Identification
- Summary
Methacholine is a parasympathomimetic bronchoconstrictor used to diagnose bronchial hyperreactivity in subjects who do not have clinically apparent asthma.
- Brand Names
- Provocholine
- Generic Name
- Methacholine
- DrugBank Accession Number
- DB06709
- Background
Asthma is a complex condition associated with phenomena such as airway hyperresponsiveness (AHR), in which the smooth muscle in the airways (ASM) excessively contracts in response to stimuli, reducing pulmonary function and causing symptoms such as difficulty breathing.1,2 Although the underlying pathology of AHR is complex, ASM contraction can be stimulated by cholinergic agonists that activate M3 muscarinic receptors that stimulate ASM contraction.2,4,8 Methacholine is a non-specific cholinergic agonist (parasympathomimetic) that acts through muscarinic receptors in the lungs to induce bronchoconstriction.11 In patients with AHR, a lower dose of methacholine is required to induce bronchoconstriction, which forms the basis for the methacholine challenge test to diagnose AHR.10,11
Methacholine was granted FDA approval on October 31, 1986, and is marketed under the trademark PROVOCHOLINE® by Methapharm Inc.11
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Methacholine (DB06709)
- Weight
- Average: 160.234
Monoisotopic: 160.133753825 - Chemical Formula
- C8H18NO2
- Synonyms
- Acetyl-beta-methylcholine
- Acetylmethylcholine
- beta-Methylacetylcholine
- MCh
- Methacholine
- Methacholinum
Pharmacology
- Indication
Methacholine is indicated in adult and pediatric patients aged five years and older without clinically apparent asthma for the diagnosis of bronchial airway hyperactivity via the methacholine challenge test.11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Bronchial airway hyperreactivity •••••••••••• ••••••• ••••••• ••• ••••••••• •••••••• - Contraindications & Blackbox Warnings
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Methacholine is a non-specific cholinergic agonist (parasympathomimetic) that acts through muscarinic receptors in the lungs to induce bronchoconstriction, which is more significant in patients with asthma than those without. Therefore, methacholine carries a risk of severe bronchoconstriction, especially in patients with pre-existing reduced pulmonary function (typically baseline FEV1 < 60% or < 1.5 L, at least in adults), clinically apparent asthma or wheezing, or other health conditions such as uncontrolled hypertension, aortic aneurysm, or history of myocardial infarction or stroke. Use in patients with epilepsy, vagotonia, peptic ulcer disease, thyroid disease, urinary tract obstruction or other conditions that could be adversely affected by a cholinergic agent is not recommended. Also, there is a potential risk to healthcare workers administering the methacholine challenge test; proper precautions and protective equipment should be used as needed.11
- Mechanism of action
Asthma is a complicated condition associated with airway remodelling, including the proliferation of airway smooth muscle (ASM) and altered extracellular matrix, aberrant pro-inflammatory immune responses, and excessive ASM contraction leading to decreased lung function.1,2 Excessive ASM contraction in response to contractile agonists, a phenomenon termed airway hyperresponsiveness (AHR), is a physical manifestation of the altered pulmonary physiology in asthma.2 Although numerous factors, such as increased ASM levels, pro-contractile molecules, pro-inflammatory cytokines, and growth factors, contribute to AHR, one of the key factors in determining ASM tone is regulated by vagal parasympathetic nerve innervation.1,2,3 The response to acetylcholine and other cholinergic agonists at these neuromuscular junctions is predominantly controlled by inhibitory Gi-coupled M2 and excitatory Gq-coupled M3 muscarinic acetylcholine receptors (mAChRs). Activation of M3 receptors results in ASM contraction and resulting bronchoconstriction through downstream calcium-dependent signalling pathways, while M2 activation inhibits neuronal acetylcholine release.2,3,4
