SummaryAlthough there is considerable evidence that the acute administration of peripheral presynaptic dopamine [dopamine-2 (02)] receptor agonists inhibits the sympathetic neuronal release of noradrenaline (norepinephrine) and decreases arterial blood pressure (BP), their effects on the sympathetic system and on cardiovascular function after long term treatment in patients with hypertension are not known. 12 patients with essential hypertension received a selective 02 receptor agonist, dihydroergotoxine 9 to 13.5 mg/day orally for I year after a preliminary single-blind placebo period of 4 weeks. Oihydroergotoxine reduced systolic and diastolic BP, heart rate and plasma noradrenaline levels, and these effects persisted for up to 1 year. The fall in BP significantly correlated with the decrease in circulating noradrenaline levels during treatment (p < 0.01).Oihydroergotoxine did not inhibit the physiological rise in plasma noradrenaline levels induced by standing and was not associated with orthostatic hypotension. The development of tolerance to dihydroergotoxine was not observed, and coupled with the lack of adverse effects, suggests 02 receptor agonists may be clinically useful in the long term treatment of essential hypertension.