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

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

Journal of medicinal chemistry 2003 Jan 2

filter terms:

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.

Citation

Premilla N Arasasingham, Christopher Fotsch, Xiaohu Ouyang, Mark H Norman, Michael G Kelly, Kevin L Stark, Bill Karbon, Clarence Hale, James W Baumgartner, Martha Zambrano, Janet Cheetham, Nuria A Tamayo. Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding. Journal of medicinal chemistry. 2003 Jan 2;46(1):9-11