On the nephrosclerotic action of 2-methyl-9-fluorocortisol, a highly active artificial mineralocorticoid.

Abstract

2-Methyl-9-fluorocortisol (2Me-9F-COL) was shown to possess extraordinarily intense mineralocorticoid but comparatively slight glucocorticoid activity, as judged by various tests (1). This compound, like other active mineralocorticoids (e.g., desoxycorticosterone and aldosterone), also exhibits a mutual antagonism with glucocorticoids (e.g., cortisone, cortisol) in the regulation of inflammation, anabolism and lymphatic-tissue development (2). On the other hand, the production by typical mineralocorticoids of renal damage and hypertension is not counteracted but rather enhanced by glucocorticoids (3, 4). It was to be expected, therefore, that a compound such as 2Me-9F-COL would produce marked renal lesions and hypertension by virtue of its strong mineralocorticoid potency, despite the fact that it also possesses some glucocorticoid activity. The experiments to be described here demonstrate that this is actually the case; indeed, 2Me-9F-COL proved to be the most potent nephrotoxic steroid among all those h...