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

Author(s): Mark D. McBriar

Journal Name: Current Topics in Medicinal Chemistry

Volume 7 , Issue 15 , 2007

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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

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Article Details

Year: 2007
Page: [1440 - 1454]
Pages: 15
DOI: 10.2174/156802607782194752
Price: $65

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