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Curr Opin Pharmacol. 2011 Feb;11(1):75-80. doi: 10.1016/j.coph.2011.01.010. Epub 2011 Feb 20.

Allosteric modulation of the 5-HT(3) receptor.

Author information

1
Department of Neuroscience, Tufts University, 136 Harrison Ave, Boston, MA 02111, USA. paul.davies@tufts.edu

Abstract

5-Hydroxytryptamine type 3 (5-HT(3)) receptors are ligand-gated ion channels that play important roles in depression, anxiety, substance abuse, emesis, inflammatory pain, spinal nociception, gastrointestinal function, and cardiovascular reflexes. Probably the most studied modulators of 5-HT(3) receptors are the high affinity competitive 'setron' antagonists typified by ondansetron. However, there exists a broad range of compounds that modulate the 5-HT(3) receptor, not through the orthosteric site but by binding to allosteric sites. Most notable are therapeutic compounds ascribed to certain targets but that allosterically modulate 5-HT(3) receptors at clinically relevant concentrations.

PMID:
21342788
PMCID:
PMC3072441
DOI:
10.1016/j.coph.2011.01.010
[Indexed for MEDLINE]
Free PMC Article

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