规格: | 98% |
分子量: | 271.78 |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
Background:
Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity[1].
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[1].
[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.