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

TY - JOUR

T1 - 3B but which 3B? And that's just one of the questions

T2 - the heterogeneity of human 5-HT3 receptors

AU - Jensen, Anders A.

AU - Davies, Paul A.

AU - Bräuner-Osborne, Hans

AU - Krzywkowski, Karen

PY - 2008

Y1 - 2008

N2 - 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 Cysloop 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.

AB - 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 Cysloop 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.

KW - Humans

KW - Receptors, Serotonin, 5-HT3

U2 - 10.1016/j.tips.2008.06.001

DO - 10.1016/j.tips.2008.06.001

M3 - Journal article

C2 - 18597859

SN - 0165-6147

VL - 29

SP - 437

EP - 444

JO - Trends in Pharmacological Sciences

JF - Trends in Pharmacological Sciences

IS - 9

ER -