| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2530149 | Current Opinion in Pharmacology | 2011 | 7 Pages |
Serotonin is known to have anorectic properties through centrally acting mechanisms. Three serotonin receptors have been implicated in mediating these effects: 5-HT1B, 5-HT2C and 5-HT6. Hypophagic effects are elicited through agonism of the former two receptors, whereas antagonism of the 5-HT6 receptor appears to have an anorectic effect. All three targets have been validated through extensive studies including knockout mice and selective ligand assessment. 5-HT1B receptor agonists have limited utility due to mechanism-based side effects, whereas 5-HT2C receptor agonists suffer from challenges associated with selectivity over the closely related 5-HT2A and 5-HT2B receptors. 5-HT6 receptor antagonists appear to offer great promise, although the mechanisms through which they reduce food intake and body weight are not fully understood.
Research highlights► Approaches towards managing weight gain through serotonin receptors are discussed. ► 5-HT1B, 5-HT2C and 5-HT6 receptors have been implicated in controlling food intake. ► 5-HT1B and 5-HT2C receptor agonists face challenges around benefit to risk ratio. ► 5-HT6 receptor antagonists offer great promise in controlling weight gain.
