Chatton J Y, Besseghir K, Roch-Ramel F
Institut de Pharmacologie de l'Université, Lausanne, Switzerland.
Am J Physiol. 1990 Oct;259(4 Pt 2):F613-8. doi: 10.1152/ajprenal.1990.259.4.F613.
To assess the role of nonionic diffusion of salicylic acid (pKa = 3) in the terminal nephron, we measured the passive permeability of [14C]salicylic acid in rabbit cortical collecting ducts isolated and perfused in vitro. This segment can produce and maintain a maximal pH gradient between blood and tubular fluid. When peritubular pH was kept constant at pH 7.4 the apparent permeability of salicylic acid (P', 10(-6) cm/s) was 6.2 +/- 1.1 at a luminal pH of 6.0, 17.2 +/- 5.3 at a luminal pH of 5.5, and 39.0 +/- 4.7 at a luminal pH of 5.0. These permeabilities were in close correlation with the percentage of nonionized salicylic acid present at each pH, indicating that only the nonionized molecule can diffuse across the collecting duct epithelium. By recalculating the permeability, taking into account only the concentration of the nonionized salicylic acid molecules, we obtained the apparent permeability of nonionized salicylic acid, which was no longer pH dependent and averaged 4,345 +/- 460 x 10(-6) cm/s. The apparent activation energy of this diffusion process was 9.3 +/- 1.2 kcal/mol as calculated from an Arrhenius plot.
为了评估水杨酸(pKa = 3)的非离子扩散在终末肾单位中的作用,我们测量了[14C]水杨酸在体外分离并灌注的兔皮质集合管中的被动通透性。该节段可在血液和肾小管液之间产生并维持最大的pH梯度。当肾小管周围pH保持在7.4不变时,水杨酸的表观通透性(P',10^(-6) cm/s)在管腔pH为6.0时为6.2±1.1,在管腔pH为5.5时为17.2±5.3,在管腔pH为5.0时为39.0±4.7。这些通透性与每个pH下存在的非离子化水杨酸的百分比密切相关,表明只有非离子化分子才能扩散穿过集合管上皮。通过重新计算通透性,仅考虑非离子化水杨酸分子的浓度,我们得到了非离子化水杨酸的表观通透性,其不再依赖于pH,平均为4345±460×10^(-6) cm/s。根据阿伦尼乌斯图计算,该扩散过程的表观活化能为9.3±1.2 kcal/mol。