Chronobiotic activity of N-[2-(2, 7-dimethoxyfluoren-9-yl) ethyl]-propanamide. Synthesis and melatonergic pharmacology of fluoren-9-ylethyl amides
JR Epperson, MA Bruce, JD Catt, JA Deskus…
Index: Epperson, James R.; Bruce, Marc A.; Catt, John D.; Deskus, Jeffrey A.; Hodges, Donald B.; Karageorge, George N.; Keavy, Daniel J.; Mahle, Cathy D.; Mattson, Ronald J.; Ortiz, Astrid A.; Parker, Michael F.; Takaki, Katherine S.; Watson, Brett T.; Yevich, Joseph P. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 17 p. 4601 - 4611
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Citation Number: 11
Abstract
A series of fluoren-9-yl ethyl amides (2) were synthesized and evaluated for human melatonin MT1 and MT2 receptor binding. N-[2-(2, 7-dimethoxyfluoren-9-yl) ethyl] propanamide (2b) was selected and evaluated in functional assays measuring intrinsic activity at the human MT1 and MT2 receptors and demonstrated full agonism at both receptors. The chronobiotic properties of 2b were demonstrated in both acute and chronic ...
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