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用于烟碱型乙酰胆碱受体的基于聚乙二醇的同系配体。

Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.

作者信息

Scates Bradley A, Lashbrook Bethany L, Chastain Benjamin C, Tominaga Kaoru, Elliott Brandon T, Theising Nicholas J, Baker Thomas A, Fitch Richard W

机构信息

Department of Chemistry, Indiana State University, 600 Chestnut Street, Science S35E, Terre Haute, IN 47809, USA.

出版信息

Bioorg Med Chem. 2008 Dec 15;16(24):10295-300. doi: 10.1016/j.bmc.2008.10.045. Epub 2008 Nov 1.

DOI:10.1016/j.bmc.2008.10.045
PMID:19006672
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2903455/
Abstract

A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity probes and multivalent ligands for nAChR.

摘要

将一系列聚乙二醇（PEG）单甲醚与三种用于烟碱型乙酰胆碱受体的配体系列进行共轭。制备了乙酰氨基胆碱、环状类似物1-乙酰基-4,4-二甲基哌嗪鎓和吡啶基醚A-84543的共轭物。发现每个系列在大鼠大脑皮层的烟碱型受体上都保留了显著的亲和力，其连接链长达六个PEG单元。这类化合物是亲水性配体，可作为荧光/亲和探针的模型以及nAChR的多价配体。

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