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

被引：37
|
作者：
Arasasingham, PN
Fotsch, C
Ouyang, X
Norman, MH
Kelly, MG
Stark, KL
Karbon, B
Hale, C
Baumgartner, JW
Zambrano, M
Cheetham, J
Tamayo, NA
机构：
[1] Amgen Inc, Dept Small Molecule Drug Discovery, Thousand Oaks, CA 91320 USA
[2] Amgen Inc, Dept Metab Disorders, Thousand Oaks, CA 91320 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 01期
关键词：
D O I：
10.1021/jm0255522
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：9 / 11
页数：3
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