ANTI-ADRENOCORTICAL ACTIVITY OF SKF-12185 AND SKF-525-A

  • 1 January 1976
    • journal article
    • research article
    • Vol. 25  (5) , 188-190
Abstract
The synthesis of aldosterone and 18-hydroxycorticosterone from tritiated corticosterone by sheep adrenal homogenate was studied in the presence of increasing concentrations of SKF 12185 [2-p-aminophenyl)-2-phenylethylamine], a known cortisol synthesis inhibitor. Approximately 98% inhibition of the synthesis of both steroids occurred with only 2 .times. 10-4 M of the drug. Incubation of a structurally closely related compound (SKF 525 A) [proadifen hydrochloride] under the same experimental conditions resulted in only 52% inhibition with higher concentrations (2 .times. 10-3 M). These findings could explain the marked aldosterone fall that occurs in SKF 12185 treated subjects and supports the therapeutic use of this product in treatment of hyperaldosteronism.

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