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3B but which 3B?: And that's just one of the questions:: the heterogeneity of human 5-HT3 receptors

Journal

TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 29, Issue 9, Pages 437-444

Publisher

ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2008.06.001

Keywords

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Funding

  1. Lundbeck Foundation
  2. Danish Medical Research Council
  3. Center for Pharmacogenomics, Denmark
  4. Department of Anesthesia and Critical Care

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The 5-hydroxytryptamine 3 (5-HT3) receptor is expressed widely in the central and peripheral nervous systems, where it mediates or modulates a wide range of physiological processes. The receptor is targeted by drugs administered for nausea and/or emesis and irritable bowel syndrome and has been proposed as a potential drug target in various psychiatric disorders. The 5-HT3 receptor is a pentameric ligand-gated ion channel and belongs to the Cys-loop receptor family. In contrast to the immense heterogeneity characterizing other Cys-loop receptors, native 5-HT3 receptors historically have been considered a much more homogenous receptor population. However, the recent discovery of additional 5-HT3 subunits and the dawning realization that central and peripheral 5-HT3 receptor populations might comprise several subtypes characterized by distinct functional properties has emphasized the complexity of human 5-HT3 receptor signaling. In this review potential implications of these findings and of the entirely new layer of interindividual diversity introduced to the 5-HT3 receptor system by genetic variations will be outlined.

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