Marshall R J, Muir A W, Sleigh T, Savage D S
Scientific Development Group, Organon Laboratories Ltd, Newhouse, Lanarshire, UK.
Eur J Anaesthesiol Suppl. 1995 Sep;11:5-10.
This article attempts to summarize more than 25 years of chemistry and pharmacology research aimed at the search for clinically useful muscle relaxants based on an amino-androstane skeleton. This research strategy has produced three clinically useful drugs (pancuronium, vecuronium and rocuronium), and in addition has demonstrated that it is indeed possible to design a non-depolarizing neuromuscular blocker with the onset/offset characteristics of suxamethonium. Lastly, much has been learned about the variable clinical predictiveness of data obtained in various animal species with these compounds. This factor is probably mainly responsible for the difficulties and delay in producing the non-depolarizing suxamethonium equivalent.
本文试图总结超过25年的化学和药理学研究，这些研究旨在寻找基于氨基雄甾烷骨架的具有临床应用价值的肌肉松弛剂。这一研究策略已产生了三种具有临床应用价值的药物（泮库溴铵、维库溴铵和罗库溴铵），此外还证明，设计一种具有琥珀胆碱起效/消退特性的非去极化神经肌肉阻滞剂确实是可行的。最后，对于使用这些化合物在各种动物物种中获得的数据的临床预测性差异，人们也有了很多了解。这一因素可能是导致生产非去极化琥珀胆碱等效物困难和延迟的主要原因。
