Is the GABA B heterodimer a good drug target?
GABA(B) receptors are a member of the G protein-coupled family of receptors which are generally considered to be excellent drug targets. Cloning of the GABA(B) receptor demonstrated that, unlike other G protein-coupled receptors, it is an obligate heterodimer. Drugs acting at GABA(B) receptors have the potential to treat a wide variety of diseases. Activation of the receptors may have utility in the treatment of pain, drug-dependence, and anxiety, whereas blockade of receptors may have benefit in cognitive disorders and depression. To date, development of drugs has been hampered by the lack of receptor subtypes and the inability to separate therapeutic benefit from side effects such as sedation. Recently, novel compounds that act via an allosteric mechanism have been identified and are providing hope that future drugs may be developed that target this receptor.
Marshall
Fiona H
FH
Department of Pharmacology, University of Cambridge, Cambridge CB2 1QJ, UK. Fhm24@cam.ac.uk
D000818:Animals; D001418:Baclofen / Q000494:pharmacology; D001921:Brain / Q000502:physiology; D003072:Cognition Disorders / Q000188:drug therapy; D003863:Depression / Q000188:drug therapy; D019281:Dimerization; D018755:GABA Agonists / Q000494:pharmacology; D018756:GABA Antagonists / Q000494:pharmacology; D006801:Humans; D018080:Receptors, GABA-B / Q000737:chemistry* / Q000187:drug effects / Q000378:metabolism*
D018755:GABA Agonists; D018756:GABA Antagonists; D018080:Receptors, GABA-B; D001418:Baclofen