Oxitropium Bromide
(Synonyms: 氧托溴铵) 目录号 : GC32049
Oxitropiumbromide是毒蕈碱受体拮抗剂。它是一种用于治疗哮喘和慢性阻塞性肺疾病的抗胆碱能支气管扩张剂药物。
Cas No.:30286-75-0
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
Animal experiment: | Mice: In the oxitropium bromide inhalation group, animals are given 2 puffs of inhalation from a oxitropium bromide MDI (metered dose inhaler) via a 75-mL spacer, and then diaphragm muscles are dissected and measured as to contractility immediately, 1 hour, 2 hours and 4 hours later (n=5 animals each). An animal is placed in a centrifugal tube (inner diameter=30 mm) with a round hole (diameter=10 mm) in the bottom, its nose and mouth being exposed through the hole to breath. An oxitropium bromide MDI (metered dose inhaler) releases 2 puffs into a spacer attached to the tube. Aerosols of oxitropium bromide are inhaled for about 10 seconds, while the animal is breathing spontaneously through the hole of the tube[1]. |
References: [1]. Shindoh C, et al. Effects of inhalation or incubation of oxitropium bromide on diaphragm muscle contractility in mice. Allergol Int. 2011 Sep;60(3):365-72. | |
Oxitropium bromide is an mAChR antagonist used as an anticholinergic bronchodilator drug for the treatment of asthma and chronic obstructive pulmonary disease.
Oxitropium bromide is a muscarinic antagonist which blocks musucarinic acetylcholine receptors (mAChR). Incubation with oxitropium bromide of untreated diaphragm muscle and diaphragm muscle injected with endotoxin does not increase the force-frequency curves dose-dependently in vitro; however, it causes both types of muscle to be fatigue resistant[1].
Oxitropium bromide inhalation shifts force-frequency curves upward at 2 h after inhalation and inhibits the decrease of force-frequency curves due to endotoxin injection in vivo[1]. Oxitropium bromide strongly and persistently inhibits the acetylcholine (ACh)-induced resistance. The increase in resistance induced by histamine, serotonin, leukotriene D4 or antigen is prevented by oxitropium bromide oxitropium bromide[2]. Inhalation of the anticholinergic agent oxitropium bromide at doses of 1.5 μg and higher greatly attenuates the decrease in mucus score produced by intravenous histamine but not by inhaled histamine[3].
[1]. Shindoh C, et al. Effects of inhalation or incubation of oxitropium bromide on diaphragm muscle contractility in mice. Allergol Int. 2011 Sep;60(3):365-72. [2]. Kohno SW, et al. Effect of oxitropium bromide (Ba253) on increased airway resistance induced by various agonists and antigen in the guinea pig. Jpn J Pharmacol. 1989 Aug;50(4):455-66. [3]. Takeyama K, et al. Effect of oxitropium bromide on histamine-induced airway goblet cell secretion. Am J Respir Crit Care Med. 1996 Jul;154(1):231-6.
| Cas No. | 30286-75-0 | SDF | |
| 别名 | 氧托溴铵 | ||
| Canonical SMILES | CC[N@@+]1([C@H]2[C@@H](O3)[C@@H]3[C@@H]1C[C@H](OC([C@@H](C4=CC=CC=C4)CO)=O)C2)C.[Br-] | ||
| 分子式 | C19H26BrNO4 | 分子量 | 412.32 |
| 溶解度 | Soluble in DMSO | 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 | 2.4253 mL | 12.1265 mL | 24.253 mL |
| 5 mM | 0.4851 mL | 2.4253 mL | 4.8506 mL |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4253 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。
Synthesis and characterization of Oxitropium Bromide related substances and novel stability indicating HPLC methods
J Pharm Biomed Anal 2020 May 10;183:113145.PMID:32058292DOI:10.1016/j.jpba.2020.113145.
