Bufuralol (hydrochloride) (Synonyms: Ro 3-4787) |
| Catalog No.GC15347 |
Bufuralol(염산염)(Ro 3-4787 염산염)은 부분 작용제 활성을 갖는 강력한 비선택적 경구 활성 β-아드레날린 수용체 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 60398-91-6
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 60398-91-6 | SDF | |
| Synonyms | Ro 3-4787 | ||
| Chemical Name | α-[[(1,1-dimethylethyl)amino]methyl]-7-ethyl-2-benzofuranmethanol, monohydrochloride | ||
| Canonical SMILES | CCC1=C(OC(C(O)CNC(C)(C)C)=C2)C2=CC=C1.Cl | ||
| Formula | C16H24ClNO2 | M.Wt | 297.82 |
| Solubility | ≤15mg/ml in ethanol;10mg/ml in DMSO;15mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3577 mL | 16.7887 mL | 33.5773 mL |
| 5 mM | 0.6715 mL | 3.3577 mL | 6.7155 mL |
| 10 mM | 0.3358 mL | 1.6789 mL | 3.3577 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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