Bioorganic and Medicinal Chemistry Letters p. 1467 - 1470 (2005)
Update date:2022-07-31
Topics: Obesity Discovery SAR (Structure-Activity Relationship)
Smith, Brian M.
Smith, Jeffrey M.
Tsai, James H.
Schultz, Jeffrey A.
Gilson, Charles A.
Estrada, Scott A.
Chen, Rita R.
Park, Douglas M.
Prieto, Emily B.
Gallardo, Charlemagne S.
Sengupta, Dipanjan
Thomsen, William J.
Saldana, Hazel R.
Whelan, Kevin T.
Menzaghi, Frederique
Webb, Robert R.
Beeley, Nigel R.A.
We report on the synthesis, biological evaluation and structure-activity relationships for a series of 3-benzazepine derivatives as 5-HT2C receptor agonists. The compounds were evaluated in functional assays measuring [3H] phosphoinositol turnover in HEK-293 cells transiently transfected with h5-HT2C, h5-HT2A or h5-HT2B receptors. Several compounds are shown to be potent and selective 5-HT 2C receptor agonists, which decrease food intake in a rat feeding model.
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