芬太尼及其衍生物对σ1-受体的亲和力。

IF 3.597 Q2 Pharmacology, Toxicology and Pharmaceutics

MedChemComm Pub Date : 2019-06-13 eCollection Date: 2019-07-01 DOI:10.1039/c9md00222g

Piotr F J Lipiński, Edina Szűcs, Małgorzata Jarończyk, Piotr Kosson, Sándor Benyhe, Aleksandra Misicka, Ján Cz Dobrowolski, Joanna Sadlej

引用次数: 8

摘要

研究了芬太尼及其11种市售衍生物对σ1受体的亲和力。母体化合物是相当差的粘合剂（IC50＝4973nM），但其紧密衍生物（苄基芬太尼或对氟芬太尼）具有亚摩尔亲和力。建模为观察到的活动趋势提供了结构基础。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Affinity of fentanyl and its derivatives for the σ<sub>1</sub>-receptor.

查看原文本刊更多论文

Affinity of fentanyl and its derivatives for the σ₁-receptor.

Fentanyl and its 11 commercially available derivatives were investigated as to their affinity for the σ₁ receptor. The parent compound is a rather poor binder (IC₅₀ = 4973 nM), but its close derivatives (benzylfentanyl or p-fluorofentanyl) have submicromolar affinities. Modelling provides a structural basis for the observed trends in activity.

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来源期刊

MedChemComm BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL

CiteScore

4.70

自引率

0.00%

发文量

审稿时长

2.2 months

期刊介绍： Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry. In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.