Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation

被引：24

作者：

Cameron, KS

Fielding, L

Mason, R

Muir, AW

Rees, DC

Thorn, S

Zhang, MQ

机构：

[1] Organon Res Labs Ltd, Dept Med Chem, Newhouse ML1 5SH, Lanark, Scotland

[2] Organon Res Labs Ltd, Dept Pharmacol, Newhouse ML1 5SH, Lanark, Scotland

[3] Organon Res Labs Ltd, Dept Analyt Chem, Newhouse ML1 5SH, Lanark, Scotland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(02)00017-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of carboxyl-containing cyclophanes have been designed and synthesised as chemical chelators (or host molecules) of cationic muscle relaxant drugs (or guest molecules). Three of these cyclophane derivatives, 1-3, have been shown by NMR to form 1:1 complexes with the muscle relaxants pancuronium. 4 and gallamine, 5 in D2O, with association constants up to 10(4) M-1. When tested in an in vitro chick biventer muscle preparation, the cyclophanes reversed the neuromuscular block induced by pancuronium and gallamine, with 3 having the most effective reversal against pancuronium (EC50 40 muM). (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：753 / 755

页数：3

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