DGIdb - CHRM2 Gene Record

CHRM2 1129 Druggable Genome

Alternate Names:

1129
CHOLINERGIC RECEPTOR MUSCARINIC 2
CHRM2
HM2
118493
1951
ENSG00000181072
OTTHUMG00000155658
P08172
ACM2_HUMAN
MUSCARINIC ACETYLCHOLINE RECEPTOR M2. [SOURCE:UNIPROT/SWISSPROT;ACC:P08172]
MUSCARINIC ACETYLCHOLINE RECEPTOR M2
PA111
T46185

Gene Info:

Target Main Class	Receptors
Target Subclass	Rhodopsin
Transmembrane Helix Count	6
Target Subclass	GPCR
Human Readable Name	DRUGGABLE GENOME
Target Class	Receptors
Interpro Acc	IPR000276
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Uniprot Evidence	1: Evidence at protein level
Interpro Name	GPCR, rhodopsin-like, 7TM
Interpro Short Name	7TM_GPCR_Rhodpsn
Uniprot Status	Swiss-Prot
Interpro Type	Family
Gene Biotype	PROTEIN_CODING

(7 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Hou et al., 1998, Neuromuscular relaxants as antagonists for M2 and M3 muscarinic receptors., Anesthesiology
Milchert et al., 2009, Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro., J. Physiol. Pharmacol.
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Barnes et al., 1995, Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airways disease., Life Sci.
Hansel et al., 2002, Tiotropium bromide: a novel once-daily anticholinergic bronchodilator for the treatment of COPD., Drugs Today
Snyder et al., 1974, Antischizophrenic drugs and brain cholinergic receptors. Affinity for muscarinic sites predicts extrapyramidal effects., Arch. Gen. Psychiatry
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
Ehlert et al., 1990, The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart., J. Pharmacol. Exp. Ther.
Nelson et al., 2006, Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor., J. Pharmacol. Exp. Ther.
Roman et al., 2005, Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors., Brain Res.
Minaba et al., 2006, Activation of nematode G protein GOA-1 by the human muscarinic acetylcholine receptor M2 subtype. Functional coupling of G-protein-coupled receptor and G protein originated from evolutionarily distant animals., FEBS J.
Cembala et al., 2007, Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors., Eur. J. Pharmacol.
May et al., 2005, Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators., J. Pharmacol. Exp. Ther.
McNamara et al., 2009, Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist., Eur. J. Pharmacol.
Sellers et al., 2000, M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro., J Auton Pharmacol
Schneider et al., 2004, Signal transduction underlying carbachol-induced contraction of human urinary bladder., J. Pharmacol. Exp. Ther.
Mobascher A et al., 2010, Association of a variant in the muscarinic acetylcholine receptor 2 gene (CHRM2) with nicotine addiction., Am J Med Genet B Neuropsychiatr Genet
Golembiewski et al., 2002, A systematic approach to the management of postoperative nausea and vomiting., J. Perianesth. Nurs.
Larson et al., 1991, Selectivity of antimuscarinic compounds for muscarinic receptors of human brain and heart., Psychopharmacology (Berl.)
Waelbroeck et al., 1992, Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors., Eur. J. Pharmacol.
Waelbroeck et al., 1990, Stereoselectivity of procyclidine binding to muscarinic receptor subtypes M1, M2 and M4., Eur. J. Pharmacol.
Myhrer, 2010, Identification of neuronal target areas for nerve agents and specification of receptors for pharmacological treatment., Neurotoxicology
Ito et al., 2009, Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout mice., Eur. J. Pharmacol.
Dmochowski, 2005, Improving the tolerability of anticholinergic agents in the treatment of overactive bladder., Drug Saf
Oki et al., 2007, Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder., J. Urol.
Sinha et al., 2010, AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder., Br. J. Pharmacol.
Yarker YE et al., 1995, Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability., Drugs Aging
Sawatzky et al., 2003, Eosinophil-induced release of acetylcholine from differentiated cholinergic nerve cells., Am. J. Physiol. Lung Cell Mol. Physiol.
Peter et al., 2004, Modulation of the M2 muscarinic acetylcholine receptor activity with monoclonal anti-M2 receptor antibody fragments., J. Biol. Chem.
Zuchner et al., 2005, Down-regulation of muscarinic acetylcholine receptor M2 adversely affects the expression of Alzheimer's disease-relevant genes and proteins., J. Neurochem.
Sterin-Borda et al., 2002, Therapeutic use of muscarinic acetylcholine receptor peptide to prevent mice chagasic cardiac dysfunction., J. Mol. Cell. Cardiol.
Almadhoun K et al., 2020, Bronchodilators,
Wellington, 2005, Ipratropium bromide HFA., Treat Respir Med
Rehder KJ, 2017, Adjunct Therapies for Refractory Status Asthmaticus in Children., Respir Care
Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.
Dahl et al., 1986, Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding., Biochem. Pharmacol.
Jovanović et al., 1994, Endothelium-dependent relaxation in response to acetylcholine in the human uterine artery., Eur. J. Pharmacol.
Pavía et al., 1997, Pharmacological characterization and distribution of muscarinic receptors in human placental syncytiotrophoblast brush-border and basal plasma membranes., Eur. J. Pharmacol.
Varoli et al., 1999, Synthesis and antagonistic activity at muscarinic receptor subtypes of some 2-carbonyl derivatives of diphenidol., Bioorg. Med. Chem.
Braverman et al., 2002, Interaction between muscarinic receptor subtype signal transduction pathways mediating bladder contraction., Am. J. Physiol. Regul. Integr. Comp. Physiol.
Kovacs et al., 1998, Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line., J. Pharmacol. Exp. Ther.
Pelat et al., 1999, Characterization of the central muscarinic cholinoceptors involved in the cholinergic pressor response in anesthetized dogs., Eur. J. Pharmacol.
Waelbroeck et al., 1991, Stereoselectivity of (R)- and (S)-hexahydro-difenidol binding to neuroblastoma M1, cardiac M2, pancreatic M3, and striatum M4 muscarinic receptors., Chirality
Lazartigues et al., 1998, Pressor and bradycardic effects of tacrine and other acetylcholinesterase inhibitors in the rat., Eur. J. Pharmacol.
Greco et al., 2008, The role of combination medical therapy in benign prostatic hyperplasia., Int. J. Impot. Res.
Abbiati et al., 1988, Receptor binding studies of the flavone, REC 15/2053, and other bladder spasmolytics., Pharm. Res.
Uckert et al., 2000, Responses of isolated normal human detrusor muscle to various spasmolytic drugs commonly used in the treatment of the overactive bladder., Arzneimittelforschung
Moreno-Vinasco et al., 2009, Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects., Am. J. Physiol. Lung Cell Mol. Physiol.
Figueroa et al., 2009, Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes., J. Pharmacol. Exp. Ther.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Mansfield et al., 2009, Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa., J. Pharmacol. Exp. Ther.
Schmitz J et al., 2014, Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity., J Med Chem
Schjelderup et al., 1988, Antimuscarinic effects of (R)- and (S)- oxyphencyclimine hydrochloride., Pharm. Res.
Johnson et al., 2005, The role of muscarinic receptor antagonism in antipsychotic-induced hippocampal acetylcholine release., Eur. J. Pharmacol.

