Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity
2005
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 [ 3 H] 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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