Ozegović B, Schön E, Milković S
Arch Int Pharmacodyn Ther. 1979 Sep;241(1):16-23.
Triamterene (2,4,7-triamino-6-phenylpteridine) is a potassium-sparing diuretic whose mechanism of action is not clear. Experiments were performed to study the effect of triamterene upon the activity of Na-K-ATP-ase in the kidney plasma membranes. This enzyme, dissolved within the membrane bilayer, has been considered to be a biochemical vehicle for the active transport of sodium across the cell membrane. Intact and adrenalectomized rats were subjected to a five-day treatment with triamterene in a daily dose of 1.5 mg/100 g body weight. Triamterene was also administered to a group of intact, salt-loaded, rats. The activity of Na-K-ATP-ase in the kidney plasma membranes of intact and adrenalectomized rats treated with triamterene was decreased by 22.4% (p less than 0.05) and 37.2% (p less than 0.05), respectively. The activity of Na-K-ATP-ase in the renal plasma membranes of intact, salt-loaded, rats underwent greater decrease--63% (p less than 0.05). If the decreased activity of Na-K-ATP-ase in the kidney plasma membranes of rats treated with triamterene manifested the diuretic action of triamterene, results obtained in adrenalectomized rats would suggest that triamterene acts directly on the kidney, not via the adrenal glands.
氨苯蝶啶(2,4,7 - 三氨基 - 6 - 苯基蝶啶)是一种保钾利尿剂,其作用机制尚不清楚。进行了实验以研究氨苯蝶啶对肾质膜中钠钾ATP酶活性的影响。这种溶解在膜双分子层中的酶被认为是钠跨细胞膜主动转运的生化载体。对完整大鼠和肾上腺切除大鼠进行为期五天的氨苯蝶啶治疗,每日剂量为1.5毫克/100克体重。也对一组完整的、盐负荷的大鼠给予氨苯蝶啶。用氨苯蝶啶治疗的完整大鼠和肾上腺切除大鼠的肾质膜中钠钾ATP酶活性分别降低了22.4%(p<0.05)和37.2%(p<0.05)。完整的、盐负荷的大鼠肾质膜中钠钾ATP酶活性下降幅度更大——63%(p<0.05)。如果用氨苯蝶啶治疗的大鼠肾质膜中钠钾ATP酶活性的降低体现了氨苯蝶啶的利尿作用,那么在肾上腺切除大鼠中获得的结果表明氨苯蝶啶直接作用于肾脏,而非通过肾上腺。