Arotinolol shows its selectivity of β-adrenergic receptors, the result of Arotinolol for β1 and β2 adrenoceptors in ¹²⁵ I-ICYP binding to rat cerebral cortical membranes with pK _i value of 9.74 and 9.26 respectively. The selectively of β1 and β2 is equal. Arotinolol shows its potency for inhibiting the binding of the same radioligand to 5HT1B-serotonergic receptor site, Arotinolol displaces ¹²⁵ I-ICYP binding to 5HT1B-receptors with the pK _i values of 7.97 and 8.16 resepectively for β1 and β2 adrenergic receptors.

Arotinolol (oral gavage; 200 mg/kg; 8 weeks) can significantly decrease central arterial pressure (CAP) and pulse wave velocity (PWV), in addition, it reduces aortic collagen depositions and finally improves arterial stiffness in SHR mouse.