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5‐Hydroxytryptamine Medications for the Treatment of Obesity
Author(s) -
Burke L. K.,
Heisler L. K.
Publication year - 2015
Publication title -
journal of neuroendocrinology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.062
H-Index - 116
eISSN - 1365-2826
pISSN - 0953-8194
DOI - 10.1111/jne.12287
Subject(s) - energy homeostasis , melanocortin , agonist , receptor , neuroscience , obesity , serotonin , 5 ht2 receptor , homeostasis , endocrinology , serotonergic , diabetes mellitus , 5 ht receptor , medicine , biology , pharmacology , bioinformatics
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‐ HTR s in energy balance and reveal the 5‐ HT 2 C R as the principal 5‐ HTR mediating this homeostatic process. Capitalising on this neurophysiological machinery, 5‐ HT 2 C R 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‐ HT 2 C R modulation of the brain melanocortin circuit via activation of pro‐opiomelanocortin neurones signalling at melanocortin4 receptors. Thus, 5‐ HT 2 C R agonists offer a means to improve obesity and type 2 diabetes, which are conditions that now represent global challenges to human health.