1-[2-[(Heteroaryloxy) heteroaryl] carbamoyl] indolines: Novel and selective 5-HT 2C receptor inverse agonists with potential as antidepressant/anxiolytic agents

…, S Dabbs, S Davies, DM Duckworth, IT Forbes…

Index: Bromidge, Steven M.; Dabbs, Steven; Davies, Susannah; Duckworth; Forbes, Ian T.; Jones, Graham E.; Jones, Jerome; King, Frank D.; Saunders, Damian V.; Blackburn, Thomas P.; Holland, Vicky; Kennett, Guy A.; Lightowler, Sean; Middlemiss, Derek N.; Riley, Graham J.; Trail, Brenda; Wood, Martyn D. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 16 p. 1863 - 1866

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Citation Number: 24

Abstract

Bisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5- HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their potential as novel non-sedating anxiolytic and antidepressants is under investigation.