5-HT3 receptors.

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Thompson AJ, Lummis SC

5-HT3 receptors.

Curr Pharm Des. 2006;12(28):3615-30. doi: 10.2174/138161206778522029.

PubMed ID

17073663 [ View in PubMed

]

Abstract

The 5-HT(3) receptor is a member of the Cys-loop family of ligand-gated ion channels. These receptors are located in both the peripheral and central nervous systems, where functional receptors are constructed from five subunits. These subunits may be the same (homopentameric 5-HT(3A) receptors) or different (heteropentameric receptors, usually comprising of 5-HT(3A) and 5-HT(3B) receptor subunits), with the latter having a number of distinct properties. The 5-HT(3) receptor binding site is comprised of six loops from two adjacent subunits, and critical ligand binding amino acids in these loops have been largely identified. There are a range of selective agonists and antagonists for these receptors and the pharmacophore is reasonably well understood. There are also a wide range of compounds that can modulate receptor activity. Studies have suggested many diverse potential disease targets that might be amenable to alleviation by 5-HT(3) receptor selective compounds but to date only two applications have been fully realised in the clinic: the treatment of emesis and irritable-bowel syndrome.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Ziprasidone	5-hydroxytryptamine 3 receptor (Protein Group)	Protein group	Humans	Unknown	Antagonist	Details