DOXACURIUM CHRM2

Interaction Score: 3.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423 9523819

Sources:
TdgClinicalTrial TEND
NAPHMETHONIUM CHRM2

Interaction Score: 2.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25051097

Sources:
DTC
DIPHENIDOL CHRM2

Interaction Score: 2.42

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8050463 9059856 10530931 12185001 9454790 10497897 1863523 9851542

Sources:
TdgClinicalTrial TEND
PROCYCLIDINE CHRM2

Interaction Score: 2.42

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2027917 1426023 2253700 20624420 17016423 17139284

Sources:
TdgClinicalTrial TEND
OXYBUTYNIN CHRM2

Interaction Score: 2.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AA-2010

Novel drug target Established target

Trial Name AP-1034,Anturol

PMIDs:
19446545 15963006 17222678 16188951 20590605 7620236

Sources:
TdgClinicalTrial ChemblInteractions TEND
FLAVOXATE CHRM2

Interaction Score: 2.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19002123 3247311 17016423 17139284 10858873

Sources:
TdgClinicalTrial TEND
MIVACURIUM CHRM2

Interaction Score: 2.02

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 9523819

Sources:
TdgClinicalTrial TEND
SCOPOLAMINE CHRM2

Interaction Score: 1.82

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15627430 11752352

Sources:
TTD
OXYPHENCYCLIMINE CHRM2

Interaction Score: 1.82

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1426023 3247303 17016423 17139284

Sources:
TdgClinicalTrial TEND
CARBACHOL CHRM2

Interaction Score: 1.7

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12948933 15485827 15333678 16181410 12505062

Sources:
TdgClinicalTrial TEND
TRIDIHEXETHYL CHRM2

Interaction Score: 1.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
ROCURONIUM CHRM2

