了解4-苯胺基哌啶类似物对μ和δ阿片受体生物活性的结构要求。
Understanding the structural requirements of 4-anilidopiperidine analogues for biological activities at mu and delta opioid receptors.
作者信息
Lee Yeon Sun, Nyberg Joel, Moye Sharif, Agnes Richard S, Davis Peg, Ma Shou-wu, Lai Josephine, Porreca Frank, Vardanyan Ruben, Hruby Victor J
机构信息
Department of Chemistry, University of Arizona, Tucson, AZ 85721, USA.
出版信息
Bioorg Med Chem Lett. 2007 Apr 15;17(8):2161-5. doi: 10.1016/j.bmcl.2007.01.114. Epub 2007 Feb 8.
Abstract
New 4-anilidopiperidine analogues in which the phenethyl group of fentanyl was replaced by several aromatic ring-contained amino acids (or acids) were synthesized to study the biological effect of the substituents on mu and delta opioid receptor interactions. These analogues showed broad (47 nM-76 microM) but selective (up to 17-fold) binding affinities at the mu opioid receptor over the delta opioid receptor, as predicted from the message-address concept.
摘要
合成了新型4-苯胺基哌啶类似物，其中芬太尼的苯乙基被几种含芳环的氨基酸（或酸）取代，以研究取代基对μ和δ阿片受体相互作用的生物学效应。如根据信息-靶点概念所预测的，这些类似物在μ阿片受体上显示出广泛（47 nM-76 μM）但具有选择性（高达17倍）的结合亲和力，对δ阿片受体的亲和力则较低。
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