5-HT receptors

Authored by: C.R. Lummis Sarah

Handbook of Ion Channels

Print publication date:  February  2015
Online publication date:  February  2015

Print ISBN: 9781466551404
eBook ISBN: 9781466551428
Adobe ISBN:


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The 5-HT3 receptor is a Cys-loop ligand-gated ion channel and is structurally and functionally distinct from the other six classes of 5-HT receptors whose actions are mediated via G-proteins. 5-HT3 receptors are pentamers, and five classes of subunit have been identified. These are widely distributed, both in the nervous system and in other tissues. 5-HT3 receptor activation opens a cation-selective ion channel, and receptor function can be modulated by a wide range of compounds including anesthetics, opioids, and alcohols. 5-HT3 receptors play a major role in the vomiting reflex; regulate gut motility, secretion, and peristalsis in the enteric nervous system; and are involved in information transfer in the gastrointestinal (GI) tract. Disturbances within the 5-HT3 receptor system may contribute to the etiopathogenesis of a range of neurological, GI, and immunological disorders.

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