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苯甲酰基哌替啶和去甲哌替啶衍生物作为选择性 5-羟色胺转运体配体的合成及构效关系研究。

Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.

机构信息

Department of Chemistry, University of New Orleans, LA 70148, USA.

出版信息

Bioorg Med Chem. 2010 Dec 1;18(23):8356-64. doi: 10.1016/j.bmc.2010.09.060. Epub 2010 Sep 29.

DOI:10.1016/j.bmc.2010.09.060
PMID:20980153
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3713777/
Abstract

A series of benzyl esters of meperidine and normeperidine were synthesized and evaluated for binding affinity at serotonin, dopamine and norepinephrine transporters. The 4-methoxybenzyl ester 8b and 4-nitrobenzyl ester 8c in the meperidine series and 4-methoxybenzyl ester 14a in the normeperidine series exhibited low nanomolar binding affinities at the SERT (K(i) values <2nM) and high SERT selectivity (DAT/SERT >1500 and NET/SERT >1500).

摘要

合成了一系列哌替啶和去甲哌替啶的苄基酯，并评估了它们在 5-羟色胺、多巴胺和去甲肾上腺素转运体上的结合亲和力。哌替啶系列的 4-甲氧基苄基酯 8b 和 4-硝基苄基酯 8c 以及去甲哌替啶系列的 4-甲氧基苄基酯 14a 在 SERT 上表现出低纳摩尔的亲和力（K(i)值<2nM）和高 SERT 选择性（DAT/SERT>1500 和 NET/SERT>1500）。

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本文引用的文献

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