Guanabenz Acetate (Wytensin) is a specific agonist of adrenergic receptor. The pEC50 for α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor is 8.25, 7.01 and ~5, respectively.

α2B-adrenoceptor:7.01(pEC50), α2C-adrenoceptor:<5(pEC50), α2A-adrenoceptor:8.25(pEC50)

Guanabenz inhibits the response of vascular contractions in various processes and initiates normal sympathetic nerve discharge, while also antagonizing the stimulation of the sympathetic nervous system. Administering 0.5 mg/kg of Guanabenz intravenously in anesthetized hypertensive rats and dogs leads to a reduction in blood pressure and heart rate. Moreover, an intravenous injection of 0.1 mg/kg Guanabenz in anesthetized dogs initially causes an increase in blood pressure due to the action of the sympathetic nervous system, followed by a decrease in cardiac output, contractility, and heart rate.

In mammalian MovS6 cells, 10 μM of Guanabenz facilitates the complete clearance of PrPSc. Additionally, in HEK293 cells transfected with rat inducible nitric oxide synthase (nNOS), 30 μM Guanabenz induces a time-dependent reduction in nNOS activity, with a Ki value of 1 μM. In HEK 293 cells, treatment with 50 μM Guanabenz for 3 hours results in approximately a 75% decrease in the accumulation of nitrites and nitrates within the cells. Furthermore, treatment with 100 μM Guanabenz for 24 hours leads to about a 35% reduction in the quantity of inducible nitric oxide synthase protein detected by immunological methods.