Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00019

Target Information
NameGamma-aminobutyric acid A receptor    
Type of targetSuccessful target    
SynonymsGABA(A) receptor    
GABA-A receptor    
DiseaseAlcoholism
[ICD9: 303   ICD10: F10.2]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[2]
Disorders of initiating and maintaining sleep [insomnias]
[ICD9: 710.0   ICD10: M32]
[2]
Dyskinesia
[ICD9: 333.8   ICD10: G24.9]
[3][4]
Epilepsy
[ICD9: 345   ICD10: G40]
[1]
Hyperkinetic extrapyramidal movement disorders
[ICD9: 333.9, 781.0   ICD10: F44.4, F98.4, G25.8-G25.9, R25]
[5]
Neurological diseases[6]
Primary headache disorders
[ICD9: 339, 784.0   ICD10: G43-G44, R51]
[7]
Drug(s)AcamprosateApprovedAlcohol dependence[8]
AprobarbitalApprovedInsomnia[9]
BarbiturateApprovedAnaesthesia[10]
BromazepamApprovedAnxiety or panic attacks[11]
DiazepamApprovedPain, Anesthesia and Anxiety[12][13][14]
DihydroergotoxineApprovedAlzheimer's disease[15]
Fospropofol disodiumApprovedMonitored anaesthesia care sedation
GaboxadolApprovedInsomnia[16]
HeptabarbitalApprovedAnesthesia[17]
IsofluraneApprovedAnesthetic[18][19]
LindaneApprovedInfestations of lice and scabies[20]
ZolpidemApprovedInsomnia[21][22][23]
ZopicloneApprovedInsomnia[24][25][26]
AZD7325Phase II completedAnxiety[27]
AZD6280Phase I completedAnxiety; Schizophrenia[27]
ELB-139Phase ISchizophrenia[13]
ELB-139Terminated in Phase II Anxiety[13]
OcinaplonHalted in Phase IIIGeneralized anxiety disorder[13]
TP-023PreclinicalAnxiety[13]
TPT-43PreclinicalAlzheimer's Disease[13]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Agonist4,5,6,7-tetrahydroisoxazolo-[5,4-c]-pyridin-3-ol[28]
AZD6280[27]
AZD7325[27]
Acamprosate[8]
Barbiturate[10]
Diazepam[12][13][14]
Dihydroergotoxine[15]
GABA[28]
Gaboxadol[16]
Isoflurane[18][19]
Isoguvacine[6]
Muscimol[6]
THIP[6]
AntagonistBicuculline[29]
Heptabarbital[17]
Lindane[20]
N-methylbicuculline[7]
ModulatorELB-139[13]
Ocinaplon[13]
TP-023[13]
TPT-43[13]
BinderAprobarbital[9]
Bromazepam[11]
Zolpidem[21][22][23]
Zopiclone[24][25][26]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Suppression by progabide of ethanol withdrawal syndrome in rats. Eur J Pharmacol. 1985 Mar 12;109(3):321-5. To Reference
Ref 2GABA mechanisms and sleep. Neuroscience. 2002;111(2):231-9. To Reference
Ref 3Pharmacological and therapeutic actions of GABA receptor agonists. J Neural Transm Suppl. 1983;18:319-26. To Reference
Ref 4Therapeutic response to progabide in neuroleptic- and L-dopa-induced dyskinesias. Clin Neuropharmacol. 1987 Jun;10(3):238-46. To Reference
Ref 5Progabide in the treatment of hyperkinetic extrapyramidal movement disorders. Acta Neurol Scand. 1985 Sep;72(3):341-3. To Reference
Ref 6Curr Top Med Chem. 2002 Aug;2(8):817-32.GABA(A) receptor ligands and their therapeutic potentials. To Reference
Ref 7GABA receptors modulate trigeminovascular nociceptive neurotransmission in the trigeminocervical complex. Br J Pharmacol. 2001 Oct;134(4):896-904. To Reference
Ref 8Predicting the effect of naltrexone and acamprosate in alcohol-dependent patients using genetic indicators. Addict Biol. 2009 Jul;14(3):328-37. To Reference
Ref 9Determination of zidovudine/lamivudine/nevirapine in human plasma using ion-pair HPLC. J Pharm Biomed Anal. 2002 Jun 1;28(5):903-8. To Reference
Ref 10Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79. To Reference
Ref 11Glutamatergic and GABAergic modulations of ultrasonic vocalizations during maternal separation distress in mouse pups. Psychopharmacology (Berl). 2009 May;204(1):61-71. Epub 2008 Dec 20. To Reference
Ref 12Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
Ref 13Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. To Reference
Ref 14The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18. To Reference
Ref 15Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97. To Reference
Ref 16Highway driving performance and cognitive functioning the morning after bedtime and middle-of-the-night use of gaboxadol, zopiclone and zolpidem. J Sleep Res. 2009 Jun 22. [Epub ahead of print] To Reference
Ref 17A computer program using disposition decomposition analysis in pharmacodynamics. Biopharm Drug Dispos. 1997 Jan;18(1):9-15. To Reference
Ref 18Transmembrane residues define the action of isoflurane at the GABAA receptor alpha-3 subunit. Brain Res. 2005 Jan 25;1032(1-2):30-5. To Reference
Ref 19Effects of GABAergic agents on anesthesia induced by halothane, isoflurane, and thiamylal in mice. Pharmacol Biochem Behav. 2002 May;72(1-2):111-6. To Reference
Ref 20NMDA-induced seizure intensity is enhanced in COX-2 deficient mice. Neurotoxicology. 2008 Nov;29(6):1114-20. Epub 2008 Sep 11. To Reference
Ref 21Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. Epub 2009 Apr 1. To Reference
Ref 22The impact of age on the hypnotic effects of eszopiclone and zolpidem in the guinea pig. Psychopharmacology (Berl). 2009 Jul;205(1):107-17. Epub 2009 Apr 3. To Reference
Ref 23Dependence on zolpidem: a report of two cases. Encephale. 2004 Mar-Apr;30(2):153-5. To Reference
Ref 24Eszopiclone: its use in the treatment of insomnia. Neuropsychiatr Dis Treat. 2007 Aug;3(4):441-453. To Reference
Ref 25The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents. CNS Drugs. 2004;18 Suppl 1:9-15; discussion 41, 43-5. To Reference
Ref 26Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 27AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 28Reduction in potency of selective gamma-aminobutyric acidA agonists and diazepam in CA1 region of in vitro hippocampal slices from chronic flurazepam-treated rats. J Pharmacol Exp Ther. 1992 Jul;262(1):204-11. To Reference
Ref 29Effects of subcutaneous administration of the gamma-aminobutyric acid(A) receptor agonist muscimol on water intake in water-deprived rats. Physiol Behav. 2002 Nov;77(2-3):445-50. To Reference



 

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