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Melanin-concentrating hormone receptor-1 antagonists as antiobesity therapeutics: current status
Timothy J Kowalski1, Thavalakulamgar Sasikumar
1Department of CV/Metabolic Diseases, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA. timothy.kowalsk@spcorp.com
Abstract:
There is compelling genetic and pharmacologic evidence to indicate that melanin-concentrating hormone receptor-1 (MCHR1) signaling is involved in the regulation of food intake and energy expenditure. The medical need for novel therapies to treat obesity and related metabolic disorders has led to a great deal of interest by pharmaceutical companies in the discovery of MCHR1 antagonists. Recent publications describing preclinical studies have demonstrated that small-molecule MCHR1 antagonists decrease food intake, bodyweight, and adiposity in rodent models of obesity. Results from ongoing early-stage clinical trials with MCHR1 antagonists are eagerly awaited, as is the movement of other MCHR1 antagonists into the clinic.
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