Author/Authors :
Joseph Pontillo، نويسنده , , Joseph A. Tran، نويسنده , , Beth A. Fleck، نويسنده , , Dragan Marinkovic، نويسنده , , Melissa Arellano، نويسنده , , Fabio C. Tucci، نويسنده , , Marion Lanier، نويسنده , , Jodie Nelson، نويسنده , , Jessica Parker، نويسنده , , John Saunders، نويسنده , , Brian Murphy، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Abstract :
SAR studies of a series of piperazinebenzylamines resulted in the discovery of potent antagonists of the human melanocortin-4 receptor. Compounds 11c, 11d, and 11l, which had Ki values of 21, 14, and 15 nM, respectively, possessed low efficacy in cAMP stimulation ( 15% of α-MSH maximal level) mediated by MC4R, and functioned as antagonists in inhibition of α-MSH-stimulated cAMP release in a dose-dependent manner (11l, IC50 = 36 nM).
Keywords :
melanocortin , MC4 , Antagonist , Piperazinebenzylamine.* Corresponding author. Tel.: +1 858 617 7600 , fax: +1 858 6177619 , e-mail: cchen@neurocrine.com
