Agonists and antagonists of 5-HT3 receptors

  • John R. Fozard
Part of the Developments in CardioCardiovascular Pharmacology of 5-Hydroxytryptamine book series (DICM, volume 106)


There can be little doubt that the basis of the recent remarkable advances in our understanding of the physiological and pathophysiological roles of 5-HT has been the identification and development of compounds with selectivity for 5-HT receptor subtypes [1–4]. Among these, none has been more spectacular nor of potentially greater therapeutic significance than the advent of ligands with potency and selectivity for the 5-HT3 receptor subtype. The purpose of this article is to describe these compounds and their use as tools to identify 5-HT3 receptors and their properties. Both selective agonists and antagonists will be considered as well as a number of their radiolabeled counterparts. The historical development of these compounds will not be dealt with since it has been the subject of recent comprehensive review [5–8].


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© Springer Science+Business Media Dordrecht 1990

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  • John R. Fozard

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