title: Heterocyclic aminopyrrolidine derivatives as melatoninergic agents.
abstract: A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned human MT(1) and MT(2) receptors, stably expressed in NIH3T3 cells. Compound 16 was identified as an orally bioavailable agonist at MT(1) and MT(2) melatonin receptors with low vasoconstrictive activity.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. sunl@bms.com
authors.forename: Li-Qiang
authors.initials: LQ
authors.lastname: Sun
authors.forename: Jie
authors.initials: J
authors.lastname: Chen
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Mattson
authors.forename: James R
authors.initials: JR
authors.lastname: Epperson
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Deskus
authors.forename: Wen Sen
authors.initials: WS
authors.lastname: Li
authors.forename: Katherine
authors.initials: K
authors.lastname: Takaki
authors.forename: Donald B
authors.initials: DB
authors.lastname: Hodges
authors.forename: Lawrence
authors.initials: L
authors.lastname: Iben
authors.forename: Cathy D
authors.initials: CD
authors.lastname: Mahle
authors.forename: Astrid
authors.initials: A
authors.lastname: Ortiz
authors.forename: David
authors.initials: D
authors.lastname: Molstad
authors.forename: Elaine
authors.initials: E
authors.lastname: Ryan
authors.forename: Krishnaswamy
authors.initials: K
authors.lastname: Yeleswaram
authors.forename: Cen
authors.initials: C
authors.lastname: Xu
authors.forename: Guanglin
authors.initials: G
authors.lastname: Luo
mesh_terms: D016475:3T3 Cells; D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D003001:Cloning, Molecular; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008550:Melatonin / Q000819:agonists* / Q000494:pharmacology; D051379:Mice; D044122:Receptor, Melatonin, MT1 / Q000187:drug effects / Q000378:metabolism; D044123:Receptor, Melatonin, MT2 / Q000187:drug effects / Q000378:metabolism; D011994:Recombinant Proteins / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; D006571:Heterocyclic Compounds; D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D011994:Recombinant Proteins; D005576:Colforsin; D000242:Cyclic AMP; D008550:Melatonin