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二异丙基氨基磺酸钠对肾小管转运的影响。

Effect of DIDS on renal tubular transport.

作者信息

Koschier F J, Stokols M F, Goldinger J M, Acara M, Hong S K

出版信息

Am J Physiol. 1980 Feb;238(2):F99-106. doi: 10.1152/ajprenal.1980.238.2.F99.

Abstract

Two stilbene derivates that had been used to covalently label the Cl- carrier in the erythrocyte were investigated for reactivity with the renal organic anion system. These compounds, 4,4'-diisothiocyanostilbene-2,2'-disulfonate (DIDS) and (4,4'-diisothiocyano)-dihydrostilbene-2,2'-disulfonate (H2DIDS), were found to be potent inhibitors (Ki congruent to 35 microM) of p-aminohippurate (PAH) transport in the renal cortical slice without affecting tetraethylammonium (TEA) transport or tissue viability. During renal clearance studies performed in the perfused kidney, DIDS decreased the PAH/inulin clearance ratio to congruent to 1. When the possible renal transport of [3H]H2DIDS was investigated, the renal slice transport or binding of [3H]H2DIDS reached a slice-to-medium ratio of congruent to 6, and this accumulation was decreased by probenecid. In perfused kidney experiments, the [3H]H2DIDS/inulin clearance ratio was congruent to 0.8. Since probenecid reduced this clearance ratio to congruent to 0.5, there was the possibility that H2DIDS underwent tubular secretion. In conclusion, DIDS and H2DIDS interacted with the renal organic anion transport system, which indicated that these compounds were possible probes for this transport system.

摘要

研究了两种曾用于对红细胞中的氯离子载体进行共价标记的芪衍生物与肾脏有机阴离子系统的反应活性。发现这些化合物,4,4'-二异硫氰酸芪-2,2'-二磺酸盐(DIDS)和(4,4'-二异硫氰基)-二氢芪-2,2'-二磺酸盐(H2DIDS),是肾皮质切片中对氨基马尿酸(PAH)转运的强效抑制剂(Ki约为35 microM),且不影响四乙铵(TEA)转运或组织活力。在灌注肾进行的肾脏清除研究中,DIDS使PAH/菊粉清除率降至约1。当研究[3H]H2DIDS可能的肾脏转运时,肾切片对[3H]H2DIDS的转运或结合达到切片与介质之比约为6,且丙磺舒可降低这种蓄积。在灌注肾实验中,[3H]H2DIDS/菊粉清除率约为0.8。由于丙磺舒将该清除率降至约0.5,因此H2DIDS有可能经历肾小管分泌。总之,DIDS和H2DIDS与肾脏有机阴离子转运系统相互作用,这表明这些化合物可能是该转运系统的探针。

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