Bioactivity | 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 5HT1B-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]. |
Target | IC50: α/β-adrenergic receptor; 5HT1B receptor |
Invitro | 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 pKi 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 pKi values of 7.97 and 8.16 resepectively for β1 and β2 adrenergic receptors[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Arotinolol hydrochloride 相关抗体: |
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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 68377-91-3 |
Formula | C15H22ClN3O2S3 |
Molar Mass | 408.00 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhou W, et al. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats.PLoS One. 2014 Feb 12;9(2):e88722 [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 |