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人肾中肾有机阳离子转运的立体选择性抑制

Stereoselective inhibition of renal organic cation transport in human kidney.

作者信息

Wong L T, Smyth D D, Sitar D S

机构信息

Department of Pharmacology and Therapeutics, University of Manitoba, Winnipeg, Canada.

出版信息

Br J Clin Pharmacol. 1992 Nov;34(5):438-40. doi: 10.1111/j.1365-2125.1992.tb05653.x.

DOI:10.1111/j.1365-2125.1992.tb05653.x
PMID:1467141
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1381475/
Abstract

Amantadine was found to be concentrated by human cortical slices, with apparent Km and Vmax values of 187 +/- 11 microM and 1.37 +/- 0.28 nmol mg-1 min-1 respectively (mean +/- s.e. mean, n = 4). Addition of quinine (8S, 9R-(-)-isomer) or quinidine (8R, 9S-(+)-isomer) competitively inhibited this accumulation (apparent Ki values of 261 +/- 44 (n = 4) and 586 +/- 68 microM (n = 3), respectively). The stereoselectivity of this inhibition is the reverse of that seen with respect to the renal clearances of the diastereoisomers.

摘要

发现金刚烷胺可被人皮质切片摄取，其表观米氏常数（Km）和最大反应速度（Vmax）值分别为187±11微摩尔和1.37±0.28纳摩尔·毫克⁻¹·分钟⁻¹（平均值±标准误平均值，n = 4）。加入奎宁（8S，9R -（-）-异构体）或奎尼丁（8R，9S -（+）-异构体）可竞争性抑制这种摄取（表观抑制常数（Ki）值分别为261±44（n = 4）和586±68微摩尔（n = 3））。这种抑制作用的立体选择性与非对映异构体的肾脏清除率情况相反。

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Stereoselective inhibition of amantadine accumulation by quinine and quinidine in rat renal proximal tubules and cortical slices.奎宁和奎尼丁对大鼠肾近端小管和皮质切片中金刚烷胺蓄积的立体选择性抑制作用。
J Pharmacol Exp Ther. 1990 Oct;255(1):271-5.
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Interference with renal organic cation transport by (-)- and (+)-nicotine at concentrations documented in plasma of habitual tobacco smokers.（-）-尼古丁和（+）-尼古丁在习惯性吸烟者血浆中记录的浓度下对肾脏有机阳离子转运的干扰。
J Pharmacol Exp Ther. 1992 Apr;261(1):21-5.
9
Human tissues in biomedical research.生物医学研究中的人体组织。
Hum Pathol. 1979 May;10(3):245-8. doi: 10.1016/s0046-8177(79)80019-2.

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