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

被引:48
作者
Jensen, Anders A. [1 ]
Davies, Paul A. [2 ]
Brauner-Osborne, Hans [1 ]
Krzywkowski, Karen [1 ]
机构
[1] Univ Copenhagen, Dept Med Chem, Fac Pharmaceut Sci, DK-2100 Copenhagen, Denmark
[2] Harvard Univ, Sch Med, Massachusetts Gen Hosp, Dept Anesthesia & Crit Care, Boston, MA 02114 USA
基金
英国医学研究理事会;
关键词
D O I
10.1016/j.tips.2008.06.001
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:437 / 444
页数:8
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