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首页> 外文期刊>Life sciences >Neuromuscular blocking N,N'-polymethylene bistropanium, bis 3alpha-hydroxytropanium and bis 3-oxotropanium compounds.
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Neuromuscular blocking N,N'-polymethylene bistropanium, bis 3alpha-hydroxytropanium and bis 3-oxotropanium compounds.

机译：神经肌肉阻滞N，N'-多亚甲基双stropanium，双3alpha-hydroxytropanium和双3-氧代tropanium化合物。

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摘要

To explore the role of ester groups in the neuromuscular blocking (NMB) property of various quaternary ammonium tropinesters, we have synthesized and pharmacologically evaluated twenty bisquaternary ammonium derivatives where two tropane (I), 3alpha-hydroxytropane (II), or 3-oxotropane (III) moieties were connected on their nitrogen atoms with a polymethylene chain of C3-C12 length. The rank order of potency of these agents in the rat (evoked EMG responses of the ant. tibial muscle) was: I, II, and III. Most potent were the longer chain (e.g. C10-C12) compounds of series I, yet they were inferior to bisquaternary ammonium tropinester derivatives (e.g. N,N'-polymethylene bisquaternary tropinesters, or bisquaternary derivatives of dicarboxylic acid tropinesters). Although some of the agents (series I and II) showed a rapid onset and short duration of action-profile, they also exhibited cardiovascular side effects (e.g. cardiac vagal block and blood pressure changes). In the design of new NMB agents of rapid onset and short duration of action the presence of different ester groups in addition to an azabicyclo ring system (e.g. tropane), seems to be essential.
机译：为了探索酯基在各种季铵盐Tropinesters的神经肌肉阻滞（NMB）特性中的作用，我们合成了20个双季铵盐衍生物，并对其进行了药理学评估，其中有两种托烷（I），3alpha-hydroxytropane（II）或3-oxotropane（ III）部分在其氮原子上与C3-C12长的多亚甲基链相连。这些药物在大鼠中的效价等级（引起胫骨肌的EMG反应）为：I，II和III。最有效的是系列I的较长链（例如C10-C12）化合物，但它们不如双季铵盐Tropinester衍生物（例如N，N'-聚亚甲基双季戊酸Tropinesters或二元羧酸Tropinesters的双季铵衍生物）。尽管某些药物（系列I和II）显示起效快且作用曲线持续时间短，但它们也表现出心血管副作用（例如心脏迷走神经阻滞和血压变化）。在设计新的起效快，作用时间短的NMB药物中，除了氮杂双环系统（例如，托烷）外，还存在着不同的酯基，这似乎是必不可少的。

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