Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR).
Amosulalol (3-30 mg/kg; p.o.; single dose) reduces acute systolic blood pressure in hypertensive rats[1].
Amosulalol (50 mg/kg; p.o.; twice daily for 12 weeks) produces an intolerant antihypertensive effect and also reduces central rate and increases PRA in hypertensive rat models[1].
References:
[1]. Honda K, et al. Autonomic and antihypertensive activity of oral amosulalol (YM-09538), a combined alpha- and beta-adrenoceptor blocking agent in conscious rats. Jpn J Pharmacol. 1985 May;38(1):31-41.