2. Academic Validation
  3. 1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents

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

Affiliation

  • 1 SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK. steve_bromidge-1@sbphrd.com
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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