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pA原理在药物效应增强方面的扩展及其在某些抗胆碱酯酶和强心苷生物测定中的应用。

An extension of pA principle to the potentiation of drug effects, and its application to the biological assay of some anticholinesterases and cardenolides.

作者信息

Ishikawa N, Ichikawa T, Tsuru H, Shigei T

出版信息

Jpn J Pharmacol. 1980 Feb;30(1):49-58. doi: 10.1254/jjp.30.49.

Abstract

A new scale for the potentiation was introduced and was termed pA1/2. The value can be calculated by using an equation; (Formula: see text), which is similar to that which is used for the calculation of pA2. For the use of the equation, the parallel shift of the dose-response curve and the unchanged maximum response are prerequisites. This experiment showed the validity and the usefulness of calculating the pA1/2 values, in the biological assay. In the assay of anticholinesterases, the potentiating effects of neostigmine or physostigmine on the acetylcholine-induced contraction were examined, by using frog's rectus abdominis. The pA1/2 values obtained in the presence of two different concentrations of anticholinesterases were the same, indicating that pA1/2 is a parameter which is specific to the potentiator. The potentiating effects of some cardenolides on the K-induced contracture were examined, by using the frog's ventricular muscles. The relative potencies of four cardenolides obtained from the pA1/2 values well agreed with those reported earlier. The amount of the cardenolides required for this assay was smaller than required for other methods.

摘要

引入了一种新的增效作用量表,称为pA1/2。该值可通过一个方程式计算得出;(公式:见文本),这与用于计算pA2的方程式相似。使用该方程式时,剂量 - 反应曲线的平行移动和最大反应不变是前提条件。本实验证明了在生物测定中计算pA1/2值的有效性和实用性。在抗胆碱酯酶测定中,使用青蛙的腹直肌研究了新斯的明或毒扁豆碱对乙酰胆碱诱导收缩的增效作用。在两种不同浓度的抗胆碱酯酶存在下获得的pA1/2值相同,表明pA1/2是增效剂特有的参数。使用青蛙心室肌研究了一些强心苷对钾诱导挛缩的增效作用。从pA1/2值获得的四种强心苷的相对效价与先前报道的结果非常一致。该测定所需的强心苷量比其他方法所需的量小。

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