A new approach to the control of arterial hypertension involving the administration of a methylated derivative of the naturally-occurring amino-acid dihydroxyphenylalanine (DOPA) has been studied in 33 patients. Alpha-methyl DOPA given orally was found to be a potent, and, in general, a smooth and well-tolerated hypotensive agent for treatment of severe and malignant hypertension. The agent seemed to have less adverse effect on renal function than other hypotensive agents. Also, the compound had no specific effect on sodium balance or aldosterone secretion. The data indicate that the compound does not interfere with endogenous norepinephrine synthesis as was thought at first. It has been suggested that alpha-methyl DOPA interferes with the activity or tissue release of norepinephrine. These results have interesting theoretical and practical implications in hypertensive vascular disease.
Cannon PJ, Whitlock RT, Morris RC, Angers M, Laragh JH. Effect of Alpha-Methyl DOPA in Severe and Malignant Hypertension. JAMA. 1962;179(9):673-681. doi:10.1001/jama.1962.03050090001001