It has been suggested that asymmetric dimethylarginine (ADMA), an endogenous nitric oxide synthase inhibitor, is linked to hypertension and vascular reactivity. Retinal arteriolar narrowing has been observed to associate early with increased risk of hypertension. The objective of this study was to evaluate the role of ADMA as a biomarker for early vascular changes of retinal vessels and thus as a possible biomarker of hypertension risk. Thirty-five healthy white men aged 50.1 years (range, 45-55 years) were studied. Using digitized fundus photography, the following diameters of retinal arterioles and venules were measured 1 disc diameter from the optic disc edge: the mean arteriole width (MAW) and venule width (MVW), the sum of squares of widths of arterioles (SSWA) and venules (SSWV), and the central retinal artery equivalent (CRAE) and venous equivalent (CRVE). Arteriovenous ratio was determined using MAW/MVW, SSWA/SSWV, and CRAE/CRVE. Blood pressure was measured by 24-hour ambulatory recordings and also by resting measurements. Plasma ADMA was determined by a high-performance liquid chromatography tandem mass spectrometry. Plasma ADMA had a strong negative association with MAW, MVW, SSWA, SSWV, CRAE, and CRVE. Arteriovenous ratio measurements did not associate with plasma ADMA or with l-arginine to ADMA ratio, but arteriovenous ratios had a strong association with blood pressure. In a multivariate linear model, plasma ADMA concentration was the most significant predictor of arteriole and venule diameter measurements. These results suggest that plasma ADMA is associated with vascular phenomenon seen in early hypertension and that ADMA may be a potential biomarker candidate for development of hypertension.