The comparative study of the vascular effects of agmatine and L-arginine as physiological precursors of NO indicated the following: When administered intravenously, both vasoactive substances produced a decrease of the systemic blood pressure in rats and rabbits, diminished in the case of agmatine and suppressed in that of arginine by the previous administration of L-NAME. Myorelaxing vascular effects were obtained in isolated thoracic aorta rings, precontracted with phenylephrine and noradrenaline. Endothelium removal suppressed the myorelaxing properties of L-arginine, without affecting the effects of agmatine, both before and after administration of L-NAME or yohimbine. The persistence of the relaxing effects of agmatine after NOS and guanylate-cyclase inhibition with methylene blue excludes the participation of NO and cGMP in their occurrence. The enhancement of agmatine myorelaxation by moxonidine pleads for the stimulation of imidazoline receptors.