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: α/β-adrenergic receptor^[1]; 5HT_1B receptor^[2]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

408.00

C₁₅H₂₂ClN₃O₂S₃

68377-91-3

O=C(N)C1=CC=C(S1)C2=CSC(SCC(CNC(C)(C)C)O)=N2.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhou W, et al. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats.PLoS One. 2014 Feb 12;9(2):e88722  [Content Brief]

  [2]. Hiroshi TSUCHIHASHI, et al. Characteristics of 1251-lodocyanopindolol Binding to 8-Adrenergic and Serotonin-1B Receptors of Rat Brain: Selectivity of 19-Adrenergic Agents