Holohan P D, Ross C R
J Pharmacol Exp Ther. 1981 Feb;216(2):294-8.
The active step in the renal secretion of the organic cation N1-methylnicotinamide has been proposed to be the translocation across the luminal membrane. The presence of a H+:N1-methylnicotinamide antiport system has been found in luminal membrane vesicles isolated from dog kidney cortex but not in the antiluminal membrane. The conclusion reached is that N1-methylnicotinamide secretion is "secondarily active" and is driven by a proton gradient (urine to cell). The ph gradient in turn is created by the Na+:H+ antiport which is present in the luminal membrane. Therefore, two functionally linked antiport systems supply the energy for the active secretion of cationic drugs.
有机阳离子N1-甲基烟酰胺在肾脏分泌过程中的活跃步骤被认为是跨腔膜的转运。在从犬肾皮质分离出的腔膜囊泡中发现了H⁺:N1-甲基烟酰胺反向转运系统,但在反腔膜中未发现。得出的结论是,N1-甲基烟酰胺的分泌是“继发性主动转运”,由质子梯度(从尿液到细胞)驱动。反过来,pH梯度是由存在于腔膜中的Na⁺:H⁺反向转运体产生的。因此,两个功能相连的反向转运系统为阳离子药物的主动分泌提供能量。