Methacholine chloride
(Synonyms: 醋甲胆碱; Acetyl-β-methylcholine chloride) 目录号 : GC33434
A muscarinic receptor agonist
Cas No.:62-51-1
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
Acetyl-β-methylcholine is a muscarinic (M) receptor agonist.1 In wild-type mice, acetyl-β-methylcholine decreases heart rate and blood pressure and increases the airway pressure time index, a measure of bronchoconstriction, in a dose-dependent manner. Cardiac and pulmonary responses are abolished in M2 and M3 knockout mice, respectively, suggesting that acetyl-β-methylcholine acts on cardiac M2 and pulmonary M3 receptors. Formulations containing acetyl-β-methylcholine have been used to diagnose asthma and to monitor response to asthma therapies.2
1.Fisher, J.T., Vincent, S.G., Gomeza, J., et al.Loss of vagally mediated bradycardia and bronchoconstriction in mice lacking M2 or M3 muscarinic acetylcholine receptorsFASEB J.18(67)711-713(2004) 2.Choi, S.H., Sheen, Y.H., Kim, M.A., et al.Clinical implications of oscillatory lung function during methacholine bronchoprovocation testing of preschool childrenBiomed. Res. Int.20171-9(2017)
| Cas No. | 62-51-1 | SDF | |
| 别名 | 醋甲胆碱; Acetyl-β-methylcholine chloride | ||
| Canonical SMILES | CC(OC(C)=O)C[N+](C)(C)C.[Cl-] | ||
| 分子式 | C8H18ClNO2 | 分子量 | 195.69 |
| 溶解度 | DMSO : ≥ 42 mg/mL (214.63 mM) | 储存条件 | Store at -20°C, stored under nitrogen |
| 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 | 5.1101 mL | 25.5506 mL | 51.1012 mL |
| 5 mM | 1.022 mL | 5.1101 mL | 10.2202 mL |
| 10 mM | 0.511 mL | 2.5551 mL | 5.1101 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。
Stability of Methacholine chloride solutions under different storage conditions over a 9 month period
Eur Respir J 1998 Apr;11(4):946-8.PMID:9623702DOI:10.1183/09031936.98.11040946.
Methacholine chloride solutions, routinely used for testing bronchial hyperreactivity, have been shown to degrade over time. The data published addressing the optimal conditions for Methacholine chloride storage are conflicting and incomplete. This study investigated the effects of a variety of conditions on the stability of Methacholine chloride. Methacholine chloride, dissolved in phosphate buffered saline (PBS) or sodium chloride (NaCl) at 50 and 0.39 g x L(-1), was subjected to various light and temperature conditions for 9 months. Methacholine chloride degradation was determined by high performance liquid chromatography, and all solutions underwent bacterial and pH testing. By 9 months, all 50 g x L(-1) solutions of Methacholine chloride had degraded by 65+/-0.8%. All 0.39 g x L(-1) solutions in NaCl had degraded by 11.0+/-0.33%. The 0.39 g x L(-1) solutions in PBS which had been frozen, refrigerated or stored at room temperature had degraded by 8.0%, 16.0+/-0.3% and 63.8+/-0.5%, respectively. The pH of Methacholine chloride was 7.2 in PBS at 0.39 g x L(-1), 5.8 in PBS at 50 g x L(-1), 3.9 in NaCl at 0.39 and 2.7 in NaCl at 50 g x L(-1). Bacterial contamination was minimal. The results of this study demonstrate that Methacholine chloride is more stable at the higher concentration. However, the pH of the more concentrated solutions of Methacholine chloride in sodium chloride could cause bronchoconstriction in some subjects. We therefore recommend storing Methacholine chloride at 50 g x L(-1) in phosphate-buffered saline.
Stability of Methacholine chloride in isotonic sodium chloride using a capillary electrophoresis assay
J Clin Pharm Ther 1999 Oct;24(5):365-8.PMID:10583699DOI:10.1046/j.1365-2710.1999.00237.x.
Objective: To investigate the stability of Methacholine chloride in 0.9% sodium chloride solutions. Method: Methacholine powder was mixed with diluent to a final concentration of 5 and 10 mg/ml. Duplicates of each admixture were divided and stored in glass vials at 25 degrees C, 4 degrees C and -20 degrees C for 12 months. At appropriate times intervals, samples were removed from solutions and analysed. Methacholine concentrations were measured using a high performance capillary electrophoresis assay. Results: No colour or other visual changes were seen in any sample. However, an additional peak was observed in some samples. Conclusion: Methacholine chloride solutions 5 mg/ml were stable in isotonic sodium chloride after refrigeration or freezing over a period of one year; Methacholine chloride solutions 10 mg/ml were stable for one year after freezing. The solutions stored at ambient temperature were stable for 35 days and for less than 14 days, respectively, for the 5 and the 10 mg/ml solutions.
