19-Acetylenic-deoxycorticosterone (19-A-DOC) is believed to be a compe
titive irreversible inhibitor of the synthesis of 19-nor-deoxycorticos
terone (19-nor-DOC), a potent mineralocorticoid implicated in some for
ms of human and animal hypertension. It has been shown to inactivate 1
1 beta/19-hydroxylase in hamster adrenal mitochondria. Dispersed bovin
e zona fasciculata cells were incubated for one hour with 1.5 X 10(-8)
M ACTH and 0, 1, 10, or 100 mu M 19-A-DOC and tritiated deoxycorticos
terone (DOC) substrate. Steroids were separated using two sequential t
hin-layer chromatography systems and their tritium content was counted
and corrected for recovery. The 19-A-DOC decreased synthesis of 19-hy
droxydeoxycorticosterone, the precursor of 19-nor-DOC. The inhibitor a
lso impaired 11-hydroxylation of DOC to form corticosterone. The data
suggest that 19-A-DOC is an effective inhibitor of 11 beta/19-hydroxyl
ase activity in dispersed bovine adrenal cells.