Melanin-concentrating hormone receptor-1 antagonists as antiobesity therapeutics: current status.
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.
Kowalski
Timothy J
TJ
Department of CV/Metabolic Diseases, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA. timothy.kowalsk@spcorp.com
Sasikumar
Thavalakulamgar
T
D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000639:trends; D004435:Eating / Q000187:drug effects; D004734:Energy Metabolism / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009765:Obesity / Q000188:drug therapy* / Q000503:physiopathology; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects
D019440:Anti-Obesity Agents; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin