Arotinolol (hydrochloride)

Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker^[1]. Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites^[2]. Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases^[1]. IC50 & Target:IC50: α/β-adrenergic receptor^[1]; 5HT_1B receptor^[2] In Vitro:Arotinolol hydrochloride shows its selectivity of β-adrenergic receptors, the result of Arotinolol for β1 and β2 adrenoceptors in ¹²⁵I-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^[2].
Arotinolol hydrochloride shows its potency for inhibiting the binding of the same radioligand to 5HT1B-serotonergic receptor site, Arotinolol hydrochloride displaces ¹²⁵I-ICYP binding to 5HT1B-receptors with the pK_i values of 7.97 and 8.16 resepectively for β1 and β2 adrenergic receptors^[2].
In Vivo:Arotinolol hydrochloride (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^[1].