Allosteric modulation of the 5-HT(3) receptor

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


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.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Allosteric Site
  • Animals
  • Humans
  • Ondansetron / pharmacology
  • Protein Binding
  • Receptors, Serotonin, 5-HT3 / chemistry*
  • Receptors, Serotonin, 5-HT3 / metabolism*


  • Receptors, Serotonin, 5-HT3
  • Ondansetron