袢利尿剂不与Tamm-Horsfall尿糖蛋白结合。

Loop-acting diuretics do not bind to Tamm-Horsfall urinary glycoprotein.

Brunisholz M C, Lynn K L, Hunt J S

Department of Nephrology, Christchurch Hospital, New Zealand.

Clin Sci (Lond). 1987 Sep;73(3):305-10. doi: 10.1042/cs0730305.

Abstract

Binding between the radiolabelled loop-acting diuretics ([14C]frusemide, [14C]ethacrynic acid and [3H]bumetanide) and human Tamm-Horsfall glycoprotein or human serum albumin in vitro was evaluated by equilibrium dialysis. 2. The diuretic action and binding to urinary Tamm-Horsfall glycoprotein of the radiolabelled diuretics in vivo, after intravenous administration, were examined in rabbits. 3. In vitro, all three radiolabelled diuretics bound strongly to human serum albumin, but not to Tamm-Horsfall glycoprotein. 4. Radiolabelled frusemide and bumetanide, but not ethacrynic acid, caused a diuresis in rabbits, but no binding between the drugs and Tamm-Horsfall glycoprotein was seen in vivo. 5. Binding to Tamm-Horsfall glycoprotein does not appear to be an important mechanism in the action of loop diuretics.

摘要

通过平衡透析评估放射性标记的襻利尿剂（[14C]呋塞米、[14C]依他尼酸和[3H]布美他尼）与人类Tamm-Horsfall糖蛋白或人血清白蛋白在体外的结合情况。2. 在兔子体内静脉注射后，研究放射性标记利尿剂的利尿作用及其与尿Tamm-Horsfall糖蛋白的结合情况。3. 在体外，所有三种放射性标记的利尿剂都与人血清白蛋白强烈结合，但不与Tamm-Horsfall糖蛋白结合。4. 放射性标记的呋塞米和布美他尼（而非依他尼酸）可使兔子产生利尿作用，但在体内未观察到药物与Tamm-Horsfall糖蛋白之间的结合。5. 与Tamm-Horsfall糖蛋白的结合似乎不是襻利尿剂作用的重要机制。