[CAS NO. 62-51-1] Methacholine chloride
PRODUCTS SPECIFICATIONS [62-51-1]
DESCRIPTION [62-51-1]
Overview
| MDL | MFCD00011817 |
|---|---|
| Molecular Weight | 195.69 |
| Molecular Formula | C8H18ClNO2 |
| SMILES | CC(OC(C)=O)C[N+](C)(C)C.[Cl-] |
1 Publications Citing Use of MCE
Summary
Methacholine (Acetyl-β-methylcholine) choride is a potent muscarinic-3 (M3) agonist. Methacholine choride acts directly on acetylcholine receptors on smooth muscle causing bronchoconstriction and airway narrowing. Methacholine choride shows a high sensitivity to identify bronchial hyperresponsiveness (BHR). Methacholine choride can be used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates [1] [2] [3] [4] .
In Vivo
Methacholine choride (0.5 µg/kg plus 5 µg/kg/min for 30 min) induces bronchoconstriction in dogs
[4]
.
Methacholine choride (0.5 mg/kg; i.v.) induces bronchoconstriction was inhibited by bradykinin (4-40 µg/kg; i.v.) in a a dose-dependent manner in mouse
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 9-week female BALB/c mice [6] |
| Dosage: | 0.03, 0.1, 0.3, 1 mg/kg |
| Administration: | I.v. |
| Result: | Induced severe bronchoconstriction. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04912596 | Intech Biopharm Ltd. |
Mild Asthma
|
August 15, 2022 | Not Applicable |
| NCT02584257 | Lupin, Inc.|Lupin Ltd. |
Mild Persistent Asthma
|
April 2016 | Phase 3 |
| NCT01269528 | Rambam Health Care Campus |
Bronchial Hyperreactivity|Infant, Premature
|
August 2013 | |
| NCT02343419 | Medical University of Warsaw |
Bronchial Hyperreactivity|Abnormal Respiratory Airway Resistance
|
November 2014 | Not Applicable |
| NCT03505489 | University of Saskatchewan |
Asthma
|
June 1, 2018 | Phase 3 |
| NCT01297907 | Rambam Health Care Campus |
Crohn´s Disease
|
May 2008 | |
| NCT01699594 | University of Saskatchewan |
Allergic Asthma
|
October 2012 | Not Applicable |
| NCT00513487 | Novartis |
Allergic Rhinitis
|
July 2007 | Not Applicable |
| NCT02502825 | Guangzhou Institute of Respiratory Disease|Firestone Institute for Respiratory Health |
Asthma
|
July 2015 | Not Applicable |
| NCT02104284 | BL&H Co., Ltd |
Asthma
|
July 2011 | Not Applicable |
| NCT03825302 | Vanderbilt University Medical Center |
Asthma
|
December 1, 2021 | |
| NCT02630511 | University of Alberta |
Asthma
|
December 2015 | Not Applicable |
| NCT00503659 | Johann Wolfgang Goethe University Hospital |
Bronchial Hyperreactivity|Bronchial Asthma
|
February 2007 | Not Applicable |
| NCT01919424 | McMaster University |
Asthma
|
April 2011 | Not Applicable |
| NCT04109534 | Stefan Zielen|Johann Wolfgang Goethe University Hospital |
Allergic Asthma|Allergy to House Dust Mite
|
October 1, 2019 | Not Applicable |
| NCT02230189 | Prescott Woodruff|National Institute of Allergy and Infectious Diseases (NIAID)|University of California, San Francisco |
Asthma
|
March 2015 | Phase 2 |
| NCT05292976 | Aurobindo Pharma Ltd |
Bronchial Asthma
|
April 2022 | Phase 3 |
| NCT04001465 | University of Saskatchewan |
Airway Hyper Responsiveness
|
May 14, 2019 | Not Applicable |
| NCT01907334 | University of Florida|Teva Branded Pharmaceutical Products R&D, Inc. |
Asthma
|
August 2013 | Phase 4 |
| NCT02263976 | Boehringer Ingelheim |
Healthy
|
August 2003 | Phase 1 |
| NCT01642745 | University of Saskatchewan |
Asthma
|
November 2011 | Phase 4 |
| NCT01144910 | Johann Wolfgang Goethe University Hospital |
Intrinsic Asthma|Allergic Asthma|Allergy|Bronchial Hyperresponsiveness
|
May 2011 | |
| NCT01847768 | National Institute of Allergy and Infectious Diseases (NIAID)|Asthma and Allergic Diseases Cooperative Research Centers |
Asthma
|
