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Advantages of an antagonist: bicuculline and other GABA antagonists
Author(s) -
Johnston Graham AR
Publication year - 2013
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12127
Subject(s) - bicuculline , gabaa receptor , gaba receptor antagonist , pharmacology , ionotropic effect , chemistry , antagonist , neuroscience , convulsants , receptor , biology , biochemistry , anticonvulsant , epilepsy , nmda receptor
The convulsant alkaloid bicuculline continues to be investigated more than 40 years after the first publication of its action as an antagonist of receptors for the inhibitory neurotransmitter GABA . This historical perspective highlights key aspects of the discovery of bicuculline as a GABA antagonist and the sustained interest in this and other GABA antagonists. The exciting advances in the molecular biology, pharmacology and physiology of GABA receptors provide a continuing stimulus for the discovery of new antagonists with increasing selectivity for the myriad of GABA receptor subclasses. Interesting GABA antagonists not structurally related to bicuculline include gabazine, salicylidene salicylhydrazide, RU5135 and 4‐(3‐biphenyl‐5‐(4‐piperidyl)‐3‐isoxazole. Bicuculline became the benchmark antagonist for what became known as GABA A receptors, but not all ionotropic GABA receptors are susceptible to bicuculline. In addition, not all GABA A receptor antagonists are convulsants. Thus there are still surprises in store as the study of GABA receptors evolves.

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