title: Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors.forename: Joe A
authors.initials: JA
authors.lastname: Tran
authors.forename: Caroline W
authors.initials: CW
authors.lastname: Chen
authors.forename: Wanlong
authors.initials: W
authors.lastname: Jiang
authors.forename: Fabio C
authors.initials: FC
authors.lastname: Tucci
authors.forename: Beth A
authors.initials: BA
authors.lastname: Fleck
authors.forename: Dragan
authors.initials: D
authors.lastname: Marinkovic
authors.forename: Melissa
authors.initials: M
authors.lastname: Arellano
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D002460:Cell Line; D006801:Humans; D011759:Pyrrolidines / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*
chemical_list: D011759:Pyrrolidines; D044105:Receptor, Melanocortin, Type 4