Stability of stored Methacholine chloride solutions: clinically useful information
Am Rev Respir Dis 1982 Oct;126(4):717-9.PMID:6751179DOI:10.1164/arrd.1982.126.4.717.
Methacholine inhalation challenge (MIC) has been shown to be an extremely useful diagnostic test. Because a decrease in the time and expense involved in the preparation of Methacholine chloride solutions might encourage more laboratories to perform MIC, we assessed the stability of several different concentrations of Methacholine chloride in solution over a period of 4 months. We used and compared 2 different assay techniques: a high pressure liquid chromatography assay and a colorimetric assay. Comparable results were obtained by both assays and demonstrated that methacholine solutions stored either at room temperature or at 4 degrees C showed no significant decomposition over a period of 4 months. From our results, we conclude that: (1) Methacholine chloride solutions are much more stable than stated in the Merck Manual, (2) the original data of MacDonald and coworkers on the stability of Methacholine chloride solution are accurate, (3) our high pressure liquid chromatography method is an accurate and highly specific technique for measuring Methacholine chloride solutions. The major clinical implication of our results is that the time and cost necessary to prepare Methacholine chloride solutions is much less than previously thought. This should encourage a more widespread use of this important diagnostic technique for the demonstration of bronchial hyperreactivity.
Effect of pH on the stability of Methacholine chloride in solution
Respir Med 1998 Mar;92(3):588-92.PMID:9692128DOI:10.1016/s0954-6111(98)90314-6.
Methacholine chloride bronchoprovocation challenges are performed for the diagnosis and investigation of hyperreactive airways. Over the last 20 yrs various formulations and pH values for the preparation of solutions of methacholine have been described. To determine the stability of Methacholine chloride solutions prepared in a variety of buffers with differing pH values and under varying storage temperatures, we measured methacholine concentrations at intervals from 1 to 5 weeks. It was found that Methacholine chloride solutions rapidly decompose if the pH is greater than 6 and that decomposition is more rapid as the pH is raised; solutions at pH 9, i.e. bicarbonate buffer, and stored at 27 degrees C have degradation up to 36% after only one week. Solutions of the same pH but prepared in different buffers can have both varied rates of deterioration and different absolute amounts of methacholine hydrolysed, e.g. solutions prepared in pH 9 borate buffer and stored at 27 degrees C have up to 60% degradation after 1 week. Solutions prepared in saline are stable probably because methacholine solutions are weakly acidic. The results emphasise the importance of preparing Methacholine chloride in the proper buffers for use in the accurate assessment of airway responsiveness.
Measurement of Airway Hyperresponsiveness in Mice
Methods Mol Biol 2022;2506:95-109.PMID:35771466DOI:10.1007/978-1-0716-2364-0_7.
Asthma has been the most prevalent chronic respiratory disease (Mensah et al. J Allergy Clin Immunol 142:744-748, 2018). To explore pathogenic mechanism or new treatments of asthma, mice have been utilized to model the disease. Eosinophilic airway inflammation, allergen specific-IgE, and airway hyperresponsiveness have been characteristic features of allergic asthma (Drake et al. Pulm Ther 5:103-115, 2019). In mouse models, airway hyperresponsiveness to inhaled broncho-constrictor agents such as Methacholine chloride (MCh) has been a key disease marker (Alessandrini et al. Front Immunol 11:575936, 2020). A variety of systems to assess airway reactivity in mice are currently available. Here, three distinct systems are described as these have been used in many publications. In the first system, an invasive system in which mice are anesthetized and intubated followed by mechanical ventilation, lung resistance (R), dynamic compliance (C), and other respiratory parameters with MCh challenge are measured. In the second system, a noninvasive system equipped with a chamber in which mice can move freely and spontaneously breathe, changes in airways with MCh challenge are measured as enhanced pause (Penh) values. In the third system, in vitro airway smooth muscle (ASM) reactivity is monitored in an extracted mouse tracheal duct with a cholinergic agonist challenge or electrical stimulation. Each of these systems has unique features, benefits, or disadvantages.