Holm J
Arch Int Pharmacodyn Ther. 1978 Jul;234(1):15-23.
The polymethylene-bisquaternary amine 14C-decamethonium accumulates in mouse kidney cortex slices incubated in Krebs-Ringer bicarbonate buffer (37 degrees C, pH 7.4) aerated with O2-CO2 95:5 v/v%. The accumulation rate was enhanced in the presence of monoquaternary amines which on the other hand depressed maximum accumulation ratio of decamethonium in the tissue. The stimulation phenomenon was apparently related to the intracellular concentration of monoquaternary amine since tissue preloaded with a monoquaternary amine took up decamethonium at an increased rate. This effect was due to an accelerated influx of decamethonium and not to inhibition of efflux since no decamethonium efflux was shown to occur in wash-out experiments. Flux stimulation may represent an interaction phenomenon of accelerative exchange diffusion type. Furthermore, various amines inhibited accumulation of decamethonium in a competitive manner. The study supports the idea that common steps are involved in cellular transport of monoquaternary and polymethylene-bisquaternary amines in the kidney.
聚亚甲基双季铵盐14C - 十烃季铵在含有95:5(v/v%)氧气 - 二氧化碳的克雷布斯 - 林格碳酸氢盐缓冲液(37摄氏度,pH 7.4)中孵育的小鼠肾皮质切片中蓄积。在单季铵盐存在的情况下,蓄积速率会提高,而单季铵盐另一方面会降低十烃季铵在组织中的最大蓄积率。这种刺激现象显然与单季铵盐的细胞内浓度有关,因为预先加载了单季铵盐的组织以增加的速率摄取十烃季铵。这种效应是由于十烃季铵的流入加速,而不是由于流出受到抑制,因为在洗脱实验中未显示有十烃季铵流出。通量刺激可能代表加速交换扩散类型的相互作用现象。此外,各种胺以竞争方式抑制十烃季铵的蓄积。该研究支持这样一种观点,即单季铵盐和聚亚甲基双季铵盐在肾脏中的细胞转运涉及共同步骤。