Bioorganic & Medicinal Chemistry Letters 2000-08-21

1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.

S M Bromidge, S Dabbs, S Davies, D M Duckworth, I T Forbes, G E Jones, J Jones, F D King, D V Saunders, T P Blackburn, V Holland, G A Kennett, S Lightowler, D N Middlemiss, G J Riley, B Trail, M D Wood

Index: Bioorg. Med. Chem. Lett. 10(16) , 1863-6, (2000)

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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.