The European Pharmacopoeia (Ph. Eur.) described two separate HPLC methods for determination of organic impurities in Oxitropium Bromide, a synthetic anticholinergic agent used by inhalation in the treatment of asthma and other bronchial disorders, and a potentiometric titration assay method which is not a stability indicating method. During synthetic process development and analytical studies of oxitropium; besides known Ph. Eur.-impurities new process related and degradation impurities were determined, identified by LC-MS, synthesized, characterized, and then used in development and validation studies of oxitropium analytical methods. As a result of these studies, a single HPLC related substances method was developed and validated according to international conference on harmonisation (ICH) guidelines for determination of all oxitropium related substances by using an inertsil ODS-4 (250 mm × 4.6 mm, 5 μm) column at 15 °C with 50 μL injection volume at a wavelength of 210 nm with gradient elution of phosphate-buffer/acetonitrile mixture flowing at a rate of 1.2 mL/min during 60 min. Also, a stability indicating HPLC assay method was developed and validated by using an XBridge C18 (150 mm × 4.6 mm, 3.5 μm) column at 25 °C with 10 μL injection volume at a wavelength of 210 nm and with phosphate-buffer/acetonitrile (85/15) mixture flowing at a rate of 1.0 mL/min during 10 min. Stress-testing and stability studies of Oxitropium Bromide was carried out and samples were analyzed by using newly developed stability-indicating HPLC assay and related substances methods.
Oxitropium Bromide, ipratropium bromide and fenoterol in exercise-induced asthma
Respiration 1982;43(1):57-63.PMID:6211753DOI:10.1159/000194464.
Oxitropium Bromide (Ba 253) is a new inhaled bronchodilating agent with anticholinergic properties. The effect of this compound (100 micrograms) was compared to that of ipratropium bromide (40 micrograms), the beta 2-receptor stimulant fenoterol (400 micrograms) and placebo in 8 patients with exercise-induced asthma. The drugs were administered by metered dose inhalers, after which exercise test were performed on ergometer cycles at the times of the drugs' maximal effects. Forced expiratory volume during 1 S and vital capacity were recorded basally, repeatedly during 20 min after exercise and following the inhalation of isoprenaline (160 micrograms) which was given 20 min after exercise. Fenoterol possessed a very good protective effect against exercise-induced bronchoconstriction in all patients, whereas the other drugs differed very little from placebo. Thus, only 4 patients did benefit from ipratropium bromide, 1 patient from Oxitropium Bromide and 2 patients from placebo. No side effect occurred. In the doses used the two anticholinergic agents ipratropium bromide and Oxitropium Bromide were less effective than a beta 2-adrenoreceptor stimulant like fenoterol in protecting against exercise-induced asthma.
Effects of inhalation or incubation of Oxitropium Bromide on diaphragm muscle contractility in mice
Allergol Int 2011 Sep;60(3):365-72.PMID:21593578DOI:10.2332/allergolint.10-OA-0266.
Background: Although Oxitropium Bromide is used clinically as an anticholinergic drug (i.e., parasympathetic antagonist) to relax airway smooth muscle, we examined whether it has or does not have any effects on diaphragm muscle. Methods: Three treatment sets, an Oxitropium Bromide inhalation only group, an Oxitropium Bromide inhalation plus endotoxin injection group (in vivo) and an Oxitropium Bromide incubation group (in vitro) were studied as to diaphragm muscle contractile properties. Results: Oxitropium Bromide inhalation shifted force-frequency curves upward at 2 h after inhalation (p < 0.05) and inhibited the decrease of force-frequency curves due to endotoxin injection in vivo. Incubation with Oxitropium Bromide of untreated diaphragm muscle and diaphragm muscle injected with endotoxin did not increase the force-frequency curves dose-dependently in vitro; however, it caused both types of muscle to be fatigue resistant. Conclusions: We speculate that the increment of muscle contractility with the inhalation of Oxitropium Bromide was induced by the antagonization of musucarinic acetylcholine receptors (mAChR). In addition, the changes of fatigue resistance provoked by Oxitropium Bromide, which also is speculated to antagonize mAChR, may be beneficial in the treatment of patients with COPD.
