Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity.
性状
Solid
IC50 & Target[1][2]
β-adrenoceptor
体外研究(In Vitro)
Bupranolol (1~3 μM) shifts isoprenaline-induced relaxation in the presence of 30 μM propranolol. Bupranolol acts as a competitive antagonist of isoprenaline-induced relaxation in the presence of 300 nM propranolol, with a pA2 value of 5.90. Bupranolol antagonizes β1- and β2-ARs with pA2 values of ≈9.0, and also antagonizes β3-AR with a pA2 value of 6.0. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Chino D, et al. Pharmacological identification of β-adrenoceptor subtypes mediating isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle. J Smooth Muscle Res. 2018;54(0):13-27.[2]. Babu RJ, et al. Effect of cyclodextrins on the complexation and transdermal delivery of bupranolol through rat skin. Int J Pharm. 2004;271(1-2):155-165.
溶解度数据
In Vitro: DMSO : 50 mg/mL (183.97 mM; ultrasonic and warming and heat to 60°C)配制储备液