Author/Authors :
Joe A. Tran، نويسنده , , Joseph Pontillo، نويسنده , , Melissa Arellano، نويسنده , , Nicole S. White، نويسنده , , Beth A. Fleck، نويسنده , , Dragan Marinkovic، نويسنده , , Fabio C. Tucci، نويسنده , , Marion Lanier، نويسنده , , Jodie Nelson، نويسنده , , John Saunders، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Abstract :
SAR studies of a series of piperazinebenzylamines resulted in identification of potent agonists and antagonists of the human melanocortin-4 receptor. Thus, the 1,2,3,4-tetrahydroisoquinolin-1-ylacetyl compound 12e and the quinolin-3-ylcarbonyl analogue 12l possessed Ki values of 6.3 and 4.5 nM, respectively. Interestingly, 12e was a full agonist with an EC50 value of 31 nM, and 12l was a weak partial agonist (IA = 17%) and functioned as an antagonist (IC50 = 300 nM).
Keywords :
melanocortin , MC4R , Agonists , Antagonist
