Yusufi A N, Szczepanska-Konkel M, Kempson S A, McAteer J A, Dousa T P
Biochem Biophys Res Commun. 1986 Sep 14;139(2):679-86. doi: 10.1016/s0006-291x(86)80044-4.
Phosphonoformic acid was a potent competitive inhibitor of Na+/Pi cotransport by brush border membrane vesicles isolated from human renal cortex (Ki 31 microM). The Na+/Pi cotransport system in rat renal brush border membrane vesicles was much less sensitive to inhibition (Ki 210 microM). Na+/Pi cotransport by cultured cells derived from human renal cortex also was inhibited by phosphonoformic acid. Both in isolated membranes and cells the inhibition was dose-dependent, competitive, and specific for Pi. The effectiveness of phosphonoformic acid on Na+/Pi cotransport in human kidney suggests that its administration may be a useful maneuver to increase renal Pi excretion.
膦甲酸是从人肾皮质分离的刷状缘膜囊泡对Na⁺/Pi共转运的一种强效竞争性抑制剂（Ki为31微摩尔）。大鼠肾刷状缘膜囊泡中的Na⁺/Pi共转运系统对抑制作用的敏感性要低得多（Ki为210微摩尔）。来自人肾皮质的培养细胞的Na⁺/Pi共转运也受到膦甲酸的抑制。在分离的膜和细胞中，抑制作用都是剂量依赖性的、竞争性的且对Pi具有特异性。膦甲酸对人肾中Na⁺/Pi共转运的作用表明，给予膦甲酸可能是增加肾Pi排泄的一种有效方法。
