5-Hydroxytryptamine Medications for the Treatment of Obesity

Luke K. Burke; Lora Heisler

doi:10.1111/jne.12287

5-Hydroxytryptamine Medications for the Treatment of Obesity

Luke K. Burke, Lora Heisler

The Rowett Institute of Nutrition and Health

Research output: Contribution to journal › Literature review › peer-review

63 Citations (Scopus)

Abstract

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 15years. 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.

Original language	English
Pages (from-to)	389-398
Number of pages	10
Journal	Journal of Neuroendocrinology
Volume	27
Issue number	6
Early online date	26 May 2015
DOIs	https://doi.org/10.1111/jne.12287
Publication status	Published - Jun 2015

Bibliographical note

Date of Acceptance: 23/04/15

Acknowledgements
The present study was supported by the Wellcome Trust (093566 to LKB and LKH; 098012 to LKH). We wish to acknowledge Patricia Bain for her support in graphics design.

Note
A Study to Evaluate the Effect of Long-term Treatment With BELVIQ (Lorcaserin HCl) on the Incidence of Major Adverse Cardiovascular Events and Conversion to Type 2 Diabetes Mellitus in Obese and Overweight Subjects With Cardiovascular Disease or Multiple Cardiovascular Risk Factors (CAMELLIA-TIMI)

Keywords

serotonin
5-HT2CR
obesity
type 2 diabetes
lorcaserin
neurons regulate energy
receptor knockout mice
central-nervous-system
behavioral satiety sequence
type-2 diabetes-mellitus
blood-glucose control
food-intake
5-HT1B receptor
D-fenfluramine
weight-loss

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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Cite this

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abstract = "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 15years. 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.",

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author = "Burke, {Luke K.} and Lora Heisler",

note = "Date of Acceptance: 23/04/15 Acknowledgements The present study was supported by the Wellcome Trust (093566 to LKB and LKH; 098012 to LKH). We wish to acknowledge Patricia Bain for her support in graphics design. Note A Study to Evaluate the Effect of Long-term Treatment With BELVIQ (Lorcaserin HCl) on the Incidence of Major Adverse Cardiovascular Events and Conversion to Type 2 Diabetes Mellitus in Obese and Overweight Subjects With Cardiovascular Disease or Multiple Cardiovascular Risk Factors (CAMELLIA-TIMI)",

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AB - 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 15years. 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.

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KW - behavioral satiety sequence

KW - type-2 diabetes-mellitus

KW - blood-glucose control

KW - food-intake

KW - 5-HT1B receptor

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DO - 10.1111/jne.12287

M3 - Literature review

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JF - Journal of Neuroendocrinology

IS - 6

ER -

5-Hydroxytryptamine Medications for the Treatment of Obesity

Abstract

Bibliographical note

Keywords

UN SDGs

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