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一类与利多氟嗪和米奥氟嗪相关的新化合物对人红细胞核苷摄取的抑制作用。

Inhibition of nucleoside uptake in human erythrocytes by a new series of compounds related to lidoflazine and mioflazine.

作者信息

Pirovano I M, Van Belle H, Ijzerman A P

机构信息

Dept. of Medicinal Chemistry, Center for Bio-Pharmaceutical Sciences, Leiden, The Netherlands.

出版信息

Eur J Pharmacol. 1990 Dec 15;189(6):419-22. doi: 10.1016/0922-4106(90)90040-5.

Abstract

The zero-trans influx of uridine in human erythrocytes is inhibited by lidoflazine and analogs thereof. The concentrations required for inhibition of nucleoside transport were higher when the compounds were simultaneously added with uridine than upon preincubation of the inhibitors with the erythrocytes. R70380 proved to be the most active compound in this respect, its IC50 value being 13 nM after preincubation. Even the reference compounds nitrobenzylthioinosine and dilazep were remarkably more potent with preincubation; dipyridamole, however, was not.

摘要

利多氟嗪及其类似物可抑制人红细胞中尿苷的零转运流入。当这些化合物与尿苷同时添加时,抑制核苷转运所需的浓度高于抑制剂与红细胞预孵育时的浓度。在这方面,R70380被证明是最具活性的化合物,预孵育后的IC50值为13 nM。即使是参考化合物硝基苄硫基肌苷和地拉齐普在预孵育时也明显更有效;然而,双嘧达莫并非如此。

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