Oxitropium Bromide improves exercise performance in patients with COPD
Chest 1994 Dec;106(6):1740-5.PMID:7988193DOI:10.1378/chest.106.6.1740.
Inhaled anticholinergics may be the first-line therapy for stable COPD. However, the effect of inhaled anticholinergic agents on exercise capacity is still controversial. Fourteen patients with stable COPD (age, 64.6 +/- 5.9 years) completed a randomized, double-blind placebo-controlled crossover trial. All the patients were studied by symptom-limited progressive cycle ergometry before and 90 min after the inhalation of either Oxitropium Bromide, 800 micrograms, or an identical placebo. Spirometry was assessed before and after each exercise test. While FEV1 averaged 0.85 +/- 0.34 L at 90 min after the inhalation of placebo, FEV1 was 1.01 +/- 0.41 L at 90 min after the inhalation of oxitropium, 800 micrograms (significant from placebo, p < 0.001). The maximal workload of 94.0 +/- 25.8 W after oxitropium administration was significantly greater than the 87.6 +/- 24.7 W measured after placebo (p < 0.01). The maximal minute ventilation was 40.2 +/- 12.3 L/min after oxitropium inhalation and 36.8 +/- 10.5 after placebo inhalation (p < 0.05). The differences in maximal oxygen consumption, maximal carbon dioxide production, and maximal heart rate between oxitropium and placebo inhalation also were statistically significant (p < 0.05, p < 0.05, and p < 0.01, respectively). There was a significant correlation between the change in maximal workload and the change in FEV1 before and after inhalation (r = 0.625, p < 0.01). The inhalation of Oxitropium Bromide, 800 micrograms, can improve the exercise capacity of patients with stable COPD. It is suggested that the effect is due to the bronchodilation induced by this drug.
Oxitropium Bromide. Dose-response and time-response study of a new anticholinergic bronchodilator drug
Chest 1986 Feb;89(2):249-53.PMID:3510822DOI:10.1378/chest.89.2.249.
The efficacy and side effects of Oxitropium Bromide, a new anticholinergic bronchodilator drug, were tested in a double-blind placebo-control study. Twenty-four men, aged 58 to 72 years, with chronic partially reversible obstruction of the airways were used as subjects. Three doses of oxitropium were tested (100 micrograms, 200 micrograms, and 300 micrograms) to determine the optimum dose by metered-dose inhaler. A comparison was also made between oxitropium, fenoterol (400 micrograms), and a combination of oxitropium (200 micrograms) and fenoterol (400 micrograms). Fenoterol produced a greater degree of maximal bronchodilatation than each of the three doses of oxitropium, and its effect was more rapid in onset (30 vs 120 minutes to peak effect); however, the duration of action of oxitropium was greater than that of fenoterol (ie, the forced expiratory volume in one second [FEV1] remained within 5 percent of peak FEV1 for three hours, compared to one hour). Oxitropium in the 100 micrograms dose was inferior to 200 micrograms and 300 micrograms in subjective efficacy scores, peak percent change in FEV1, forced vital capacity, (FVC), mean forced expiratory flow over the middle half of the FVC, and duration of action; there was no difference between 200 micrograms and 300 micrograms. The oxitropium-fenoterol combination had a rapid onset of action, and a greater peak effect was achieved than for oxitropium alone. The main unwanted effect was a mildly unpleasant taste. Anticholinergic effects were not seen in this group of elderly men. Oxitropium Bromide therefore is an effective bronchodilator with slow onset but prolonged activity and few side effects when used in patients with moderately severe obstruction of the airways. An appropriate dose appears to be 200 micrograms. Addition of oxitropium to fenoterol appears to offer even greater efficacy.