Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-6- …

…, IT Forbes, LM Gaster, P Ham, GE Jones…

Index: Bromidge, Steven M.; Dabbs, Steven; Davies, David T.; Davies, Susannah; Duckworth, D. Malcolm; Forbes, Ian T.; Gaster, Laramie M.; Ham, Peter; Jones, Graham E.; King, Frank D.; Mulholland, Keith R.; Saunders, Damian V.; Wyman, Paul A.; Blaney, Frank E.; Clarke, Stephen E.; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Lightowler, Sean; Middlemiss, Derek N.; Trail, Brenda; Riley, Graham J.; Wood, Martyn D. Journal of Medicinal Chemistry, 2000 , vol. 43, # 6 p. 1123 - 1134

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Citation Number: 79

Abstract

The evolution, synthesis, and biological activity of a novel series of 5-HT2C receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT2C affinity and selectivity over 5-HT2A receptors. In addition,(pyridyloxypyridyl) carbamoylindolines have been discovered with additional selectivity over the closely related 5-HT2B receptor. Compounds from this series are inverse agonists at the human cloned 5 ...