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Bioorg Med Chem Lett. 2005 May 16;15(10):2541-6.

A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.

Author information

1
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.

Abstract

Optimization on a series of piperazinebenzylamines resulted in analogues with low nanomolar binding at the human MC4 receptor but weak affinity (Ki > 500 nM) at the MC3 receptor. Compound 14c was identified to be a potent MC4R antagonist (Ki = 3.2 nM) with a selectivity of 240-fold over MC3R. It proved to be an insurmountable antagonist in a cAMP assay. Compound 14c potently stimulated food intake in satiated mice when given by intracerebroventricular administration.

PMID:
15863313
DOI:
10.1016/j.bmcl.2005.03.053
[Indexed for MEDLINE]

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