The actions of some cholinomimetic drugs on the isolated taenia of the guinea‐pig caecum
The actions of some cholinomimetic drugs on the isolated taenia of the guinea‐pig caecum
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某些拟胆碱药物对豚鼠盲肠孤立带绦虫的作用
DOI：
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发表时间：
1969
影响因子：
7.3
通讯作者：
M. Rand
中科院分区：
文献类型：
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作者：
F. Hobbiger;F. Mitchelson;M. Rand
1 已检查了 4-(间氯苯基氨基甲酰氧基)-2-丁炔基三甲基氯化铵 (McN-A-343)、N-苄基-3-吡咯烷基乙酸甲溴化物 (AHR-602)、四甲基铵 (TMA) 和胆碱苯醚对带绦虫的作用，并与乙酰胆碱、尼古丁和乙酰胆碱的作用进行了比较。 1,1-二甲基-4-苯基哌嗪 (DMPP)。 2 带绦虫对这些激动剂的反应在数量上和通常在质量上取决于制剂的基调。描述了一种考虑到音调对收缩高度的影响的方法。 3 乙酰胆碱、McN-A-343 和 AHR-602 仅产生收缩； TMA 产生收缩或双相反应；胆碱苯醚、尼古丁和DMPP产生收缩、松弛或双相反应。 4 通过东莨菪碱、神经节阻滞药物、河豚毒素和局部麻醉药对这些化合物的作用方式进行了分析。 5 结论是乙酰胆碱、McN-A-343、AHR-602、TMA 和胆碱苯醚作用于平滑肌中的毒蕈碱受体。胆碱苯醚对胆碱能神经元的烟碱受体有额外的作用。尼古丁和 DMPP 作用于胆碱能神经元和抑制性神经元的烟碱受体。有时还可以看到 TMA 和胆碱苯醚对后者有作用。 6 在东莨菪碱存在下，使用尼古丁或 DMPP、TMA 或胆碱苯醚，双相反应的部分收缩阶段（放松后收缩）最好解释为由初始放松触发，即“反弹收缩”。 7 所测试的化合物均未对神经元产生阿托品敏感作用。 8 在东莨菪碱存在的情况下，高浓度激动剂可以作用于低浓度激动剂不涉及的位点。 9 普鲁卡因对作用于平滑肌毒蕈碱受体的化合物的拮抗程度随测试化合物的不同而变化。
1 The actions on the taenia of 4‐(m‐chlorophenylcarbamoyloxy)‐2‐butynyltrimethylammonium chloride (McN‐A‐343), N‐benzyl‐3‐pyrrolidyl acetate methobromide (AHR‐602), tetramethylammonium (TMA) and choline phenyl ether have been examined and compared with the actions of acetylcholine, nicotine and 1,1‐dimethyl‐4‐phenylpiperazinium (DMPP). 2 Responses of the taenia to these agonists are quantitatively and often qualitatively dependent on the tone of the preparation. A method is described which makes allowance for the effect of tone on heights of contractions. 3 Acetylcholine, McN‐A‐343 and AHR‐602 produced only contractions; TMA produced contractions or biphasic responses; and choline phenyl ether, nicotine and DMPP produced contractions, relaxations or biphasic responses. 4 The mode of action of these compounds has been analysed by means of hyoscine, ganglion‐blocking drugs, tetrodotoxin and local anaesthetics. 5 It is concluded that acetylcholine, McN‐A‐343, AHR‐602, TMA and choline phenyl ether act on muscarinic receptors in the smooth muscle. Choline phenyl ether has an additional action on nicotinic receptors of cholinergic neurones. Nicotine and DMPP act on nicotinic receptors of cholinergic neurones and of inhibitory neurones. An action on the latter is sometimes also seen with TMA and choline phenyl ether. 6 With nicotine or DMPP, and TMA or choline phenyl ether in the presence of hyoscine, part of the contraction phase of biphasic responses (in which a contraction follows relaxation) is best explained as being triggered by the initial relaxation—that is, as a “rebound contraction”. 7 None of the compounds tested appeared to exert an atropine‐sensitive action on neurones. 8 In the presence of hyoscine high concentrations of agonists can act on sites not involved with lower concentrations. 9 The degree of antagonism obtained with procaine against compounds acting on muscarinic receptors on the smooth muscle varies with the compound tested.