[杯芳烃C-90对肌层质膜Ca2+、Mg2+- atp酶活性和肌层非兴奋细胞Ca2+浓度的动力学性质]。

Veklich To, Shkrabak Oa, Mazur IuIu, Rodik Rv, Boĭko Vi, V. Kalchenko, S. Kosterin
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引用次数: 1

摘要

质膜Ca2+,Mg2+- atp酶是一般肌张力控制机制的重要组成部分,它也有助于肌肉收缩后的紧张松弛。实验采用0.1%洋地黄苷溶液处理子宫肌层细胞膜悬浮液。作者研究了杯[4]芳烃C-90(5,11,17,23-四(三氟)甲基(苯基磺酰亚胺)-甲基氨基-25,26,27,28-四丙氧杯[4]芳烃)对Ca2+,Mg2+- atp酶活性的抑制作用(10.5量级为20.2 +/- 0.5 mkM)。杯[4]芳烃C-90对Ca2+, Mg2+- atp酶活性的抑制作用可以解释为杯[4]芳烃碱基上四个三氟甲基(苯基磺酰基)甲基胺基的协同作用,而不是与四酚大环或单独的药效团磺胺基的协同作用。考虑到杯[4]芳烃C-90抑制质膜Ca2+,Mg2+- atp酶活性的既定动力学模式,建立了非兴奋子宫肌细胞基础钙浓度控制的稳态动力学模型。假设所获得的结果可能有希望在杯[4]芳烃C-90的基础上创造新一代(“超分子”)药理学药物-子宫基底张力刺激剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Kinetic properties of calixarene C-90 action on the myometrial plasma membrane Ca2+,Mg2+-Atpase activity and on the Ca2+ concentration in unexcited cells of the myometrium].
Plasma membrane Ca2+,Mg2+-ATPase is an important element of general myometrium tonus control mechanism, which also makes a contribution to muscle tension relaxation after its contraction. Expiriments were done on the myometrial cell plasma membrane suspension, which was treated with 0.1% digitonin solution. The authors have investigated the inhibitory action of calix[4]arene C-90 (5,11,17,23-tetra(trifluor) methyl(phenylsulphonylimino)-methylamino-25,26,27,28-tetra propoxi-calix[4]arene) on the Ca2+,Mg2+-ATPase activity (the magnitude of 10.5 was 20.2 +/- 0.5 mkM). The inhibitory action of calix[4]arene C-90 on the activity of Ca2+, Mg2+-ATPase is explained as cooperative action of four trifluormethyl(phenylsulfonylimino)methylamino groups that are spatially oriented on the calix[4]-arene base rather than with the action of tetra-phenol macrocycle or separate pharmacophore sulphonilamidin groups. Considering established kinetic pattern of calix[4]arene C-90 inhibitory action on the plasma membrane Ca2+,Mg2+-ATPase activity, stationary kinetical model of basal calcium concentration control in unexcited uterus myocytes was developed. It is assumed that obtained results may be promising for creation of new generation ("supramolecular") pharmacological agent - uterus basal tonus stimulator - on the base of calix[4] arene C-90.
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