Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00403

Target Information
NameGamma-aminobutyric acid receptor subunit alpha-1    
Type of targetSuccessful target    
SynonymsGABA(A) receptor subunit alpha-1    
GABRA1    
DiseaseAnxiety disorders
[ICD9: 300   ICD10: F40-F42]
[1]
Insomnia
[ICD9: 307.41, 307.42, 327.0, 780.51, 780.52   ICD10: F51.0, G47.0]
[1]
Drug(s)AmobarbitalApprovedInsomnia[2][3]
BarbitalApprovedInsomnia[2][3]
Barbituric acidApprovedDepression[2][3]
ButabarbitalApprovedInsomnia[2][1][3]
ButalbitalApprovedHeadache[2]
ButethalApprovedInsomnia[2]
ClobazamApprovedEpilepsy and anxiety disorder[2]
EthanolApprovedIntractable chronic pain[2]
EthchlorvynolApprovedInsomnia[2]
EtomidateApprovedAnesthetic[2][4]
FlumazenilApprovedGeneral anesthesia[2]
HalazepamApprovedAnxiety disorder[2]
HexobarbitalApprovedAnesthetic[2][3]
MeprobamateApprovedAnxiety disorder[2]
MetharbitalApprovedEpilepsy[2]
MethohexitalApprovedAnesthetic[2]
MethoxyfluraneApprovedAnesthetic[2]
MethylphenobarbitalApprovedAnxiety disorder[2][3]
MethyprylonApprovedInsomnia[2]
NitrazepamApprovedInsomnia[2]
PentobarbitalApprovedInsomnia[2][3]
PicrotoxinApprovedRespiratory distress[2]
PrazepamApprovedAnxiety disorder[2]
PrimidoneApprovedEpilepsy[2]
QuazepamApprovedInsomnia[2]
SecobarbitalApprovedInsomnia[2][3]
TalbutalApprovedSedation[2]
ThiamylalApprovedAnesthesia[2]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP14867
SequenceMRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target ValidationClick to Find Target Validation Information.    
Inhibitor (4R)-4-ammoniopentanoate[5]
(4S)-4-ammoniopentanoate[5]
ALLOPREGNANOLONE[6]
AMENTOFLAVONE[7]
BETA-CCM[8]
Barbital[9]
Barbituric acid derivative[9]
CGP-27492[10]
CGS-13767[11]
CGS-8216[11]
CGS-9895[12]
CGS-9896[13]
CI-218872[14]
Divaplon[15]
ELTANOLONE[6]
GABAZINE[16]
GABAZINE[17]
GAMMA-AMINO-BUTANOIC ACID[18]
GNF-PF-3645[19]
GNF-PF-4421[19]
NORHARMANE[20]
NSC-19028[21]
NSC-73613[21]
NSC-93394[21]
PNU-91571[22]
RIPAZEPAM[23]
RO-054520[24]
RO-145974[25]
RO-145975[25]
RO-147437[25]
RO-194603[25]
RWJ-16979[26]
RY-066[27]
Ro-151310[25]
Ro-154513[25]
Ro-4882224[28]
Ro-4938581[28]
THIOCOLCHICOSIDE[18]
TPA-023[29]
U-78875[22]
U-89267[30]
ZK-93423[31]
AntagonistAmobarbital[2][3]
Barbital[2][3]
Barbituric acid[2][3]
Butabarbital[2][1][3]
Butalbital[2]
Butethal[2]
Clobazam[2]
Ethanol[2]
Ethchlorvynol[2]
Etomidate[2][4]
Flumazenil[2]
Halazepam[2]
Hexobarbital[2][3]
Meprobamate[2]
Metharbital[2]
Methohexital[2]
Methoxyflurane[2]
Methylphenobarbital[2][3]
Methyprylon[2]
Nitrazepam[2]
Pentobarbital[2][3]
Picrotoxin[2]
Prazepam[2]
Primidone[2]
Quazepam[2]
Secobarbital[2][3]
Talbutal[2]
Thiamylal[2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Hypnotic drugs. Med Lett Drugs Ther. 2000 Aug 7;42(1084):71-2. To Reference
Ref 2DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. To Reference
Ref 3Effect of barbiturates on polyphosphoinositide biosynthesis and protein kinase C activity in synaptosomes. Neuropharmacology. 1989 Dec;28(12):1317-23. To Reference
Ref 4Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. To Reference
Ref 5J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 6J Med Chem. 2005 Apr 21;48(8):3051-9.Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one. To Reference
Ref 7Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 8J Med Chem. 1995 Jan 6;38(1):189-98.Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high affinities for the benzodiazepine receptor. To Reference
Ref 9Whiting 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 10J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. To Reference
Ref 11J Med Chem. 1991 Jan;34(1):281-90.Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. To Reference
Ref 12J Med Chem. 1987 Oct;30(10):1737-42.1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. To Reference
Ref 13J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. To Reference
Ref 14J Med Chem. 1994 Dec 23;37(26):4576-80.Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. To Reference
Ref 15J Med Chem. 1988 Jun;31(6):1220-6.(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics. To Reference
Ref 16J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. To Reference
Ref 17J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. To Reference
Ref 18J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. To Reference
Ref 19J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling. To Reference
Ref 20J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. To Reference
Ref 21Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997) To Reference
Ref 22J Med Chem. 1999 Apr 8;42(7):1123-44.Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. To Reference
Ref 23J Med Chem. 1985 May;28(5):683-5.Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in rat cerebral cortex. To Reference
Ref 24J Med Chem. 1988 Dec;31(12):2235-46.Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. To Reference
Ref 25J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors. To Reference
Ref 26J Med Chem. 1995 Jan 6;38(1):16-20.Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. To Reference
Ref 27J 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 28Bioorg 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 29J 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
Ref 30J Med Chem. 1994 Mar 18;37(6):758-68.Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. To Reference
Ref 31J Med Chem. 1990 Mar;33(3):1062-9.Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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