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[奇诺因-103对大鼠心脏钠钾激活三磷酸腺苷酶的作用]

[Effect of Chinoin-103 on Na+, K+-activated adenosine triphosphatase of the rat heart].

作者信息

Szabó J, Nosztray K, Papp Z, Szegi J

出版信息

Acta Pharm Hung. 1989 Jul;59(4):179-88.

PMID:2570501
Abstract

Effect of a new beta-blocking agent, a cardioselective aryl oxybutanolamine derivative, the Chinoin-103 on basal and total ATP-aze activities has been studied in total homogenizatum of rat heart. The effect has been compared to previous results of propranolol and to effect of practolol, respectively. It has been established that DL-Chinoin-103-similarly to DL-propranolol but in a little higher concentration--has significantly impeted both basal and total ATP-aze activities. Since in the nase of practolol similar effect was not obsreved and furthermore the effect could not be suspended by isoproterenol, the authors suppose that impediment of sarcolemmal ATP-aze activities cannot primarily be attributed to beta-blocking effect of compounds. Study of effect of racemic Chinoin-103 on enzymatic kinetic parameters of basal and total ATP-aze acticities has shown that primarily the reaction rate had decreased, affinity to substratum had not changed in the case of total ATP-aze and it has moderately decreased in the case of basal ATP-aze. The results of this publication has drawn attention to the fact that some beta-receptor blocking compounds may have other specific membrane effects besides antagonism on beta-receptors.

摘要

一种新型β受体阻滞剂,一种心脏选择性芳氧基丁醇胺衍生物Chinoin-103对大鼠心脏全匀浆中基础和总ATP酶活性的影响已被研究。该影响已分别与普萘洛尔的先前结果以及醋丁洛尔的影响进行了比较。已确定DL-Chinoin-103——与DL-普萘洛尔类似,但浓度稍高——显著抑制了基础和总ATP酶活性。由于在醋丁洛尔的情况下未观察到类似效果,而且该效果不能被异丙肾上腺素消除,作者推测肌膜ATP酶活性的抑制不能主要归因于化合物的β受体阻滞作用。对消旋Chinoin-103对基础和总ATP酶活性的酶动力学参数的影响研究表明,主要是反应速率降低,对于总ATP酶而言对底物的亲和力未改变,而对于基础ATP酶而言适度降低。该出版物的结果引起了人们对以下事实的关注,即一些β受体阻断化合物除了对β受体的拮抗作用外,可能还有其他特定的膜效应。

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