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首页> 外文期刊>Journal of pharmacokinetics and biopharmaceutics >Competitive inhibition of p-aminohippurate transport by quinapril in rabbit renal basolateral membrane vesicles.
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Competitive inhibition of p-aminohippurate transport by quinapril in rabbit renal basolateral membrane vesicles.

机译：奎那普利在兔肾基底外侧膜囊泡中对对氨基马尿酸盐转运的竞争性抑制。

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摘要

The mechanism of quinapril's interaction with the organic anion transporter was characterized by studying its effect on the transport of p-aminohippurate (PAH) in rabbit renal basolateral membrane vesicles (BLMV). Cis-inhibition studies demonstrated that quinapril was a specific and potent inhibitor of PAH. The Ki of quinapril was about 20 microM, a value similar to that of probenecid and eight-times lower than the K(m) value of 165 microM for PAH. Even though quinapril resulted in trans-inhibition of PAH uptake during counterflow studies, kinetic studies revealed that quinapril was a competitive inhibitor of PAH transport. This latter findings suggests that quinapril and PAH share a common binding site on the transporter. Overall, the results indicate that quinapril is a high-affinity inhibitor of the organic anion transporter in renal BLMV, and that drug-drug interactions may occur with other organic anions at the basolateral membrane of proximal cells.
机译：通过研究其对兔肾基底外侧膜囊泡（BLMV）中对氨基氨基嘌呤（PAH）转运的影响，表征了喹那普利与有机阴离子转运蛋白的相互作用机理。顺式抑制研究表明，奎那普利是PAH的特异有效抑制剂。奎那普利的Ki约为20 microM，与丙磺舒相似，且比PAH的165 microM的K（m）值低八倍。即使奎那普利在逆流研究期间导致反式抑制PAH摄取，动力学研究也显示奎那普利是PAH转运的竞争性抑制剂。后一个发现表明奎纳普利和多环芳烃在转运蛋白上有一个共同的结合位点。总体而言，结果表明奎纳普利是肾脏BLMV中有机阴离子转运蛋白的高亲和力抑制剂，并且药物-药物相互作用可能与近端细胞基底外侧膜上的其他有机阴离子发生。

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