5-Hydroxytryptamine Medications for the Treatment of Obesity

The central 5‐hydroxytryptamine (5‐HT; serotonin) system represents a fundamental component of the brain's control of energy homeostasis. Medications targeting the 5‐HT pathway have been at the forefront of obesity treatment for the past 15 years. Pharmacological agents targeting 5‐HT receptors...

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Bibliographic Details
Published in:Journal of neuroendocrinology 2015-06, Vol.27 (6), p.389-398
Main Authors: Burke, L. K., Heisler, L. K.
Format: Article
Language:English
Subjects:
5-HT2CR
Appetite - drug effects
Biological Availability
Energy Metabolism
Humans
lorcaserin
obesity
Obesity - drug therapy
Pro-Opiomelanocortin - physiology
serotonin
Serotonin - physiology
Serotonin 5-HT2 Receptor Agonists - pharmacokinetics
Serotonin 5-HT2 Receptor Agonists - pharmacology
Serotonin 5-HT2 Receptor Agonists - therapeutic use
type 2 diabetes
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Summary:The central 5‐hydroxytryptamine (5‐HT; serotonin) system represents a fundamental component of the brain's control of energy homeostasis. Medications targeting the 5‐HT pathway have been at the forefront of obesity treatment for the past 15 years. Pharmacological agents targeting 5‐HT receptors (5‐HTR), in combination with genetic models of 5‐HTR manipulation, have uncovered a role for specific 5‐HTRs in energy balance and reveal the 5‐HT2CR as the principal 5‐HTR mediating this homeostatic process. Capitalising on this neurophysiological machinery, 5‐HT2CR agonists improve obesity and glycaemic control in patient populations. The underlying therapeutic mechanism has been probed using model systems and appears to be achieved primarily through 5‐HT2CR modulation of the brain melanocortin circuit via activation of pro‐opiomelanocortin neurones signalling at melanocortin4 receptors. Thus, 5‐HT2CR agonists offer a means to improve obesity and type 2 diabetes, which are conditions that now represent global challenges to human health.
ISSN:0953-8194
1365-2826
DOI:10.1111/jne.12287