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1-[2-[(杂芳氧基)杂芳基]氨基甲酰基]吲哚啉:新型选择性5-HT2C受体反向激动剂,具有作为抗抑郁/抗焦虑药物的潜力。

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

作者信息

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

机构信息

SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK.

出版信息

Bioorg Med Chem Lett. 2000 Aug 21;10(16):1863-6. 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.

摘要

双芳基醚已被确定对5-HT2C具有优异的亲和力,且对5-HT2A和5-HT2B受体具有选择性。诸如化合物11、27和38在5-HT2C功能的中枢介导药效学模型中具有强效口服活性,其作为新型非镇静抗焦虑药和抗抑郁药的潜力正在研究中。

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