Holohan P D, Ross C R
J Pharmacol Exp Ther. 1980 Oct;215(1):191-7.
Transport for organic cations has been described in both luminal and antiluminal membranes. The two transport systems difer from one another on the basis of kinetic parameters and countertransport. By using N1-[3H]methylnicotinamide as the indication cation, a series of organic cations (which were known to be secreted) were tested for their capacity to stimulate countertransport. The phenomenon of countertransport was symmetrical in that it was observed for both influx and efflux in both membranes. However, under appropriate conditions, certain organic cations were effective in producing "uphill" transport of N1-[3H]methylnicotinamide in the luminal membrane and the effect was limited to that membrane exclusively. Detailed analysis of countertransport in the luminal membrane showed quantitative differences in the maximal stimulation produced by the various cations: giving rise to the relationship that the concentration of organic cation which gave one-half maximal N1-[3H]methylnicotinamide countertransport approximated its affinity constant. The data were interpreted to suggest that all the members of the organic cation series tested are translocated across the luminal membrane by the same carrier but that they are moved at different rates.
有机阳离子的转运已在管腔膜和反管腔膜中得到描述。这两种转运系统在动力学参数和逆向转运方面彼此不同。以N1-[3H]甲基烟酰胺作为指示阳离子,测试了一系列已知会被分泌的有机阳离子刺激逆向转运的能力。逆向转运现象是对称的,因为在两种膜的流入和流出过程中都观察到了这种现象。然而,在适当条件下,某些有机阳离子能有效地使管腔膜中的N1-[3H]甲基烟酰胺进行“上坡”转运,且这种作用仅限于该膜。对管腔膜中逆向转运的详细分析表明,各种阳离子产生的最大刺激存在定量差异:导致这样一种关系,即产生半数最大N1-[3H]甲基烟酰胺逆向转运的有机阳离子浓度近似于其亲和常数。这些数据被解释为表明所测试的有机阳离子系列的所有成员都是通过同一载体跨管腔膜转运的,但它们的转运速率不同。