Pharmacological targeting of the serotonergic system for the treatment of obesity

AS Garfield, LK Heisler - The Journal of Physiology, 2009 - Wiley Online Library
AS Garfield, LK Heisler
The Journal of Physiology, 2009Wiley Online Library
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 serotonin2C receptor (5‐HT2CR), serotonin1B …
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 serotonin2C receptor (5‐HT2CR), serotonin1B (rodent)/serotonin1Dβ (human) receptor (5‐HT1B/1DβR) and serotonin6 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.
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