Methacholine is a non-specific mAChR agonist, capable of acting on all mAChR subtypes.5,6,7 However, in the context of AHR, methacholine's ability to induce bronchoconstriction through M3 receptors is clinically relevant.2,4,8 In addition, M3 agonism may increase the release of pro-inflammatory cytokines, further contributing to AHR.9 The inhibitory effect of M2 agonism by methacholine is likely also important, as shown by animal studies using mice with impaired M2 function, and by observations that eosinophilic inflammation, such as occurs in asthma, negatively impacts M2 function.3 Hence, asthmatic patients are more sensitive to inhaled cholinergic agonists such as methacholine; this forms the basis for the methacholine challenge test, which diagnoses AHR through an increased methacholine-induced response.10,11
Target Actions Organism AMuscarinic acetylcholine receptor M3 agonistHumans AMuscarinic acetylcholine receptor M2 agonistHumans UMuscarinic acetylcholine receptor M1 agonistHumans UMuscarinic acetylcholine receptor M4 agonistHumans UMuscarinic acetylcholine receptor M5 agonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol Acebutolol may increase the bronchoconstrictory activities of Methacholine. Aclidinium Aclidinium may decrease effectiveness of Methacholine as a diagnostic agent. Amantadine Amantadine may decrease effectiveness of Methacholine as a diagnostic agent. Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with Methacholine. Amikacin The therapeutic efficacy of Methacholine can be decreased when used in combination with Amikacin. - Food Interactions
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Methacholine chloride 0W5ETF9M2K 62-51-1 JHPHVAVFUYTVCL-UHFFFAOYSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Methacholine Chloride, USP Powder, for solution 160 mg / vial Respiratory (inhalation) Panda Pharmaceuticals Inc. Not applicable Not applicable Canada 
Methacholine Chloride, USP Powder, for solution 1280 mg / vial Respiratory (inhalation) Panda Pharmaceuticals Inc. Not applicable Not applicable Canada Methacholine Chloride, USP Powder, for solution 100 mg / vial Respiratory (inhalation) Panda Pharmaceuticals Inc. Not applicable Not applicable Canada Methacholine Chloride, USP Powder, for solution 320 mg / vial Respiratory (inhalation) Panda Pharmaceuticals Inc. Not applicable Not applicable Canada Methacholine Chloride, USP Powder, for solution 1600 mg / vial Respiratory (inhalation) Panda Pharmaceuticals Inc. Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Provocholine Inhalation Solution Methacholine chloride (0.0625 mg / mL) + Methacholine chloride (0.25 mg / mL) + Methacholine chloride (1 mg / mL) + Methacholine chloride (16 mg / mL) + Methacholine chloride (4 mg / mL) Solution Respiratory (inhalation) Methapharm, Inc. Not applicable Not applicable Canada Provocholine Inhalation Solution Methacholine chloride (0.1875 mg/3mL) + Methacholine chloride (0.75 mg/3mL) + Methacholine chloride (3 mg/3mL) + Methacholine chloride (12 mg/3mL) + Methacholine chloride (48 mg/3mL) Kit; Solution Respiratory (inhalation) Methapharm Inc. 2022-03-03 Not applicable US 
Provocholine Inhalation Solution Methacholine chloride (0.0625 mg / mL) + Methacholine chloride (0.25 mg / mL) + Methacholine chloride (1 mg / mL) + Methacholine chloride (16 mg / mL) + Methacholine chloride (4 mg / mL) Solution Respiratory (inhalation) Methapharm, Inc. Not applicable Not applicable Canada Provocholine Inhalation Solution Methacholine chloride (0.1875 mg/3mL) + Methacholine chloride (0.75 mg/3mL) + Methacholine chloride (3 mg/3mL) + Methacholine chloride (12 mg/3mL) + Methacholine chloride (48 mg/3mL) Kit; Solution Respiratory (inhalation) Methapharm Inc. 2022-03-03 Not applicable US Provocholine Inhalation Solution Methacholine chloride (0.0625 mg / mL) + Methacholine chloride (0.25 mg / mL) + Methacholine chloride (1 mg / mL) + Methacholine chloride (16 mg / mL) + Methacholine chloride (4 mg / mL) Solution Respiratory (inhalation) Methapharm, Inc. Not applicable Not applicable Canada
