A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT 2C receptor antagonists

…, SM Bromidge, D Clapham, FD King, PJ Lovell…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4989 - 4993

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Citation Number: 25

Abstract

Bisaryl cyclic ureas have been identified as high affinity 5-HT 2C receptor antagonists with selectivity over 5-HT 2A and 5-HT 2B . Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT 2C function in rodents. ... A series of novel bisaryl imidazolidinones have been prepared and evaluated both in vitro and in vivo for their 5-HT 2C receptor antagonist activity. ... The 5-HT 2 superfamily consists of three subtypes, namely, ...