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Bufuralol(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bufuralol(hydrochloride)图片
CAS NO:60398-91-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Bufuralol (hydrochloride) (Ro 3-4787 hydrochloride) 是一种有效的非选择性、口服活性 β-肾上腺素受体拮抗剂,具有部分激动剂活性。
Cas No.60398-91-6
别名丁呋洛尔盐酸盐,Ro 3-4787
化学名α-[[(1,1-dimethylethyl)amino]methyl]-7-ethyl-2-benzofuranmethanol, monohydrochloride
Canonical SMILESCCC1=C(OC(C(O)CNC(C)(C)C)=C2)C2=CC=C1.Cl
分子式C16H23NO2o HCl
分子量297.8
溶解度≤15mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Bufuralol is a non-specific β-adrenergic blocker.

Beta adrenergic agonists are medications relaxing muscles of the airways, which widens the airways and leads to easier breathing. Beta adrenergic agonists are a class of sympathomimetic agents that act upon the beta adrenoceptors.

In vitro: Bufuralol was identified as a non-cardioselective β-adrenoceptor antagonist which possessed partial agonist activity at the β-adrenoceptor. Bufuralol also showed membrane-stabilizing properties [1].

In vivo: Previous pharmacological studies in several species of animals showed that bufuralol exhibited non-selective β-adrenoceptor blocking properties similar to those of propranolol with comparable potency. Such effects were exerted on the β-adrenoceptor stimulant actions of injected amines and of sympathetic nerve stimulation. However, unlike propranolol, bufuralol possessed some instrinsic sympathomimetic activity as demonstrated by tachycardia in reserpinized rats [2].

Clinical trial: Clinical observations were made in eight subjects who exercised before and after the oral administration of placebo, bufuralol and propranolol. Results showed that the exercise heart rate remained constant after placebo. Bufuralol at 7.5 mg and propranolol at 40 mg could reduce exercise heart rate but bufuralol at 15, 30, 60 and 120 mg and propranolol at 160 mg were still active at 24 h. The lowest exercise heart rate occurred at 2 h after treatments. Bufuralol at 60 and 120 mg could produce similar reduction in exercise tachycardia as propranolol at 40 mg but less than propranolol at 160 mg [2].

References:
[1] Fothergill GA, Francis RJ, Hamilton TC, Osbond JM, Parkes MW.  Bufuralol, a new beta-adrenoceptor blocking agent. Experientia. 1975 Nov 15;31(11):1322-3.
[2] Pringle, T. H.,Francis, R.J.,East, P.B., et al. Pharmacodynamic and pharmacokinetic studies on bufuralol in man. Br.J.Clin.Pharmac. 22, 527-534 (1986).