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

  • Bioorg Med Chem Lett. 2000 Aug 21;10(16):1863-6. doi: 10.1016/s0960-894x(00)00364-4.
S M Bromidge  1 ,  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
Affiliations
  • 1. SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. [email protected]
PMID: 10969986 DOI: 10.1016/s0960-894x(00)00364-4
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.

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