Muscarinic acetylcholine receptor binding affinities of pethidine analogs

被引：2
|
作者：
Lee, Na-Ra [1 ]
Zhang, Xuan [2 ]
Darna, Mahesh [1 ]
Dwoskin, Linda P. [1 ]
Zheng, Guangrong [2 ]
机构：
[1] Univ Kentucky, Dept Pharmaceut Sci, Coll Pharm, Lexington, KY 40536 USA
[2] Univ Arkansas Med Sci, Dept Pharmaceut Sci, Coll Pharm, Little Rock, AR 72205 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 22期
基金：
美国国家卫生研究院;
关键词：
Pethidine; Muscarinic acetylcholine receptors; H-3]NMS binding affinity; Drug abuse; VENTRAL TEGMENTAL AREA; NUCLEUS-ACCUMBENS; ANTAGONISTS; EXPRESSION;
D O I：
10.1016/j.bmcl.2015.10.029
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of pethidine analogs were synthesized and their affinities for the [H-3]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M-1, M-3 or M-5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M-1, M-3 and M-5 mAChRs (K-i = 0.67, 0.37, and 0.38 mu M, respectively). (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5032 / 5035
页数：4
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