N-环己基乙基-N-去甲羟吗啡吲哚：一种对μ阿片受体具有选择性的纳曲吲哚类似物。

N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.

作者信息

Coop A, Jacobson A E, Aceto M D, Harris L S, Traynor J R, Woods J H, Rice K C

机构信息

Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore 21201, USA.

出版信息

Bioorg Med Chem Lett. 2000 Nov 6;10(21):2449-51. doi: 10.1016/s0960-894x(00)00479-0.

DOI:10.1016/s0960-894x(00)00479-0

PMID:11078198

Abstract

The position of the indole in the indolomorphinans, which includes the delta opioid antagonist naltrindole, is considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be mu preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands.

摘要

吲哚在吲哚吗啡喃类化合物（其中包括δ阿片受体拮抗剂纳曲吲哚）中的位置，被认为是这类配体对δ阿片受体具有选择性的原因。本文描述了N-环己基乙基取代的N-去甲衍生物，该衍生物显示出对μ阿片受体具有偏好性。因此，N-取代基的性质对于这类配体的受体选择性同样重要。