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Therapeutic Applications of 5-HT4 Receptor Agonists and Antagonists

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5-HT4 Receptors in the Brain and Periphery

Part of the book series: Biotechnology Intelligence Unit ((BIOIU))

Abstract

Metoclopramide is used to stimulate ‘upper gut’ motility and prevent nausea and vomiting. These clinical benefits are attributed, respectively, to 5-HT4 receptor activation23 and to antagonism at dopamine D2 and/or 5-HT3 receptors.52 However, since antagonism at dopamine D2 receptors within the striatum may also cause extrapyramidal reactions and akathisia, alternative 5-HT4 receptor agonists have been developed, with lower affinity for the D2 receptor. The most notable is cisapride. Metoclopramide and cisapride are marketed for gastrointestinal hypomotility disorders such as gastro-esophageal reflux (heartburn; mild esophagitis), functional or nonulcer dyspepsia and gastroparesis (e.g., caused by diabetic neuropathy).7 For both drugs, the most common side-effect attributed to 5-HT4 receptor activation is the promotion of loose stools and in more severe cases, diarrhea and abdominal pain.

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Authors
  1. Gareth J. Sanger
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  1. Roche Bioscience, Palo Alto, California, USA

    Richard M. Eglen Ph.D.

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Sanger, G.J. (1998). Therapeutic Applications of 5-HT4 Receptor Agonists and Antagonists. In: Eglen, R.M. (eds) 5-HT4 Receptors in the Brain and Periphery. Biotechnology Intelligence Unit. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-05553-3_10

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  • DOI: https://doi.org/10.1007/978-3-662-05553-3_10

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-662-05555-7

  • Online ISBN: 978-3-662-05553-3

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