(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.
(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.
Sun
Li-Qiang
LQ
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. sunl@bms.com
Takaki
Katherine
K
Chen
Jie
J
Bertenshaw
Stephen
S
Iben
Lawrence
L
Mahle
Cathy D
CD
Ryan
Elaine
E
Wu
Dedong
D
Gao
Qi
Q
Xu
Cen
C
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*
D001572:Benzofurans; D008024:Ligands; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D011994:Recombinant Proteins; D014662:Vasoconstrictor Agents; D008550:Melatonin