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新型选择性 sigma1 配体的设计、合成与 SAR 分析(第 2 部分)。

Design, synthesis and SAR analysis of novel selective sigma1 ligands (Part 2).

机构信息

Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.

出版信息

Bioorg Med Chem. 2010 Feb;18(3):1204-12. doi: 10.1016/j.bmc.2009.12.039. Epub 2009 Dec 21.

Abstract

In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards sigma(1)- and sigma(2)-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.

摘要

为了研究涉及 sigma 受体(sigma-Rs)结合的分子特征,合成了基于芳基烷基氨基醇、芳烯基和芳基烷基胺骨架的新化合物,并评估了它们对 sigma(1)-和 sigma(2)-Rs 亚型的亲和力。最有前途的化合物也被筛选其对微阿片受体、德尔塔阿片受体和kappa 阿片受体的亲和力。本文呈现并讨论了生物学结果。

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