短效神经肌肉阻滞剂的研究方法：非对称双四氢异喹啉单酯和二酯

Approaches to short-acting neuromuscular blocking agents: nonsymmetrical bis-tetrahydroisoquinolinium mono- and diesters.

作者信息

Dhar N C, Maehr R B, Masterson L A, Midgley J M, Stenlake J B, Wastila W B

机构信息

Department of Pharmaceutical Sciences, University of Strathclyde, Glasgow, Scotland.

出版信息

J Med Chem. 1996 Jan 19;39(2):556-61. doi: 10.1021/jm950477z.

DOI:10.1021/jm950477z

PMID:8558527

Abstract

Nonsymmetrical bisquaternary mono- and diesters combining the potency-enhancing properties of the (1R)-laudanosinium group with a second unhindered quaternary ammonium moiety have been studied as a means of promoting short action with high-potency neuromuscular block. Atracurium-related nonsymmetrical diesters showed high potency, freedom from vagal blockade at neuromuscular blocking doses, and short action. Nonsymmetrical monoesters were short acting but showed varying degrees of vagal block.

摘要

已对不对称双季铵单酯和双酯进行了研究，这些化合物将(1R)-劳丹辛鎓基团的增强效力特性与第二个无阻碍的季铵部分相结合，作为促进高效能神经肌肉阻滞的短效作用的一种手段。与阿曲库铵相关的不对称双酯显示出高效力、在神经肌肉阻滞剂量下无迷走神经阻滞作用以及短效作用。不对称单酯作用时间短，但显示出不同程度的迷走神经阻滞作用。