Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
性状
Solid
IC50 & Target[1][2]
5-HT1A Receptor
体内研究(In Vivo)
Alprenolol (p.o., 50 mg/kg) causes a significant drop in blood pressure which averages 20 mm Hg (at 3-hr) and an increase in heart rate by 39 beats/min (at 3-hr) in conscious renal hypertensive dogs.
Alprenolol (i.p., 5 mg/kg) effectively blockes the anxiolytic effects of indorenate and ipsapirone but do not reduce the motor activity in adult male Swiss Webster mice.
Alprenolol (intravenous injection, 0.5 or 1.0 mg/kg) can decrease systolic pressure by a mean of 10 mm Hg, diastolic pressure by a mean of 10 mm Hg) and heart rate by 23 beats/min, as well as slightly reduce both myocardial and liver blood flows by mean of 17% and 15% respectively at a dose of 1.0 mg/kg in cats. 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]. Himori N, et al. Effects of beta-adrenoceptor blocking agents, pindolol, alprenolol and practolol on blood pressure and heart rate in conscious renal hypertensive dogs. Arch Int Pharmacodyn Ther. 1977 Jan;225(1):152-65.[2]. Fernández-Guasti A, et al. Evidence for the involvement of the 5-HT1A receptor in the anxiolytic action of indorenate and ipsapirone. Psychopharmacology (Berl). 1990;101(3):354-8.
溶解度数据
In Vitro: DMSO : 100 mg/mL (401.04 mM; Need ultrasonic)H2O : 0.67 mg/mL (2.69 mM; Need ultrasonic)配制储备液