Just M, Röckel A, Stanjek A, Bode F
Naunyn Schmiedebergs Arch Pharmacol. 1975;289(3):229-36. doi: 10.1007/BF00499977.
The bovine protease inhibitor aprotinin (Trasylol) has a high affinity to the kidney and is preferentially pinocytized in the proximal tubule. After i.v. injection of 1mug 124 I aprotinin the blood content decreases to 2.8% of the primary injected amount within 3 hrs, while simultaneously each kidney contains 29%. This substance was used to test whether or not a peptide which is pinocytized, is released in the intact form into the peritubular blood. By a cross circulation technique with two unilaterally nephrectomized rats we were unable to detect any transport of pinocytized, intact peptide through the proximal tubule cell over the observed cross circulation period of 1-8 hrs even when using 5000 times the above dosage. Since the total amount of aprotinin in the kidney is immunologically reactive (ca. 97%), and 65% of the radioactivity in the blood is not reactive after 6 hrs, we believe that the last step in the absorption process consists in digestion inside the lysosomes and instantaneous release of the split products into the blood.
牛蛋白酶抑制剂抑肽酶(特血乐)对肾脏具有高亲和力,且优先在近端小管中被胞饮。静脉注射1μg ¹²⁴I抑肽酶后,血液中的含量在3小时内降至初始注射量的2.8%,而与此同时,每个肾脏中含有29%。该物质被用于测试被胞饮的肽是否以完整形式释放到肾小管周围血液中。通过对两只单侧肾切除大鼠采用交叉循环技术,即使使用上述剂量的5000倍,在观察到的1 - 8小时交叉循环期间,我们也未能检测到被胞饮的完整肽通过近端小管细胞的任何转运。由于肾脏中抑肽酶的总量具有免疫反应性(约97%),且6小时后血液中65%的放射性无反应,我们认为吸收过程的最后一步在于溶酶体内的消化以及裂解产物立即释放到血液中。