Fenoterol (hydrobromide)
(Synonyms: 非诺特罗氢溴酸盐; Th-1165a; Phenoterol hydrobromide) 目录号 : GC43661
An Analytical Reference Standard
Cas No.:1944-12-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fenoterol is an analytical reference standard categorized as a β2-adrenergic receptor agonist. β2-adrenergic receptor agonists, including fenoterol, have been used as performance-enhancing drugs in sports doping and are banned by the World Anti-Doping Agency (WADA). This product is intended for research and forensic applications.
| Cas No. | 1944-12-3 | SDF | |
| 别名 | 非诺特罗氢溴酸盐; Th-1165a; Phenoterol hydrobromide | ||
| Canonical SMILES | OC(CNC(C)CC1=CC=C(O)C=C1)C2=CC(O)=CC(O)=C2.Br | ||
| 分子式 | C17H21NO4•HBr | 分子量 | 384.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 5 mg.ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6021 mL | 13.0107 mL | 26.0213 mL |
| 5 mM | 0.5204 mL | 2.6021 mL | 5.2043 mL |
| 10 mM | 0.2602 mL | 1.3011 mL | 2.6021 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
A review of ipratropium bromide/Fenoterol hydrobromide (Berodual) delivered via Respimat Soft Mist Inhaler in patients with asthma and chronic obstructive pulmonary disease
Drugs 2004;64(15):1671-82.PMID:15257628DOI:10.2165/00003495-200464150-00005.
Asthma and chronic obstructive pulmonary disease (COPD) can be effectively treated by the use of bronchodilator therapies delivered by inhalation. Berodual is a fixed combination of the anticholinergic agent ipratropium bromide (IB) and the beta2-adrenergic agonist Fenoterol hydrobromide (FEN). IB/FEN has been available for the treatment of asthma and COPD in a pressurised metered dose inhaler (MDI) [pMDI] formulation for many years. The pMDI is the most widely used device for the delivery of inhaled medications, such as IB/FEN. However, most conventional pMDIs contain chlorofluorocarbon (CFC) propellants, which are currently being withdrawn because of their detrimental effects on the environment. This has resulted in alternative methods of drug delivery being developed. Respimat Soft Mist Inhaler (SMI) is a new generation, propellant-free inhaler that generates a fine, slow-moving cloud (the Soft Mist) which can be easily inhaled. Scintigraphic studies have shown that this improves deposition of drugs in the lung and results in less oropharyngeal deposition than the CFC-MDI. A clinical development programme has been conducted to compare the efficacy and safety of IB/FEN delivered via Respimat SMI with that of IB/FEN via CFC-MDI in the treatment of patients with asthma or COPD. Five clinical studies (two phase II and three phase III) investigated dosages of IB/FEN 5/12.5 microg to 320/800 microg via Respimat SMI in single and multiple dose administration regimens. Four of the trials were conducted in patients with asthma (three in adults and one in children), while one phase III trial was conducted in patients with COPD. In phase III, 2058 patients participated, with a total of 1112 patients treated with IB/FEN via Respimat SMI. In the phase III studies, each dose from Respimat SMI was given in one actuation compared with two actuations with the CFC-MDI. In the paediatric asthma phase III study, all CFC-MDI doses were delivered via a spacer device. The results of the trials demonstrated that IB/FEN via Respimat SMI allows a reduction in the nominal dose of IB/FEN, while offering similar therapeutic efficacy and safety to a CFC-MDI. In children, Respimat SMI obviates the need for a spacer.
Fenoterol hydrobromide delivered via HFA-MDI or CFC-MDI in patients with asthma: a safety and efficacy comparison
Respir Med 2000 Oct;94(10):948-53.PMID:11059947DOI:10.1053/rmed.2000.0864.
The main objective of the study was to compare the long-term safety and tolerability of Fenoterol hydrobromide delivered using a metered-dose inhaler formulated with the alternative propellant, hydrofluoroalkane 134a (HFA-MDI), with delivery using the currently available chlorofluorocarbon MDI (CFC-MDI; Berotec 100). A further objective was to compare the efficacy of Fenoterol HFA-MDI with Fenoterol CFC-MDI, using the pulmonary function parameters of forced expiratory volume in 1 sec (FEV1), forced vital capacity (FVC) and peak expiratory flow (PEF). Following a 2-week run-in phase, a 12-week, double-blind parallel group comparison was undertaken in 290 patients randomized on a 2:1 basis to two puffs of 100 microg Fenoterol four times a day (HFA-MDI=197 patients; CFC-MDI=93 patients). A total of 236 patients in this multi-centre study completed the trial as planned. The overall incidence of adverse events (AEs) was similar in both groups (29.9% of HFA-MDI patients and 28% of CFC-MDI patients). Reports of respiratory disorder AEs were also comparable (21.8% HFA-MDI; 22.6% CFCMDI). End of study laboratory tests, ECG, pulse, blood pressure and physical examination showed no significant differences from pre-study baselines in either group and both treatments appeared to be well tolerated. Pre-dose FEV1 measurements taken at the three clinic visits were constant and increase in FEV1 at 5 and 30 min post-dose demonstrated equivalent efficacy for the two formulations. No difference between the two groups was observed in PEF or in the use of rescue medication. We conclude from these findings that the long-term safety and efficacy profile of Fenoterol HFA-MDI is comparable to that of the Fenoterol CFC-MDI.
