Pharmacological targeting of the serotonergic system for the treatment of obesity
Pharmacological targeting of the serotonergic system for the treatment of obesity
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DOI：
10.1113/jphysiol.2008.164152
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发表时间：
2009-01-01
影响因子：
5.5
通讯作者：
Heisler, Lora K.
中科院分区：
文献类型：
--
作者：
Garfield, Alastair S.;Heisler, Lora K.
由于5-羟色胺(5-羟色胺，5-羟色胺)功效的增加而导致的食物摄入量的减少一直是减肥药物治疗的目标。然而，耐受性和/或副作用的诱导限制了最早的5-羟色胺相关药物的临床应用。随着全球肥胖率的上升，作为药物干预点的5-羟色胺能系统的操纵重新引起了人们的兴趣。5-羟色胺(2C)受体(5-HT2CR)、5-羟色胺(1B)(啮齿动物)/5-羟色胺(1Dβ)(人)受体(5-HT1B/1DβR)和5-羟色胺(6)受体(5-HT6R)是最有前景的5-羟色胺受体治疗靶点。经典的5-羟色胺受体化合物已经让位于无数新的受体选择性配体，其中许多具有明显的厌食作用。在这里，我们综述了减少摄食行为的5-羟色胺能化合物，并讨论了它们治疗肥胖症的临床潜力。
The attenuation of food intake as induced by an increase in serotonergic (5-hydroxytryptamine, 5-HT) efficacy has been a target of antiobesity pharmacotherapies. However, the induction of tolerance and/or side-effects limited the clinical utility of the earliest serotonin-related medications. With the global prevalence of obesity rising, there has been renewed interest in the manipulation of the serotonergic system as a point of pharmacological intervention. The serotonin(2C) receptor (5-HT2CR), serotonin(1B) (rodent)/serotonin(1D beta) (human) receptor (5-HT1B/1D beta R) and serotonin(6) receptor (5-HT6R) represent the most promising serotonin receptor therapeutic targets. Canonical serotonin receptor compounds have given way to a myriad of novel receptor-selective ligands, many of which have observable anorectic effects. Here we review serotonergic compounds reducing ingestive behaviour and discuss their clinical potential for the treatment of obesity.