GABAB receptor: a site of therapeutic benefit.
Although the presence of functional GABAB receptors in mammalian brain has been known for more than 20 years, there is still only one therapeutic agent in use, baclofen, which mediates its effects directly via this receptor. However, activation of this receptor can produce numerous effects that might be amenable to drug development. Evidence from preclinical studies also suggests that antagonism of the GABAB receptor produces beneficial clinical effects.
Bowery
Norman G
NG
GlaxoSmithKline, Verona Biology, Psychiatry Centre of Excellence for Drug Discovery - Psychiatry, Via A Fleming 4, 37135 Verona, Italy. Norman.2.Bowery@GSK.com
D000818:Animals; D001418:Baclofen / Q000494:pharmacology* / Q000627:therapeutic use; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002986:Clinical Trials as Topic; D003071:Cognition / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004832:Epilepsy, Absence / Q000188:drug therapy / Q000378:metabolism; D018755:GABA Agonists / Q000494:pharmacology* / Q000627:therapeutic use; D018756:GABA Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D009128:Muscle Spasticity / Q000188:drug therapy / Q000378:metabolism; D009943:Organophosphorus Compounds / Q000494:pharmacology / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy / Q000378:metabolism; D018080:Receptors, GABA-B / Q000145:classification / Q000187:drug effects* / Q000378:metabolism; D019966:Substance-Related Disorders / Q000188:drug therapy / Q000378:metabolism
D018755:GABA Agonists; D018756:GABA Antagonists; D009943:Organophosphorus Compounds; D018080:Receptors, GABA-B; C079148:(3-aminopropyl)(n-butyl)phosphinic acid; D001418:Baclofen