Categories
- ATC Codes
- V04CX03 — Methacholine
- Drug Categories
- Amines
- Ammonium Compounds
- Autonomic Agents
- Bronchoconstrictor Agents
- Cholinergic Agents
- Cholinergic Agonists
- Cholinergic Receptor Agonist
- Diagnostic Agents
- Methacholine Compounds
- Miotics
- Muscarinic Agonists
- Neurotransmitter Agents
- Nitrogen Compounds
- Onium Compounds
- Other Diagnostics
- Parasympathomimetics
- Peripheral Nervous System Agents
- Quaternary Ammonium Compounds
- Respiratory System Agents
- Trimethyl Ammonium Compounds
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as tetraalkylammonium salts. These are organonitrogen compounds containing a quaternary ammonium substituted with four alkyl chains.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Quaternary ammonium salts
- Direct Parent
- Tetraalkylammonium salts
- Alternative Parents
- Carboxylic acid esters / Monocarboxylic acids and derivatives / Organopnictogen compounds / Organic salts / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds / Amines / Organic cations
- Substituents
- Aliphatic acyclic compound / Amine / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Organic cation / Organic oxide / Organic oxygen compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- quaternary ammonium ion, acetate ester (CHEBI:6804)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 03V657ZD3V
- CAS number
- 55-92-5
- InChI Key
- NZWOPGCLSHLLPA-UHFFFAOYSA-N
- InChI
- InChI=1S/C8H18NO2/c1-7(11-8(2)10)6-9(3,4)5/h7H,6H2,1-5H3/q+1
- IUPAC Name
- [2-(acetyloxy)propyl]trimethylazanium
- SMILES
- CC(C[N+](C)(C)C)OC(C)=O
References
- General References
- Aghasafari P, George U, Pidaparti R: A review of inflammatory mechanism in airway diseases. Inflamm Res. 2019 Jan;68(1):59-74. doi: 10.1007/s00011-018-1191-2. Epub 2018 Oct 10. [Article]
- Lam M, Lamanna E, Bourke JE: Regulation of Airway Smooth Muscle Contraction in Health and Disease. Adv Exp Med Biol. 2019;1124:381-422. doi: 10.1007/978-981-13-5895-1_16. [Article]
- Castro JM, Resende RR, Mirotti L, Florsheim E, Albuquerque LL, Lino-dos-Santos-Franco A, Gomes E, de Lima WT, de Franco M, Ribeiro OG, Russo M: Role of m2 muscarinic receptor in the airway response to methacholine of mice selected for minimal or maximal acute inflammatory response. Biomed Res Int. 2013;2013:805627. doi: 10.1155/2013/805627. Epub 2013 Apr 18. [Article]
- Gosens R, Bromhaar MM, Tonkes A, Schaafsma D, Zaagsma J, Nelemans SA, Meurs H: Muscarinic M(3) receptor-dependent regulation of airway smooth muscle contractile phenotype. Br J Pharmacol. 2004 Mar;141(6):943-50. doi: 10.1038/sj.bjp.0705709. Epub 2004 Mar 1. [Article]
- Gonzalez JC, Albinana E, Baldelli P, Garcia AG, Hernandez-Guijo JM: Presynaptic muscarinic receptor subtypes involved in the enhancement of spontaneous GABAergic postsynaptic currents in hippocampal neurons. Eur J Neurosci. 2011 Jan;33(1):69-81. doi: 10.1111/j.1460-9568.2010.07475.x. Epub 2010 Nov 23. [Article]
- Meyer EM, Otero DH: Pharmacological and ionic characterizations of the muscarinic receptors modulating [3H]acetylcholine release from rat cortical synaptosomes. J Neurosci. 1985 May;5(5):1202-7. [Article]
- Tulic MK, Wale JL, Petak F, Sly PD: Muscarinic blockade of methacholine induced airway and parenchymal lung responses in anaesthetised rats. Thorax. 1999 Jun;54(6):531-7. doi: 10.1136/thx.54.6.531. [Article]
- Borchers MT, Biechele T, Justice JP, Ansay T, Cormier S, Mancino V, Wilkie TM, Simon MI, Lee NA, Lee JJ: Methacholine-induced airway hyperresponsiveness is dependent on Galphaq signaling. Am J Physiol Lung Cell Mol Physiol. 2003 Jul;285(1):L114-20. doi: 10.1152/ajplung.00322.2002. Epub 2003 Feb 28. [Article]
