title: Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists.
abstract: A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar K(i) values in a competition binding assay.
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: Melissa
authors.initials: M
authors.lastname: Arellano
authors.forename: Beth A
authors.initials: BA
authors.lastname: Fleck
authors.forename: Joseph
authors.initials: J
authors.lastname: Pontillo
authors.forename: Dragan
authors.initials: D
authors.lastname: Marinkovic
authors.forename: Fabio C
authors.initials: FC
authors.lastname: Tucci
authors.forename: Jenny
authors.initials: J
authors.lastname: Wen
authors.forename: John
authors.initials: J
authors.lastname: Saunders
authors.forename: Chen
authors.initials: C
authors.lastname: Chen
mesh_terms: D000818:Animals; D001596:Benzylamines / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007700:Kinetics; D010627:Phenethylamines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D001596:Benzylamines; D010627:Phenethylamines; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4