Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist that effectively blocks both α- and β-adrenergic receptors, effectively producing antihypertensive and vasodilating effects [1].

Medroxalol (0.1-10 μM; 20 min) shows α- and β-adrenergic receptor antagonism in isolated rabbit aortic strip [1]. Cell Viability Assay [1] Cell Line: Isolated rabbit aortic strip Concentration: 0.1-10 μM Incubation Time: 20 min Result: Showed pA 2 values of 6.09 and 7.73 for α-adrenergic receptors and β-adrenergic receptors, respevtively.

Medroxalol (oral gavage; 12.5-50 mg/kg; once daily; 12 d) treatment shows antihypertensive activity in spontaneously hypertensive rats [1]. Animal Model: Male spontaneously hypertensive rats (SHR) [1] Dosage: 12.5, 25, or 50 mg/kg Administration: Oral gavage; 12.5, 25, or 50 mg/kg; once daily; 12 days Result: Produced a dose-related fall in blood pressure.