Relationship between anti-acetylcholine and anti-tremorine activity in anti-parkinsonian and related drugs

机译：抗帕金森病及相关药物中抗乙酰胆碱和抗震颤活性的关系

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摘要

The anti-acetylcholine potency of a number of anti-Parkinsonism drugs and related phenothiazine compounds was determined using the isolated guinea-pig ileum. The antagonism was assessed by the difference between the pA2 and pA10 values and by log concentration-response curves for acetylcholine in presence and absence of the antagonists. All compounds except chlorpromazine showed some evidence of competitive antagonism to acetylcholine. The anti-tremor potency of the compounds was assessed from suppression of Tremorine-induced tremors in mice. There was a relation between anti-acetylcholine and anti-Tremorine potency among the anti-Parkinsonism drugs, but not among the phenothiazine compounds. Some implications of the findings are discussed in relation to the mode of action of anti-Parkinsonism drugs.

机译：使用分离的豚鼠回肠测定了许多抗帕金森氏症药物和相关的吩噻嗪化合物的抗乙酰胆碱效能。通过存在和不存在拮抗剂时乙酰胆碱的pA2和pA10值之间的差异以及对数浓度-响应曲线来评估拮抗作用。除氯丙嗪外，所有化合物均显示出对乙酰胆碱具有竞争性拮抗作用的证据。通过抑制小鼠中震颤诱导的震颤来评估化合物的抗震颤能力。在抗帕金森氏症药物中，抗乙酰胆碱和抗-Tremorine的效力之间存在关系，但在吩噻嗪类化合物之间则没有关系。讨论了有关发现的一些意义，涉及抗帕金森氏病药物的作用方式。

著录项

期刊名称 British Journal of Pharmacology and Chemotherapy
作者
A. Ahmed; P. B. Marshall;
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作者单位

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年(卷),期 1962(18),2
年度 1962
页码 247–254
总页数 8
原文格式 PDF
正文语种
中图分类药学;
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1. Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationships. [J] . Azam F, Ibn Rajab IA, Alruiad AA Die Pharmazie . 2009,第12期

机译：腺苷A2A受体拮抗剂作为新型抗帕金森病药物：结构-活性关系的综述。
2. Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationships. [J] . Azam F, Ibn Rajab IA, Alruiad AA Die Pharmazie . 2009,第12期

机译：腺苷A2A受体拮抗剂作为新型抗帕金森代理商：对结构活动关系的综述。
3. Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationships. [J] . Azam F, Ibn Rajab IA, Alruiad AA Die Pharmazie . 2009,第12期

机译：腺苷A2A受体拮抗剂作为新型抗帕金森代理商：对结构活动关系的综述。
4. Machine learning algorithms used in Quantitative structure-activity relationships studies as new approaches in drug discovery [C] . Mourad Stitou, Hamid Toufik, Mohammed Bouachrine, International Conference on Intelligent Systems and Advanced Computing Sciences . 2019

机译：定量结构与活性关系研究中使用的机器学习算法作为药物发现的新方法
5. A structure-activity approach to drug action in pharmacology: (A) Structure-activity relationships involved in DT-diaphorase (NQO1) mediated reduction kinetics and mode of action of anticancer bioreductive benzoquinone alkylating agents. (B) Structural characteristics of novel NMDA receptor antagonists required for renal tubule organic cation secretion . [D] . Fourie, Jeanne. 2004

机译：一种在药理学中用于药物作用的结构活性方法：（A）DT-黄递酶（NQO1）介导的抗癌生物还原苯醌烷基化剂的还原动力学和作用方式的结构活性关系。（B）肾小管有机阳离子分泌所需的新型NMDA受体拮抗剂的结构特征。
6. Integrating Drug’s Mode of Action into Quantitative Structure-Activity Relationships for Improved Prediction of Drug-Induced Liver Injury [O] . Leihong Wu, Zhichao Liu, Scott Auerbach, -1

机译：将药物的作用方式整合到定量的构效关系中以更好地预测药物引起的肝损伤
7. Relationship between anti-acetylcholine and anti-tremorine activity in anti-parkinsonian and related drugs [O] . Ahmed, A., Marshall, P. B. 1962

机译：抗帕金森病及相关药物中抗乙酰胆碱和抗震颤活性的关系

Relationship between anti-acetylcholine and anti-tremorine activity in anti-parkinsonian and related drugs

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