title: (R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.
abstract: (R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives (e.g., 3 and 4) were synthesized as novel melatoninergic ligands with significantly lower vasoconstrictive activity in vitro in the rat tail artery. Binding affinity assays were performed on cloned human MT1 and MT2 receptors stably expressed in NIH3T3 cells.
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: Katherine
authors.initials: K
authors.lastname: Takaki
authors.forename: Jie
authors.initials: J
authors.lastname: Chen
authors.forename: Stephen
authors.initials: S
authors.lastname: Bertenshaw
authors.forename: Lawrence
authors.initials: L
authors.lastname: Iben
authors.forename: Cathy D
authors.initials: CD
authors.lastname: Mahle
authors.forename: Elaine
authors.initials: E
authors.lastname: Ryan
authors.forename: Dedong
authors.initials: D
authors.lastname: Wu
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
authors.forename: Cen
authors.initials: C
authors.lastname: Xu
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003001:Cloning, Molecular; D006801:Humans; D008024:Ligands; D008550:Melatonin / Q000819:agonists* / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D044122:Receptor, Melatonin, MT1 / Q000187:drug effects / Q000378:metabolism; D044123:Receptor, Melatonin, MT2 / Q000187:drug effects / Q000378:metabolism; D011994:Recombinant Proteins / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D014661:Vasoconstriction / Q000187:drug effects; D014662:Vasoconstrictor Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D001572:Benzofurans; D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D011994:Recombinant Proteins; D014662:Vasoconstrictor Agents; D008550:Melatonin