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A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists
Authors:Goodacre Caroline J  Bromidge Steven M  Clapham David  King Frank D  Lovell Peter J  Allen Mike  Campbell Lorraine P  Holland Vicky  Riley Graham J  Starr Kathryn R  Trail Brenda K  Wood Martyn D
Affiliation:Psychiatry Centre of Excellence in Drug Discovery, GlaxoSmithkline Pharmaceuticals, Third Avenue, Harlow, Essex CM19 5AW, UK. Caroline_Goodacre@GSK.com
Abstract:Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
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