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    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[2]
Asthma
[ICD9: 493   ICD10: J45]
[3]
Cognitive deficits
[ICD9: 290-294, 294.0, 780.09, 780.9, 780.93   ICD10: F01-F07, F04, R41.3]
[2]
Convulsions
[ICD9: 780.3   ICD10: R56.0]
[4]
Depression
[ICD9: 311   ICD10: F32]
[2]
Dyskinesia
[ICD9: 333.8   ICD10: G24.9]
[5][6]
Epilepsy
[ICD9: 345   ICD10: G40]
[2]
Gastroesophageal reflux disease
[ICD9: 530   ICD10: K21]
[7]
Hyperkinetic extrapyramidal movement disorders
[ICD9: 333.9, 781.0   ICD10: F44.4, F98.4, G25.8-G25.9, R25]
[8]
Meige's disease[9]
Neurological diseases[10]
Nociceptive disorders[2]
Parkinson's disease
[ICD9: 332   ICD10: F02.3, G20]
[11]
Psychiatric illness[10]
Drug(s)BaclofenApprovedMultiple sclerosis[12][13][7][9]
GabapentinApprovedPartial Seizures[14]
ProgabideApprovedDepression[15][16][17]
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]
([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]
(R)-4-Amino-3-[23]
(R)-5-Amino-3-[23]
3-Amino-propane-1-sulfonic acid[22]
3-ammoniopropane-1-sulfinate[24]
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]
CGP-27492[22]
CGP-34938[20]
CGP-35024[22]
CGP-35348[22]
CGP-35582[20]
CGP-36216[22]
GAMMA-AMINO-BUTANOIC ACID[25]
Agonist (+/-)-baclofen[3]
AZD3355[18]
Baclofen[12][13][7][9]
CGP-44532[19][27]
Progabide[15][16][17]
SKF-97541[27]
AntagonistGabapentin[14]
Phaclofen[28][29]
SCH 50911[11]
SGS-742[19][4]
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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543