Author/Authors :
Joe A. Tran، نويسنده , , Caroline W. Chen، نويسنده , , Wanlong Jiang، نويسنده , , Fabio C. Tucci، نويسنده , , Beth A. Fleck، نويسنده , , Dragan Marinkovic، نويسنده , , Melissa Arellano، نويسنده , , Chen Chen، نويسنده ,
Abstract :
A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a Ki of 13 nM in binding affinity and EC50 of 6.9 nM in agonist potency with an intrinsic activity of 100% of the endogenous ligand α-MSH.
Keywords :
agonist , synthesis , melanocortin-4 receptor , pyrrolidine
