Generic placeholder image

Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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

Author(s): Mark D. McBriar

Volume 7, Issue 15, 2007

Page: [1440 - 1454] Pages: 15

DOI: 10.2174/156802607782194752

Price: $65

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


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy