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Advantages of an Antagonist: Bicuculline and Other GABA Antagonists

Advantages of an Antagonist: Bicuculline and Other GABA Antagonists

Graham A R Johnston

Br J Pharmacol. 2013 May;169(2):328-36.

PMID: 23425285

Abstract:

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 GABAA receptors, but not all ionotropic GABA receptors are susceptible to bicuculline. In addition, not all GABAA receptor antagonists are convulsants. Thus there are still surprises in store as the study of GABA receptors evolves.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP3232368	Salicylidene salicylhydrazide		3232-36-8	Price
AP485494-A	(+)-Bicuculline		485-49-4	Price

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