- Gosens R, Rieks D, Meurs H, Ninaber DK, Rabe KF, Nanninga J, Kolahian S, Halayko AJ, Hiemstra PS, Zuyderduyn S: Muscarinic M3 receptor stimulation increases cigarette smoke-induced IL-8 secretion by human airway smooth muscle cells. Eur Respir J. 2009 Dec;34(6):1436-43. doi: 10.1183/09031936.00045209. Epub 2009 May 21. [Article]
- Davis BE, Blais CM, Cockcroft DW: Methacholine challenge testing: comparative pharmacology. J Asthma Allergy. 2018 May 14;11:89-99. doi: 10.2147/JAA.S160607. eCollection 2018. [Article]
- FDA Approved Drug Products: PROVOCHOLINE (methacholine chloride) inhalation [Link]
- External Links
- Human Metabolome Database
- HMDB0015654
- KEGG Compound
- C07471
- PubChem Compound
- 1993
- PubChem Substance
- 99443261
- ChemSpider
- 1916
- BindingDB
- 48918
- 155080
- ChEBI
- 6804
- ChEMBL
- CHEMBL978
- PharmGKB
- PA165958382
- Wikipedia
- Methacholine
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder, for solution Respiratory (inhalation) Powder, for solution Respiratory (inhalation) 1 % Powder, for solution Respiratory (inhalation) 6.4 % Powder, for solution Respiratory (inhalation) 1600 mg / vial Powder, for solution Respiratory (inhalation) 480 mg / vial Powder, for solution Respiratory (inhalation) 100 mg/100mg Powder, for solution Respiratory (inhalation) 100 mg / vial Powder, for solution Respiratory (inhalation) 1280 mg / vial Powder, for solution Respiratory (inhalation) 160 mg / vial Powder, for solution Respiratory (inhalation) 1600 mg/1600mg Powder, for solution Respiratory (inhalation) 320 mg / vial Kit; solution Respiratory (inhalation) Solution Respiratory (inhalation) Solution Respiratory (inhalation) 16 mg / mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 170-174 https://www.tcichemicals.com/GB/en/p/M0073 - Predicted Properties
Property Value Source Water Solubility 0.0678 mg/mL ALOGPS logP -2.7 ALOGPS logP -3.8 Chemaxon logS -3.5 ALOGPS pKa (Strongest Basic) -7 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 26.3 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 55.76 m3·mol-1 Chemaxon Polarizability 18.43 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9196 Blood Brain Barrier + 0.9595 Caco-2 permeable + 0.6374 P-glycoprotein substrate Non-substrate 0.7298 P-glycoprotein inhibitor I Non-inhibitor 0.9567 P-glycoprotein inhibitor II Non-inhibitor 0.8384 Renal organic cation transporter Non-inhibitor 0.8493 CYP450 2C9 substrate Non-substrate 0.8521 CYP450 2D6 substrate Non-substrate 0.8612 CYP450 3A4 substrate Substrate 0.5376 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9459 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9407 CYP450 3A4 inhibitor Non-inhibitor 0.9475 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9383 Ames test Non AMES toxic 0.8427 Carcinogenicity Carcinogens 0.754 Biodegradation Ready biodegradable 0.9303 Rat acute toxicity 2.3602 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.944 hERG inhibition (predictor II) Non-inhibitor 0.8091
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0pb9-9300000000-58ac206c8375cdba4dbe Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 131.71996 predictedDeepCCS 1.0 (2019) [M+H]+ 135.34608 predictedDeepCCS 1.0 (2019) [M+Na]+ 144.18382 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM3
- Uniprot ID
- P20309
- Uniprot Name
- Muscarinic acetylcholine receptor M3
- Molecular Weight
- 66127.445 Da
References
- Liu PS, Chen YY, Feng CK, Lin YH, Yu TC: Muscarinic acetylcholine receptors present in human osteoblast and bone tissue. Eur J Pharmacol. 2011 Jan 10;650(1):34-40. doi: 10.1016/j.ejphar.2010.09.031. Epub 2010 Oct 1. [Article]
- Fernandez-Rodriguez S, Broadley KJ, Ford WR, Kidd EJ: Increased muscarinic receptor activity of airway smooth muscle isolated from a mouse model of allergic asthma. Pulm Pharmacol Ther. 2010 Aug;23(4):300-7. doi: 10.1016/j.pupt.2010.03.001. Epub 2010 Mar 25. [Article]
- Liu T, Xie C, Chen X, Zhao F, Liu AM, Cho DB, Chong J, Yang PC: Role of muscarinic receptor activation in regulating immune cell activity in nasal mucosa. Allergy. 2010 Aug;65(8):969-77. doi: 10.1111/j.1398-9995.2009.02281.x. Epub 2009 Nov 27. [Article]
