Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a K(i) of 13 nM in binding affinity and EC(50) of 6.9 nM in agonist potency with an intrinsic activity of 100% of the endogenous ligand alpha-MSH.
Tran
Joe A
JA
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Chen
Caroline W
CW
Jiang
Wanlong
W
Tucci
Fabio C
FC
Fleck
Beth A
BA
Marinkovic
Dragan
D
Arellano
Melissa
M
Chen
Chen
C
D002460:Cell Line; D006801:Humans; D011759:Pyrrolidines / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*
D011759:Pyrrolidines; D044105:Receptor, Melanocortin, Type 4