title: N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.
abstract: N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide 3a was synthesized as an orally bioavailable agonist at MT1 and MT2 melatonin receptors with significantly 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: Katherine
authors.initials: K
authors.lastname: Takaki
authors.forename: Jie
authors.initials: J
authors.lastname: Chen
authors.forename: Lawrence
authors.initials: L
authors.lastname: Iben
authors.forename: Jay O
authors.initials: JO
authors.lastname: Knipe
authors.forename: Lori
authors.initials: L
authors.lastname: Pajor
authors.forename: Cathy D
authors.initials: CD
authors.lastname: Mahle
authors.forename: Elaine
authors.initials: E
authors.lastname: Ryan
authors.forename: Cen
authors.initials: C
authors.lastname: Xu
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000633:toxicity; D000284:Administration, Oral; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000633:toxicity; D001682:Biological Availability; D000242:Cyclic AMP / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D041681:NIH 3T3 Cells; D011869:Radioligand Assay; D051381:Rats; D044122:Receptor, Melatonin, MT1 / Q000819:agonists*; D044123:Receptor, Melatonin, MT2 / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D001572:Benzofurans; C498372:N-(2-(2-(4-phenylbutyl)benzofuran-4-yl)cyclopropylmethyl)acetamide; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D000242:Cyclic AMP