“特异性”p -糖蛋白抑制剂zosuquidar （LY335979）也能弱抑制人体有机阳离子转运体。

IF 3.1 4区医学 Q2 PHARMACOLOGY & PHARMACY

Naunyn-Schmiedeberg's archives of pharmacology Pub Date : 2025-06-01 Epub Date: 2024-12-24 DOI:10.1007/s00210-024-03743-y

Gzona Bajraktari-Sylejmani, Rajamanikkam Kamaraj, Dirk Theile, Petr Pávek, Johanna Weiss

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引用次数: 0

摘要

Zosuquidar （LY335979）是一种广泛使用的实验性p -糖蛋白（P-gp）抑制剂，被认为是非常有效的，而且对P-gp也非常特异性。在这项体外和计算机研究中，我们首次证明了zosuquidar也抑制有机阳离子转运体（OCT） 1-3，尽管不如P-gp有效。当zosuquidar被用来抑制P-gp底物的细胞外排时，这一点仍然需要记住，P-gp底物同时被oct转运到细胞中。为了避免干扰，zosuquar浓度应保持在1µM以下。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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The "specific" P-glycoprotein inhibitor zosuquidar (LY335979) also weakly inhibits human organic cation transporters.

Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs. To avoid interference in these assays, zosuquidar concentrations should be kept below 1 µM.

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来源期刊

Naunyn-Schmiedeberg's archives of pharmacology 医学-药学

CiteScore

6.20

自引率

5.60%

发文量

142

审稿时长

4-8 weeks

期刊介绍： Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.