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J Med Chem. 2003 Jan 2;46(1):9-11.

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.

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1
Department of Small Molecule Drug Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799, USA.

Abstract

Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action.(1) In the hypothalamus, melanocortin peptide agonists act as satiety-inducing factors that mediate their action through the melanocortin-4 receptor (MC4R) whereas AGRP is an opposing orexigenic agent. Novel inhibitors of the AGRP/MC4 binding based on (piperazinylethyl)piperazines were prepared, and their structure-activity relationship was established.

PMID:
12502354
DOI:
10.1021/jm0255522
[Indexed for MEDLINE]
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