Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters

Jensen Ole; Rafehi Muhammad; Tzvetkov Mladen V; Brockmoeller Juergen

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Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters

机译：有机阳离子转运蛋白的立体选择性细胞吸收肾上腺素能激动剂和拮抗剂

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摘要

Stereoselectivity is well described for receptor binding and enzyme catalysis, but so far has only been scarcely investigated in carrier-mediated membrane transport. We thus studied transport kinetics of racemic (anti) adrenergic drugs by the organic cation transporters OCT1 (wild-type and allelic variants), OCT2, OCT3, MATE1, and MATE2-K with a focus on stereospecificity.

机译：对于受体结合和酶催化描述了立体选择性良好的描述，但到目前为止仅在载体介导的膜运输中仍然在缺乏研究。因此，我们研究了由有机阳离子转运蛋白（野生型和等位基因变体），10月，Oct3，Mate1和Mate2-K的有机阳离子转运蛋白转运药物的传输动力学，并侧重于立体化。

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来源
《Biochemical Pharmacology》 |2020年第1期|共10页
作者
Jensen Ole; Rafehi Muhammad; Tzvetkov Mladen V; Brockmoeller Juergen;
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作者单位

Georg August Univ Univ Med Ctr Gottingen Inst Clin Pharmacol D-37075 Gottingen Germany;

Georg August Univ Univ Med Ctr Gottingen Inst Clin Pharmacol D-37075 Gottingen Germany;

Georg August Univ Univ Med Ctr Gottingen Inst Clin Pharmacol D-37075 Gottingen Germany;

Georg August Univ Univ Med Ctr Gottingen Inst Clin Pharmacol D-37075 Gottingen Germany;

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原文格式 PDF
正文语种 eng
中图分类药理学;
关键词
Beta-adrenergic drugs; Enantiomers; Organic cation transporters; SLC22A1; Solute carriers;

机译：β-肾上腺素能药物;对映体;有机阳离子转运蛋白;SLC22A1;溶质载体;

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专利

1. Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters [J] . Jensen Ole, Rafehi Muhammad, Tzvetkov Mladen V, Biochemical Pharmacology . 2020,第1期

机译：有机阳离子转运蛋白的立体选择性细胞吸收肾上腺素能激动剂和拮抗剂
2. The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK(1) cell monolayers. [J] . DudleyAJ, BleasbyK, BrownCD British Journal of Pharmacology . 2000,第1期

机译：有机阳离子转运蛋白OCT2介导跨肾LLC-PK（1）细胞单层的顶膜吸收β-肾上腺素受体拮抗剂。
3. Beta-2 Adrenergic Agonists Are Substrates and Inhibitors of Human Organic Cation Transporter 1 [J] . Salomon Johanna J., Hagos Yohannes, Petzke Soeren, Molecular pharmaceutics . 2015,第8期

机译：Beta 2肾上腺素能激动剂是人类有机阳离子转运蛋白1的底物和抑制剂。
4. Different inverse agonist activities ofbeta-adrenergic receptor antagonists-pharmacologicalcharacterization and therapeutical implicationsin the treatment of chronic heart failure [C] . Christoph Maack, Michael Bohm Fundaci髇 Dr. Antonio Esteve . 2003

机译：不同逆激动剂活性的β-肾上腺素能受体拮抗剂 - 药理特征和治疗意义治疗慢性心力衰竭
5. Studies on the Survival of Ovarian Cancer Cells Following Treatment with Beta-Adrenergic Receptor Agonists and Antagonists [D] . Horan, Noah Patrick. 2020

机译：用β-肾上腺素能受体激动剂和拮抗剂治疗卵巢癌细胞存活的研究
6. The organic cation transporter OCT2 mediates the uptake of β-adrenoceptor antagonists across the apical membrane of renal LLC-PK1 cell monolayers [O] . Adam J Dudley, Kelly Bleasby, Colin D A Brown 2000

机译：有机阳离子转运蛋白OCT2通过肾脏LLC-PK1细胞单层的顶膜介导β-肾上腺素受体拮抗剂的摄取。
7. The organic cation transporter OCT2 mediates the uptake of β-adrenoceptor antagonists across the apical membrane of renal LLC-PK1 cell monolayers [O] . Dudley, Adam J, Bleasby, Kelly, Brown, Colin D A 2000

机译：有机阳离子转运蛋白OCT2通过肾脏LLC-PK1细胞单层的顶膜介导β-肾上腺素受体拮抗剂的摄取。

Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters

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