Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01177

Target Information
NameGamma-aminobutyric-acid receptor alpha-2 subunit    
Type of targetResearch target    
SynonymsGABA(A)Gamma-aminobutyric-acid receptor alpha-2 subunit precursor receptor    
GABA-A receptor alpha 2    
DiseaseAnxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Disorders of initiating and maintaining sleep [insomnias]
[ICD9: 710.0   ICD10: M32]
[1]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP47869
FunctionGABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the gaba/benzodiazepine receptor and opening an integral chloride channel.    
SequenceMKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
Related US Patent6,399,608
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2E,4S)-4-ammoniopent-2-enoate[2]
(4R)-4-ammoniopentanoate[2]
(4S)-4-ammoniopentanoate[2]
3- (benzyloxy)-9H-pyrido[3,4-b]indole[3]
3- (hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole[3]
3- (isopentyloxy)-9H-pyrido[3,4-b]indole[3]
3-Ethoxy-9H-beta-carboline[4]
3-butoxy-9H-pyrido[3,4-b]indole[3]
3-ethoxy-9H-pyrido[3,4-b]indole[3]
3-isobutoxy-9H-pyrido[3,4-b]indole[3]
3-propoxy-9H-pyrido[3,4-b]indole[3]
5-[ (1R)-1-ammonioethyl]isoxazol-3-olate[2]
5-[ (1S)-1-ammonioethyl]isoxazol-3-olate[2]
AMENTOFLAVONE[5]
Barbital[6]
Barbituric acid derivative[6]
CGS-17867A[7]
CI-218872[3]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate[3]
GAMMA-AMINO-BUTANOIC ACID[8]
L-655708,   NCGC00025115-02[9]
RY-066[10]
Ro-151310[11]
Ro-154513[12]
Ro-4882224[13]
Ro-4938581[13]
TPA-023[14]
beta-Carboline-3-carboxylic acid t-butyl ester[3]
ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate[3]
sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1GABA mechanisms and sleep. Neuroscience. 2002;111(2):231-9. To Reference
Ref 2J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 3Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. To Reference
Ref 4J 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. To Reference
Ref 5Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 6Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. To Reference
Ref 7Bioorg 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. To Reference
Ref 8J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. To Reference
Ref 9J 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. To Reference
Ref 10J 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. To Reference
Ref 11Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. To Reference
Ref 12J 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. To Reference
Ref 13Bioorg 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. To Reference
Ref 14J Med Chem. 2005 Nov 17;48(23):7089-92.7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. To Reference



 

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