April 2013 | Not Applicable |
| NCT00673621 | Mannkind Corporation |
Asthma|Diabetes Mellitus
|
May 2008 | Phase 1 |
| NCT02574975 | Zhujiang Hospital |
Asthma
|
April 2015 | Phase 4 |
| NCT03105843 | Dr. Diane Lougheed|Queen´s University |
Asthma|Cough|Cough Variant Asthma
|
March 1, 2022 | Phase 4 |
| NCT02410096 | Johann Wolfgang Goethe University Hospital |
Exercise-induced Asthma
|
April 2015 | Not Applicable |
| NCT01777867 | Mayo Clinic|University of Manchester |
Gastroesophageal Reflux Disease|Chronic Cough|Broncho-hyperreactivity
|
December 2012 | |
| NCT02975258 | University of Pittsburgh|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI) |
Asthma|HIV|Adiposity
|
September 2015 | |
| NCT01578824 | Rambam Health Care Campus |
Asthma|Vitamin D Resistant Rickets
|
March 2011 | Not Applicable |
| NCT00145990 | University of Florida|GlaxoSmithKline |
Asthma
|
September 2005 | Not Applicable |
| NCT00500253 | Medical University of Lodz |
Asthma
|
February 2007 | Phase 4 |
| NCT00890539 | University of Saskatchewan |
Asthma
|
February 2009 | Not Applicable |
| NCT01547286 | Massachusetts General Hospital|National Heart, Lung, and Blood Institute (NHLBI) |
Asthma|Atopy
|
May 2012 | Not Applicable |
| NCT02100267 | Sanwa Kagaku Kenkyusho Co., Ltd. |
Asthma
|
April 2014 | Phase 3 |
| NCT02026492 | Johann Wolfgang Goethe University Hospital |
Exercise-induced Asthma
|
June 2013 | Not Applicable |
| NCT00906867 | Johann Wolfgang Goethe University Hospital |
Dyspnea
|
April 2009 | |
| NCT03062904 | Assistance Publique - Hôpitaux de Paris |
Paradoxical Fall in Maximum Expiratory Flows
|
February 2014 | Not Applicable |
| NCT01064245 | Dr. Diane Lougheed|The Ontario Thoracic Society of the Ontario Lung Association|Queen´s University (William M Spear + Start Memorial Fund)|Queen´s University |
Asthma|Cough Variant Asthma
|
February 1, 2010 | Not Applicable |
| NCT01449435 | Johann Wolfgang Goethe University Hospital |
Asthma
|
August 2011 | |
| NCT02097537 | Santen Pharmaceutical Co., Ltd. |
Asthma
|
February 2014 | Phase 3 |
| NCT01659476 | Queen´s University |
Asthma|Cough
|
October 2012 | Not Applicable |
| NCT00252291 | Pharmaxis |
Asthma
|
November 2005 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 511.01 mM ; Need ultrasonic)
H 2 O : 100 mg/mL ( 511.01 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.1101 mL | 25.5506 mL | 51.1012 mL |
| 5 mM | 1.0220 mL | 5.1101 mL | 10.2202 mL |
| 10 mM | 0.5110 mL | 2.5551 mL | 5.1101 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 130 mg/mL (664.32 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (12.78 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (12.78 mM); Clear solution
References
- [1] Cohen J, et al. Relationship between airway responsiveness to neurokinin A and methacholine in asthma. Pulm Pharmacol Ther. 2005;18(3):171-176.
- [2] Anderson SD, et al. Comparison of mannitol and methacholine to predict exercise-induced bronchoconstriction and a clinical diagnosis of asthma. Respir Res. 2009;10(1):4. Published 2009 Jan 23.
- [3] Cockcroft DW. Methacholine challenge methods. Chest. 2008;134(4):678-680.
- [4] Kabara S, et al. Differential effects of thiopental on methacholine- and serotonin-induced bronchoconstriction in dogs. Br J Anaesth. 2003 Sep;91(3):379-84.
- [5] Folkerts G, et al. Bradykinin causes inhibition of methacholine-induced bronchoconstriction in vivo in mice. Naunyn Schmiedebergs Arch Pharmacol. 2001 Jul;364(1):53-8.
- [6] Vitorasso RL, et al. Methacholine dose response curve and acceptability criteria of respiratory mechanics modeling. Exp Lung Res. 2020 Feb-Mar;46(1-2):23-31.
Synonyms