- Gosens R, Rieks D, Meurs H, Ninaber DK, Rabe KF, Nanninga J, Kolahian S, Halayko AJ, Hiemstra PS, Zuyderduyn S: Muscarinic M3 receptor stimulation increases cigarette smoke-induced IL-8 secretion by human airway smooth muscle cells. Eur Respir J. 2009 Dec;34(6):1436-43. doi: 10.1183/09031936.00045209. Epub 2009 May 21. [Article]
- Gosens R, Bromhaar MM, Tonkes A, Schaafsma D, Zaagsma J, Nelemans SA, Meurs H: Muscarinic M(3) receptor-dependent regulation of airway smooth muscle contractile phenotype. Br J Pharmacol. 2004 Mar;141(6):943-50. doi: 10.1038/sj.bjp.0705709. Epub 2004 Mar 1. [Article]
- Borchers MT, Biechele T, Justice JP, Ansay T, Cormier S, Mancino V, Wilkie TM, Simon MI, Lee NA, Lee JJ: Methacholine-induced airway hyperresponsiveness is dependent on Galphaq signaling. Am J Physiol Lung Cell Mol Physiol. 2003 Jul;285(1):L114-20. doi: 10.1152/ajplung.00322.2002. Epub 2003 Feb 28. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled acetylcholine receptor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Castro JM, Resende RR, Mirotti L, Florsheim E, Albuquerque LL, Lino-dos-Santos-Franco A, Gomes E, de Lima WT, de Franco M, Ribeiro OG, Russo M: Role of m2 muscarinic receptor in the airway response to methacholine of mice selected for minimal or maximal acute inflammatory response. Biomed Res Int. 2013;2013:805627. doi: 10.1155/2013/805627. Epub 2013 Apr 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM1
- Uniprot ID
- P11229
- Uniprot Name
- Muscarinic acetylcholine receptor M1
- Molecular Weight
- 51420.375 Da
References
- Tulic MK, Wale JL, Petak F, Sly PD: Muscarinic blockade of methacholine induced airway and parenchymal lung responses in anaesthetised rats. Thorax. 1999 Jun;54(6):531-7. doi: 10.1136/thx.54.6.531. [Article]
- Meyer EM, Otero DH: Pharmacological and ionic characterizations of the muscarinic receptors modulating [3H]acetylcholine release from rat cortical synaptosomes. J Neurosci. 1985 May;5(5):1202-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Guanyl-nucleotide exchange factor activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM4
- Uniprot ID
- P08173
- Uniprot Name
- Muscarinic acetylcholine receptor M4
- Molecular Weight
- 53048.65 Da
References
- Gonzalez JC, Albinana E, Baldelli P, Garcia AG, Hernandez-Guijo JM: Presynaptic muscarinic receptor subtypes involved in the enhancement of spontaneous GABAergic postsynaptic currents in hippocampal neurons. Eur J Neurosci. 2011 Jan;33(1):69-81. doi: 10.1111/j.1460-9568.2010.07475.x. Epub 2010 Nov 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Phosphatidylinositol phospholipase c activity
- Specific Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
- Gene Name
- CHRM5
- Uniprot ID
- P08912
- Uniprot Name
- Muscarinic acetylcholine receptor M5
- Molecular Weight
- 60073.205 Da
References
- Gonzalez JC, Albinana E, Baldelli P, Garcia AG, Hernandez-Guijo JM: Presynaptic muscarinic receptor subtypes involved in the enhancement of spontaneous GABAergic postsynaptic currents in hippocampal neurons. Eur J Neurosci. 2011 Jan;33(1):69-81. doi: 10.1111/j.1460-9568.2010.07475.x. Epub 2010 Nov 23. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- This action is predicted based on inhibition studies of inhaled β-agonists and requires confirmation by studies explicitly demonstrating inhibition of OCTN2 by methacholine.
- General Function
- Symporter activity
- Specific Function
- Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Solute carrier family 22 member 5
- Molecular Weight
- 62751.08 Da
References
- Gnadt M, Trammer B, Freiwald M, Kardziev B, Bayliss MK, Edwards CD, Schmidt M, Friedel G, Hogger P: Methacholine delays pulmonary absorption of inhaled beta(2)-agonists due to competition for organic cation/carnitine transporters. Pulm Pharmacol Ther. 2012 Feb;25(1):124-34. doi: 10.1016/j.pupt.2011.12.009. Epub 2012 Jan 5. [Article]
Drug created at May 16, 2010 15:28 / Updated at February 20, 2024 23:55