Turnheim K, Luger A
Wien Klin Wochenschr. 1980;92(20):721-4.
In isolated epithelia of rabbit descending colon the short-circuit current (Isc) is solely attributable to net transepithelial Na-transport, which in turn is identical with the unidirectional Na-influx across the luminal cell membranes. Amiloride blocks Isc by inhibiting luminal Na-influx into the cells. The type of inhibition exerted by amiloride in this tissue has to be termed mixed-type, since both the affinity of Na to its transport system and the maximal transport capacity are reduced. Na, on the other hand, is a competitive antagonist of the amiloride effect with a Ki of 136 mM; therefore KA, the amiloride-concentration at which the amiloride-effect is half-maximal, is increased from 0.14 microM at 5 mM Na in the incubation medium to 0.29 microM at 140 mM Na. It is conceivable that an "amiloride-like" action of Na may be responsible for the saturability of luminal Na-influx with increasing Na-concentrations.
在兔降结肠的离体上皮中,短路电流(Isc)完全归因于跨上皮的净钠转运,而这又与通过腔面膜进入细胞的单向钠内流相同。氨氯吡咪通过抑制钠向细胞内的腔面内流来阻断Isc。氨氯吡咪在该组织中产生的抑制类型必须称为混合型,因为钠对其转运系统的亲和力和最大转运能力都降低了。另一方面,钠是氨氯吡咪效应的竞争性拮抗剂,其Ki为136 mM;因此,使氨氯吡咪效应达到半数最大效应的氨氯吡咪浓度(KA),在孵育培养基中钠浓度为5 mM时为0.14 microM,在钠浓度为140 mM时增加到0.29 microM。可以想象,随着钠浓度的增加,钠的“氨氯吡咪样”作用可能是腔面钠内流饱和性的原因。