DT-Web

DB06709 - Methacholine


Identification
Name Methacholine
Accession Number DB06709
Type small molecule
Description Methacholine acts as a non-selective muscarinic receptor agonist to stimulate the parasympathetic nervous system. It is most commonly used for diagnosing bronchial hyperreactivity, using the bronchial challenge test. Through this test, the drug causes bronchoconstriction and people with pre-existing airway hyperreactivity, such as asthmatics, will react to lower doses of drug.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 160.234
Groups approved
Monoisotopic Weight 160.133753825
Pharmacology
Indication It is most commonly used for diagnosing bronchial hyperreactivity, using the bronchial challenge test.
Mechanism of action By agonizing the muscarinic receptors, this drug induces bronchoconstriction. This bronchoconstriction is used as a test in asthmatics and in bronchial hyperreactivity.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions
Drug Mechanism of interaction
Betaxolol Beta-Blockers like betaxolol may worsen brochoconstriction and decrease the effectiveness of agents used to treat the resulting bronchoconstriction. Use of betaxolol and methacholine concomitantly is contraindicated.
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M3
Name Muscarinic acetylcholine receptor M3
Gene Name CHRM3
Pharmacological action yes
Actions agonist
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. Epub 2010 Oct 1. - Pubmed
  • 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. Epub 2010 Mar 25. - Pubmed
  • 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. Epub 2009 Nov 27. - Pubmed
  • 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. Epub 2009 May 21. - Pubmed
DTHybrid score 0.2688

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.1446
103 Muscarinic acetylcholine receptor M1 CHRM1 0.1417
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0982
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0719
4119 Cytochrome P450 2D6 CYP2D6 0.0272
4512 Cytochrome P450 3A4 CYP3A4 0.0269
492 Histamine H1 receptor HRH1 0.0231
3923 Cholinesterase BCHE 0.0194
502 5-hydroxytryptamine 2A receptor HTR2A 0.017
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0159
590 5-hydroxytryptamine 2C receptor HTR2C 0.0146
1588 Multidrug resistance protein 1 ABCB1 0.0133
556 Alpha-1A adrenergic receptor ADRA1A 0.0133
4757 Cytochrome P450 2C9 CYP2C9 0.01
831 D(2) dopamine receptor DRD2 0.0098
4200 Cytochrome P450 1A2 CYP1A2 0.0093
789 Alpha-1D adrenergic receptor ADRA1D 0.0092
540 Sodium-dependent noradrenaline transporter SLC6A2 0.009
632 Alpha-1B adrenergic receptor ADRA1B 0.0086
6013 Cytochrome P450 2E1 CYP2E1 0.0085
6016 Cytochrome P450 2C19 CYP2C19 0.0085
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0084
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0084
23 D(1A) dopamine receptor DRD1 0.0084
833 Organic cation/carnitine transporter 1 SLC22A4 0.008
432 D(4) dopamine receptor DRD4 0.0077
6030 Cytochrome P450 2B6 CYP2B6 0.0077
4924 Cytochrome P450 2C8 CYP2C8 0.0076
824 Sodium-dependent serotonin transporter SLC6A4 0.0073
4118 Cytochrome P450 3A5 CYP3A5 0.0072
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0067
6144 Solute carrier family 22 member 2 SLC22A2 0.0066
118 Organic cation/carnitine transporter 2 SLC22A5 0.0063
6145 Solute carrier family 22 member 1 SLC22A1 0.0063
638 D(3) dopamine receptor DRD3 0.0063
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0058
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0058
320 5-hydroxytryptamine 1A receptor HTR1A 0.0055
2129 Sucrase-isomaltase, intestinal SI 0.0055
378 Alpha-2C adrenergic receptor ADRA2C 0.0053
318 Alpha-2A adrenergic receptor ADRA2A 0.0053
629 Alpha-2B adrenergic receptor ADRA2B 0.0053
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.005
528 5-hydroxytryptamine 1E receptor HTR1E 0.0048
1256 5-hydroxytryptamine 6 receptor HTR6 0.0045
163 D(1B) dopamine receptor DRD5 0.0044
5718 Cytochrome P450 2A6 CYP2A6 0.0043
716 5-hydroxytryptamine 7 receptor HTR7 0.0041
341 5-hydroxytryptamine 3 receptor HTR3A 0.0038
6107 Cytochrome P450 3A7 CYP3A7 0.0038
725 5-hydroxytryptamine 1D receptor HTR1D 0.0036
885 5-hydroxytryptamine 1B receptor HTR1B 0.0035
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0034
436 5-hydroxytryptamine 2B receptor HTR2B 0.0028
6182 Cytochrome P450 2J2 CYP2J2 0.0028
465 Calmodulin CALM1 0.0027
467 Delta-type opioid receptor OPRD1 0.0026
696 Kappa-type opioid receptor OPRK1 0.0026
6432 Transporter snf 0.0023
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0023
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0022
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0021
847 Mu-type opioid receptor OPRM1 0.0018
587 Serum albumin ALB 0.0018
6106 Cytochrome P450 2C18 CYP2C18 0.0016
1360 Sphingomyelin phosphodiesterase SMPD1 0.0016
6147 Solute carrier family 22 member 3 SLC22A3 0.0016
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0016
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0015
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0014
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0014
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0011
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0011
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0011
1618 High affinity nerve growth factor receptor NTRK1 0.0011
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0011
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.001
124 Histamine H2 receptor HRH2 0.001
164 Histamine H4 receptor HRH4 0.001
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0009
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0008
20 Prostaglandin G/H synthase 1 PTGS1 0.0008
193 Beta-1 adrenergic receptor ADRB1 0.0007
766 Beta-2 adrenergic receptor ADRB2 0.0007
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0007
1898 Cytochrome P450 1B1 CYP1B1 0.0006
6024 Cytochrome P450 1A1 CYP1A1 0.0005
↑