Comparative Pharmacology of Nucleoside Transport Inhibitors
Comparative Pharmacology of Nucleoside Transport Inhibitors
复制标题
核苷转运抑制剂的比较药理学
DOI：
10.1080/07328319108047235
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发表时间：
1991
期刊：
影响因子：
--
通讯作者：
P. Janssen
中科院分区：
文献类型：
--
作者：
H. Belle;P. Janssen
摘要现有的几种核苷转运抑制剂对洗涤的人红细胞的转运蛋白几乎是等效的。然而，在人血浆存在下的结合紧密性和活性以及静脉内或口服给药时的离体抑制和作用持续时间存在很大差异。举例说明了核苷转运抑制对缺血心肌中腺苷积累的显著影响。这可能解释了显着的心脏保护在几个模型时，核苷转运抑制剂与适当的药代动力学曲线（如R 75 231）的应用。
Abstract The few existing nucleoside transport inhibitors are almost equipotent on the transporter in washed human erythrocytes. Large differences exist however in tightness of binding and activity in the presence of human plasma, as well as in ex vivo inhibition and duration of action when given intravenously or orally. Examples are presented of the marked effect of nucleoside transport inhibition on adenosine accumulation in ischemic myocardium. That may explain the remarkable cardioprotection in several models when a nucleoside transport inhibitor with an appropriate pharmacokinetic profile (such as R 75 231) is applied.