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Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity |
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| Authors: | 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 |
| Institution: | Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121-3223, USA. bsmith@arenapharm.com |
| Abstract: | We report on the synthesis, biological evaluation and structure-activity relationships for a series of 3-benzazepine derivatives as 5-HT(2C) receptor agonists. The compounds were evaluated in functional assays measuring 3H] phosphoinositol turnover in HEK-293 cells transiently transfected with h5-HT(2C), h5-HT(2A) or h5-HT(2B) 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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