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Melanin Concentrating Hormone Receptor Antagonists as Antiobesity Agents: From M2 to MCHR-1

[ Vol. 7 , Issue. 15 ]

Author(s):

Mark D. McBriar   Pages 1440 - 1454 ( 15 )

Abstract:


Melanin concentrating hormone (MCH) is a cyclic, nonadecapeptide expressed in the CNS of all vertebrates that regulates feeding behavior and energy homeostasis. The MCH-1 receptor (MCH-R1) has been identified as a key target in MCH regulation, as small molecule antagonists of MCH-R1 have demonstrated activity in vivo. Herein, we chronicle our efforts to optimize a hit identified via high throughput screening of our proprietary compound library. Several challenges such as selectivity over other receptors, toxicity of a potential metabolite and determining receptor occupancy via a medium throughput assay will be reviewed.

Keywords:

Melanin-concentrating hormone, MCH, MCH R1, MCH R1 antagonist, obesity

Affiliation:

Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road,Kenilworth, NJ 07033-1300, USA.



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