肾腺苷酸环化酶——利尿剂的作用

Renal adenylate cyclase-effects of diuretics.

作者信息

Ebel H, Sharp G W

出版信息

Eur J Pharmacol. 1975 Dec;34(2):273-81. doi: 10.1016/0014-2999(75)90252-6.

Abstract

The in vitro effect of various diuretics on rat kidney adenylate cyclase was investigated in crude homogenates of the cortex, the outer and inner medulla. 10-3 M furosemide inhibited adenylate cyclase by 40% in the cortex, by 16% in the outer medulla and by 43% in the inner medulla. 10-3 M ethacrynic acid inhibited adenylate cyclase activity by 65% in the cortex, 59% in the outer medulla and by 57% in the inner medulla. Amiloride produced no significant inhibition of the adenylate cyclase reaction. In the cortex, furosemide partially inhibited adenylate cyclase under basal, fluoride-stimulated and parathyroid hormone-stimulated conditions. Ethacrynic acid produced a strong inhibition of adenylate cyclase activation by F- and parathyroid hormone. In the inner medulla 10-2 M F- and 1 mU antidiuretic hormone reversed the furosemide effect on adenylate cyclase. Ethacrynic acid produced a strong inhibition of adenylate cyclase in the presence of F- and antidiuretic hormone. It is suggested that inhibition of renal adenylate cyclase might be a possible mode of action of certain diuretics.

摘要

在大鼠肾皮质、外髓质和内髓质的粗匀浆中研究了各种利尿剂对大鼠肾腺苷酸环化酶的体外作用。10⁻³M速尿使皮质中的腺苷酸环化酶抑制40%，外髓质中抑制16%，内髓质中抑制43%。10⁻³M依他尼酸使皮质中的腺苷酸环化酶活性抑制65%，外髓质中抑制59%，内髓质中抑制57%。氨氯吡咪对腺苷酸环化酶反应无明显抑制作用。在皮质中，速尿在基础、氟刺激和甲状旁腺激素刺激条件下部分抑制腺苷酸环化酶。依他尼酸强烈抑制氟和甲状旁腺激素对腺苷酸环化酶的激活作用。在内髓质中，10⁻²M氟和1mU抗利尿激素可逆转速尿对腺苷酸环化酶的作用。依他尼酸在有氟和抗利尿激素存在时强烈抑制腺苷酸环化酶。提示抑制肾腺苷酸环化酶可能是某些利尿剂的一种作用方式。