RGH-5526 is a novel antihypertensive drug. It causes an increase in hypothalamic norepinephrine (NA) turnover (utilization), and the increase in hypothalamic noradrenergic neuron activity may lead to a decrease in peripheral sympathetic nerve activity, resulting in a significant reduction in blood pressure.

Following prolonged treatment, RGH-5526 does not influence the hypothalamic monoamine oxidase (MAO)-activity. Results show a sharp (61%) decrease the hypothalamic Noradrenaline (NA) level 2 h after the administration of 10 mg/kg of RGH-5526, and this effect lasts for 4 to 6 h. It is shown that RGH-5526 exerts a greater NA lowering effect in the hypothalamus than in the periphery[1].