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5-HT3 Receptors

  • Chapter
Serotonin

Abstract

By definition, responses mediated by 5-HT3 receptors are resistant to blockade by ketanserin, methysergide and methiothepin, blocked selectively by (-)cocaine, MDL 72222 or ICS 205-930 and mimicked by 2-methy1-5-HT. Other highly selective antagonists are now available including BRL 43964, GR 38032, MDL 73147 and zacopride; phenylbiguanide is now recognized to be a more selective 5-HT3 receptor agonist than 2-methyl-5-HT. Whilst 5-HT3 receptors clearly comprize a heterogeneous group, the precise definition of subtypes is not yet possible. 5-HT3 receptors are located on autonomic, afferent and enteric neurones of the periphery and in the central nervous system where they invariably induce ‘nicotine-like’ fast depolarization responses reflecting an increased conductance of both Na+ and K+. The advent of 5-HT3 receptor radioligands has confirmed the localisation of these sites in the peripheral and central nervous systems. The potential physiological and pathophysiological significance of 5-HT3 receptors is now emerging based on imaginative laboratory experiments. Gastrokinesis, amelioration of migraine and suppression of vomiting induced by cancer chemo-or radio-therapy have already been demonstrated in man with 5-HT3 receptor antagonists; the treatment of anxiety, psychoses, dementia and the symptoms of withdrawal from drugs of habituation remain potential therapeutic hopes for the future.

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Authors and Affiliations

  1. Preclinical Research, Sandoz Ltd., CH 4002, Basel, Switzerland

    J. R. Fozard

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  1. J. R. Fozard
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Editors and Affiliations

  1. Fondazione Lorenzini, Milan, Italy

    Rodolfo Paoletti

  2. Mayo Clinic, Rochester, Minnesota, USA

    Paul M. Vanhoutte

  3. Institute of Pharmacological Sciences, University of Milan, Italy

    Nicoletta Brunello  & Franco M. Maggi  & 

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© 1990 Kluwer Academic Publishers

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Fozard, J.R. (1990). 5-HT3 Receptors. In: Paoletti, R., Vanhoutte, P.M., Brunello, N., Maggi, F.M. (eds) Serotonin. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-1912-9_43

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  • DOI: https://doi.org/10.1007/978-94-009-1912-9_43

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-7353-0

  • Online ISBN: 978-94-009-1912-9

  • eBook Packages: Springer Book Archive

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