 | Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. | ||||
Ref 527005 | J Med Chem. 2004 Mar 25;47(7):1807-22.3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. | ||||
Ref 527100 | Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. | ||||
Ref 530391 | Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction. | ||||
Ref 531044 | Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. | ||||
Ref 531188 | Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. | ||||
Ref 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 533580 | J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. | ||||
Ref 534122 | J Med Chem. 1996 Apr 26;39(9):1928-34.Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors. | ||||
Ref 534660 | J Med Chem. 1998 Jul 2;41(14):2537-52.Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors. | ||||
Ref 534718 | J Med Chem. 1998 Oct 8;41(21):4130-42.Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis. |
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