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首页> 外文期刊>British Journal of Pharmacology >The pharmacological actions of polymethylene bistrimethylammonium salts
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The pharmacological actions of polymethylene bistrimethylammonium salts

机译:聚亚甲基双三甲基铵盐的药理作用

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This paper was an important milestone in the development of ideas about muscle and neuronal nico-tinic receptors. It is about the pharmacological actions of the series of compounds that consist of two quaternary ammonium groups joined by a polymethylene chain of variable length. Quaternary ammonium compounds were probably the first synthetic compounds to be investigated with a view to revealing a relationship between structure and activity (Crum Brown & Fraser, 1868, 1869), and they have featured in many studies since then. Although the paper by Paton & Zaimis (1949) is ostensibly a purely pharmacological investigation, it has actually contributed as much to physiology as to pharmacology. The paper describes in some detail the actions of compounds with 2 to 13 (and 18) meth-ylene groups between the quaternary nitrogens. A whole range of actions is investigated: neuromuscu-lar block and its (considerable) species-dependence, antagonism of neuromuscular block, direct actions on skeletal muscle (frog isolated rectus abdominis), ganglion blocking activity, anticholinesterase activity, oral activity, and surface activity effects. The main emphasis, though, was on neuromuscular block by the 10-methylene compound, C10, or decamethonium; the ganglion block effects were investigated in more detail by Paton & Zaimis (1951).
机译:这篇论文是关于肌肉和神经元烟碱受体的观念发展的重要里程碑。它涉及由两个可变长度的聚亚甲基链连接的两个季铵基团组成的一系列化合物的药理作用。为了揭示结构与活性之间的关系,季铵化合物可能是第一个被研究的合成化合物(Crum Brown&Fraser,1868,1869),从那时起,它们便在许多研究中得到了应用。尽管Paton&Zaimis(1949)的论文表面上纯粹是药理学研究,但实际上它对生理学和药理学的贡献都很大。该论文更详细地描述了在季氮之间具有2至13个(和18个)亚甲基的化合物的作用。研究了整个作用范围:神经肌肉阻滞及其(相当大的)物种依赖性,神经肌肉阻滞的拮抗作用,对骨骼肌的直接作用(青蛙分离出的腹直肌),神经节阻滞活性,抗胆碱酯酶活性,口服活性和表面活性活动效果。但是,主要重点是10-亚甲基化合物C10或十甲铵对神经肌肉的阻滞作用。 Paton&Zaimis(1951)更详细地研究了神经节阻滞作用。

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