Validation of Fenoterol to Study β2-Adrenoceptor Function in the Rat Urinary Bladder
Pharmacology 2022;107(1-2):116-121.PMID:34781292DOI:10.1159/000519720.
Fenoterol is a β2-adrenoceptor (AR)-selective agonist that is commonly used to investigate relaxation responses mediated by β2-AR in smooth muscle preparations. Some data have questioned this because Fenoterol had low potency in the rat urinary bladder when a muscarinic agonist was used as a pre-contraction agent and because some investigators proposed that Fenoterol may act in part via β3-AR. We designed the present study to investigate whether Fenoterol is a proper pharmacological tool to study β2-AR-mediated relaxation responses in the rat urinary bladder. Firstly, we have compared the effect of pre-contraction agents on Fenoterol potency and found that Fenoterol potency was about 1.5 log units greater against KCl than carbachol (pEC50 7.19 ± 0.66 and 5.62 ± 1.09 of KCl and of carbachol, respectively). To test the selectivity of Fenoterol, we have determined the effects of the β2-AR antagonist ICI 118,551 and the β3-AR antagonist L 748,337 on relaxation responses to Fenoterol. While 300 nM L 748,337 had little effect on the potency of Fenoterol (pEC50 6.56 ± 0.25 and 6.33 ± 0.61 in the absence and presence of L 748,337, respectively), the relaxation curve for Fenoterol was right-shifted in the presence 300 nM ICI 118,551 (pEC50 5.03 ± 0.18). Thus, we conclude that Fenoterol is a proper pharmacological tool to assess β2-AR-mediated responses in the rat urinary bladder and most likely in other smooth-muscle preparations containing multiple subtypes of the β-AR.
Aerosol administration of Fenoterol hydrobromide (Th 1165a) in subjects with reversible obstructive airway disease
Chest 1977 Dec;72(6):731-6.PMID:336306DOI:10.1378/chest.72.6.731.
Bronchodilatory and side effects of Fenoterol hydrobromide (Th1165a; hydroxyphenylorciprenaline; Berotec) and isoproterenol given by inhalation were compared in a double-blind crossover study involving 20 volunteer subjects with reversible obstructive disease of the airways. Subjects inhaled medications from aerosol canisters containing Fenoterol hydrobromide (0.1 mg, 0.2 mg, or 0.4 mg) or isoproterenol (0.15 mg) or an inert placebo propellant in a random sequence of five testing days. All active drugs substantially increased the forced expiratory volume in one second, the mean forced expiratory flow during the middle half of the forced vital capacity, and the specific conductance. The onset of bronchodilation after both Fenoterol and isoproterenol was rapid, but the effect from Fenoterol lasted much longer, up to eight hours. None of the medications cuased significant tachycardia or hypertension. After inhalation of 0.1 mg of Fenoterol hydrobromide, none of the subjects reported nervousness, headache, tremor, or nausea, incontrast with results reported for isoproterenol, higher aerosol doses fo Fenoterol, or oral administration of Fenoterol. No additional therapeutic benefit was found in the administration of higher doses of Fenoterol.
Fenoterol: a review of its pharmacological properties and therapeutic efficacy in asthma
Drugs 1978 Jan;15(1):3-32.PMID:342228DOI:10.2165/00003495-197815010-00002.
Fenoterol, the 4-hydroxyphenyl derivative of orciprenaline, is a resorcinol derivative with relatively high selectivity for beta2-adrenoceptors. It is active in man after inhalation or oral administration and is indicated in the treatment of bronchospasm associated with asthma, bronchitis and other obstructive airway diseases. Clinical experience has shown that Fenoterol is an effective bronchodilator with negligible effects on the cardiovascular system following aerosol administration of usual therapeutic doses. In children, inhaled Fenoterol is effective in preventing exercise-induced asthma and administration of the aerosol in young children has been successfully used to terminate acute asthma attacks. In trials in adults, inhaled Fenoterol was superior to placebo. In other controlled studies, it showed a tendency to cause a slightly greater maximum improvement in airway function as assessed spirometrically, and to have a longer duration of action than inhaled orciprenaline, salbutamol or terbutaline, although in these trials statistically significant differences were often not found. The onset of maximum effect is less rapid than with isoprenaline but is longer lasting. About 60% of the eventual maximum response to Fenoterol is reached in the first few minutes after inhalation. Oral Fenoterol is more effective than placebo, ephedrine or orciprenaline, and probably similar to salbutamol and terbutaline. Following usual aerosol doses, side-effects are minimal. Oral administration is associated with a higher incidence of side-effects than inhalation, including fine muscle tremor and tachycardia.