FORSTER R P, HONG S K
J Gen Physiol. 1962 Mar;45(4):811-20. doi: 10.1085/jgp.45.4.811.
The maximal tubular transfer rates (Tm) of both p-aminohippurate (PAH) and diodrast (3,5-diiodo-4-pyridone-N-acetic acid or iodopyracet) were found to be fixed and reproducible when measured separately in Lophius (goosefish) under standard laboratory conditions. Expressed on a molar basis Tm(PAH) was four times Tm(D). However, when these transport competitors were presented simultaneously in equimolar concentrations with the plasma levels of each sufficiently high enough to saturate the carrier system, the relative rates of excretion were reversed with the diodrast transfer rate then four times that of PAH. The combined rate of excretion was far below Tm(PAH) alone, and roughly equal to Tm(D). Interaction with a common carrier was indicated by the gradations in degree of inhibition which resulted when plasma concentration ratios of diodrast to PAH were extended from 0.1 to 3.2, and PAH transfer rates expressed as percentage of Tm(PAH) were correspondingly depressed from 17 to 1.0 per cent respectively. These observations again point up the inverse relationship between transfer rate and competitive effectiveness which exists for members of a series of substances actively transported by a common mechanism. It appears that carrier affinity and dissociation characteristics may be quite different for various compounds in a series, and also that these parameters may vary significantly from species to species.
在标准实验室条件下,分别对安康鱼(狼鱼)进行测量时,发现对氨基马尿酸(PAH)和碘司特(3,5 - 二碘 - 4 - 吡啶酮 - N - 乙酸或碘吡啦啥)的最大肾小管转运率(Tm)是固定且可重复的。以摩尔为基础表示时,Tm(PAH)是Tm(D)的四倍。然而,当这些转运竞争物以等摩尔浓度同时呈现,且每种物质的血浆水平都足够高以饱和载体系统时,排泄的相对速率发生了逆转,此时碘司特的转运率是PAH的四倍。联合排泄率远低于单独的Tm(PAH),且大致等于Tm(D)。当碘司特与PAH的血浆浓度比从0.1扩展到3.2时,抑制程度呈现出梯度变化,PAH转运率分别从Tm(PAH)的17%相应降低到1.0%,这表明存在与共同载体的相互作用。这些观察结果再次表明,对于通过共同机制进行主动转运的一系列物质的成员来说,转运率与竞争效力之间存在反比关系。似乎对于一系列中的各种化合物,载体亲和力和解离特性可能有很大差异,而且这些参数在不同物种之间也可能有显著变化。