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4-苯基-4-[1H-咪唑-2-基]-哌啶衍生物作为具有潜在抗焦虑/抗抑郁特性的非肽类选择性δ-阿片受体激动剂。第2部分。

4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives as non-peptidic selective delta-opioid agonists with potential anxiolytic/antidepressant properties. Part 2.

作者信息

Trabanco Andrés A, Aerts Nancy, Alvarez Rosa M, Andrés José I, Boeckx Inge, Fernández Javier, Gómez Antonio, Janssens Frans E, Leenaerts Joseph E, De Lucas Ana I, Matesanz Encarna, Steckler Thomas, Pullan Shirley

机构信息

Johnson & Johnson Pharmaceutical Research & Development, Research & Early Development Europe, CNS-Psychiatry, Spain.

出版信息

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3860-3. doi: 10.1016/j.bmcl.2007.05.012. Epub 2007 May 10.

Abstract

Novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives have been prepared and their synthesis described herein. In vitro affinities for delta-, micro-, and kappa-opioid receptors are reported. Evaluation of some representative compounds from this series in the mouse neonatal ultrasonic vocalization test and the mouse tail suspension test revealed anxiolytic- and antidepressant-like effects, respectively, upon subcutaneous administration.

摘要

新型4-苯基-4-[1H-咪唑-2-基]-哌啶衍生物已被制备出来,本文描述了其合成方法。报道了它们对δ-、μ-和κ-阿片受体的体外亲和力。对该系列中一些代表性化合物在小鼠新生仔超声发声试验和小鼠悬尾试验中的评估显示,皮下给药后分别具有抗焦虑样和抗抑郁样作用。

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