Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00022

Target Information
NameGamma-aminobutyric acid B receptor    
Type of targetSuccessful target    
SynonymsGABA B receptor    
GABA(B) receptor    
GABAB receptor    
Gamma-aminobutyric acid type b receptor    
[ICD9: 338   ICD10: R52]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[ICD9: 493   ICD10: J45]
Cognitive deficits
[ICD9: 290-294, 294.0, 780.09, 780.9, 780.93   ICD10: F01-F07, F04, R41.3]
[ICD9: 780.3   ICD10: R56.0]
[ICD9: 311   ICD10: F32]
[ICD9: 333.8   ICD10: G24.9]
[ICD9: 345   ICD10: G40]
Gastroesophageal reflux disease
[ICD9: 530   ICD10: K21]
Hyperkinetic extrapyramidal movement disorders
[ICD9: 333.9, 781.0   ICD10: F44.4, F98.4, G25.8-G25.9, R25]
Meige's disease[9]
Neurological diseases[10]
Nociceptive disorders[2]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
Psychiatric illness[10]
Drug(s)BaclofenApprovedMultiple sclerosis[12][13][7][9]
GabapentinApprovedPartial Seizures[14]
SSTarbaclofenPhase IIIFragile X syndrome
STX209Phase IIIFragile X syndrome, fragile X syndrome (pediatric)
AZD3355Phase II completedGastroesophageal Reflux Disease[18]
SGS-742Phase II completedAlzheimer's Disease[19][4]
SSTarbaclofenPhase IIAutism spectrum disorders
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
Related US Patent6,664,069
Target ValidationClick to Find Target Validation Information.    
Inhibitor ([20]
(3-Amino-1-ethyl-propyl)-methyl-phosphinic acid[20]
(3-Amino-1-hydroxy-propyl)-methyl-phosphinic acid[20]
(3-Amino-phenyl)-phosphonic acid diphenyl ester[21]
(3-Amino-propyl)-difluoromethyl-phosphinic acid[20]
(3-Amino-propyl)-hexyl-phosphinic acid[22]
(3-Amino-propyl)-hydroxymethyl-phosphinic acid[20]
(3-Amino-propyl)-phosphonic acid[21]
3-Amino-propane-1-sulfonic acid[22]
4-Amino-3- (2-chloro-phenyl)-butyric acid[25]
4-Amino-3- (4-fluoro-phenyl)-butyric acid[25]
4-Amino-3- (5-bromo-thiophen-2-yl)-butyric acid[25]
4-Amino-3- (5-chloro-thiophen-2-yl)-butyric acid[25]
4-Amino-3- (5-methyl-thiophen-2-yl)-butyric acid[25]
4-Amino-3-benzofuran-2-yl-butyric acid[26]
4-Amino-3-thiophen-2-yl-butyric acid[25]
Agonist (+/-)-baclofen[3]
SCH 50911[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Challenges in Analgesic Drug Development. Clin Pharmacol Ther. 2009 Aug 12. To Reference
Ref 2Heterodimerization of a functional GABAB receptor is mediated by parallel coiled-coil alpha-helices. Biochemistry. 1999 Oct 5;38(40):13263-9. To Reference
Ref 3GABAB receptor modulation of the release of substance P from capsaicin-sensitive neurones in the rat trachea in vitro. Br J Pharmacol. 1991 Apr;102(4):801-4. To Reference
Ref 4The new generation of GABA enhancers. Potential in the treatment of epilepsy. CNS Drugs. 2001;15(5):339-50. To Reference
Ref 5Pharmacological and therapeutic actions of GABA receptor agonists. J Neural Transm Suppl. 1983;18:319-26. To Reference
Ref 6Therapeutic response to progabide in neuroleptic- and L-dopa-induced dyskinesias. Clin Neuropharmacol. 1987 Jun;10(3):238-46. To Reference
Ref 7Control of transient lower oesophageal sphincter relaxations and reflux by the GABA(B) agonist baclofen in patients with gastro-oesophageal reflux disease. Gut. 2002 Jan;50(1):19-24. To Reference
Ref 8Progabide in the treatment of hyperkinetic extrapyramidal movement disorders. Acta Neurol Scand. 1985 Sep;72(3):341-3. To Reference
Ref 9Treatment of Meige disease with a GABA receptor agonist. Arq Neuropsiquiatr. 1985 Sep;43(3):260-6. To Reference
Ref 10GABA(B) receptors as potential therapeutic targets. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):248-59. To Reference
Ref 11Activation of nigral dopamine neurons by the selective GABA(B)-receptor antagonist SCH 50911. J Neural Transm. 1999;106(5-6):383-94. To Reference
Ref 12N-type calcium channels mediate a GABA(B) presynaptic modulation in the corticostriatal synapse in turtle's paleostriatum augmentatum. Synapse. 2009 Jun 26;63(10):855-862. [Epub ahead of print] To Reference
Ref 13Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Jun 15. [Epub ahead of print] To Reference
Ref 14Gabapentin increases a tonic inhibitory conductance in hippocampal pyramidal neurons. Anesthesiology. 2006 Aug;105(2):325-33. To Reference
Ref 15Interactions between dopamine and GABA in the control of ambulatory activity and neophobia in the mouse. Pharmacol Biochem Behav. 1998 Jan;59(1):239-47. To Reference
Ref 16Pentobarbital-like discriminative stimulus effects of direct GABA agonists in rats. Psychopharmacology (Berl). 1993;110(3):295-301. To Reference
Ref 17Suppression by progabide of ethanol withdrawal syndrome in rats. Eur J Pharmacol. 1985 Mar 12;109(3):321-5. To Reference
Ref 18AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 19Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. To Reference
Ref 20J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. To Reference
Ref 21J Med Chem. 1984 May;27(5):654-9.Phosphorus analogues of gamma-aminobutyric acid, a new class of anticonvulsants. To Reference
Ref 22Bioorg. Med. Chem. Lett. 3(4):515-518 (1993) To Reference
Ref 23J Med Chem. 1999 Jun 3;42(11):2053-9.Synthesis and pharmacology of the baclofen homologues 5-amino-4-(4-chlorophenyl)pentanoic acid and the R- and S-enantiomers of 5-amino-3-(4-chlorophenyl)pentanoic acid. To Reference
Ref 24Bioorg. Med. Chem. Lett. 6(14):1709-1714 (1996) To Reference
Ref 25J Med Chem. 1991 Aug;34(8):2557-60.3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies. To Reference
Ref 26J Med Chem. 1987 Apr;30(4):743-6.Synthesis and pharmacological evaluation of gamma-aminobutyric acid analogues. New ligand for GABAB sites. To Reference
Ref 27Inhibition of transient LES relaxations and reflux in ferrets by GABA receptor agonists. Am J Physiol. 1999 Oct;277(4 Pt 1):G867-74. To Reference
Ref 28Astrocytes and Interneurons in Memory Processing in the Chick Hippocampus: Roles for G-Coupled Protein Receptors, GABA(B) and mGluR1. Neurochem Res. 2009 May 5. [Epub ahead of print] To Reference
Ref 29The role of group II and III metabotropic glutamate receptors in modulation of miniature synaptic activity in frog spinal cord motoneurons. Tsitologiia. 2008;50(9):747-56. To Reference


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