• Title of article

    Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity

  • Author/Authors

    Brian M. Smith، نويسنده , , Jeffrey M. Smith، نويسنده , , James H. Tsai، نويسنده , , Jeffrey A. Schultz، نويسنده , , Charles A. Gilson، نويسنده , , Scott A. Estrada، نويسنده , , Rita R. Chen، نويسنده , , Douglas M. Park، نويسنده , , Emily B. Prieto، نويسنده , , Charlemagne S. Gallardo، نويسنده , , Dipanjan Sengupta، نويسنده , , William J. Thomsen، نويسنده , , Hazel R. Saldana، نويسنده , , Kevin T. Whelan، نويسنده , , Frédérique Menzaghi، نويسنده , , Robert R. Webb، نويسنده , , Nigel R.A. Beeley، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2005
  • Pages
    4
  • From page
    1467
  • To page
    1470
  • Abstract
    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-HT2C receptor agonists, which decrease food intake in a rat feeding model.
  • Keywords
    Benzazepine , Serotonin , 5-HT2C , obesity
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2005
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    795417

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=795417