Interaction Score: 1.01

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name rocuronium bromide,Esmeron, Zemuron, Eslax

Novel drug target Established target

PMIDs:
20400785 17016423 17139284

Sources:
TdgClinicalTrial TEND
ATROPINE CHRM2

Interaction Score: 0.99

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Trial Name inhaled atropine

PMIDs:
7855217 16188951 16248990 17087737 17588565 15333678

Sources:
TdgClinicalTrial ChemblInteractions TEND
METHIXENE CHRM2

Interaction Score: 0.97

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
IPRATROPIUM CHRM2

Interaction Score: 0.87

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ipratropium bromide + albuterol sulfate,DuoNeb

Novel drug target Established target

PMIDs:
30085570 15987237 28546381

Sources:
TdgClinicalTrial TEND
TRIFLUPROMAZINE CHRM2

Interaction Score: 0.76

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
4152054 17016423 17139284

Sources:
TdgClinicalTrial TEND
SOLIFENACIN CHRM2

Interaction Score: 0.73

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
19029429 20590605

Sources:
TdgClinicalTrial
TOLTERODINE CHRM2

Interaction Score: 0.73

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name THVD-201

Novel drug target Established target

Trial Name tolterodine extended release capsules,Detrol LA

PMIDs:
19168050 11193006 16188951 14769832

Sources:
TdgClinicalTrial TEND
TIOTROPIUM CHRM2

Interaction Score: 0.73

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tiotropium bromide,Spiriva

Novel drug target Established target

PMIDs:
10188785 12582447

Sources:
TdgClinicalTrial
BENZQUINAMIDE CHRM2

Interaction Score: 0.69

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
DARIFENACIN HYDROBROMIDE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SOLIFENACIN SUCCINATE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TROSPIUM CHLORIDE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZAMIFENACIN CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BETHANECHOL CHLORIDE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M2 agonist

PMIDs:
None found

Sources:
ChemblInteractions
TOLTERODINE TARTRATE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
FESOTERODINE FUMARATE CHRM2

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
ENDO-ATROPINE CHRM2

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25051097

Sources:
DTC
FESOTERODINE CHRM2

Interaction Score: 0.48

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
19029429

Sources:
TEND
PILOCARPINE CHRM2

Interaction Score: 0.47

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name THVD-201

PMIDs:
19465517 18824613 11752352

Sources:
TdgClinicalTrial TEND
BATEFENTEROL CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ATROPINE SULFATE CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYBUTYNIN CHLORIDE CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DESIPRAMINE CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND
METHSCOPOLAMINE CHRM2

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PROPIOMAZINE CHRM2

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TdgClinicalTrial TEND
LEVOMEPROMAZINE CHRM2

Interaction Score: 0.35

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND
PROMAZINE CHRM2

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
DOXEPIN CHRM2

Interaction Score: 0.27

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
ACECLIDINE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PIPERTRAMINE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROPANTHELINE BROMIDE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACLIDINIUM CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Aclidinium

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
DAROTROPIUM BROMIDE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROMETHAZINE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12476402

Sources:
TdgClinicalTrial TEND
PIPERTRAMINE AMIDE CHRM2

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
THIETHYLPERAZINE CHRM2

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
AFACIFENACIN CHRM2

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ASM-024 CHRM2

Interaction Score: 0.17

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OLANZAPINE CHRM2

Interaction Score: 0.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ALKS 3831

Trial Name OREX-003, olanzapine plus zonisamide SR

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

PMIDs:
17848919 10227113 25032030

Sources:
TdgClinicalTrial TEND
NICOTINE CHRM2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19644963

Sources:
PharmGKB

Ensembl: ENSG00000181072
- Version: 101_38
Alternate Names:

CHRM2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000181072
- Version: 26-July-2011
Alternate Names:

CHRM2 Display Id

MUSCARINIC ACETYLCHOLINE RECEPTOR M2. [SOURCE:UNIPROT/SWISSPROT;ACC:P08172] Description

ENSG00000181072 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P08172
- Version: January-2014
Alternate Names:

CHRM2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
HopkinsGroom: P08172
- Version: 11-September-2012
Alternate Names:

P08172 Uniprot Accession

MUSCARINIC ACETYLCHOLINE RECEPTOR M2 Uniprot Protein Name

CHRM2 Uniprot Gene Name

Gene Info:

Interpro Acc IPR000276

Human Readable Name G PROTEIN COUPLED RECEPTOR

Uniprot Evidence 1: Evidence at protein level

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P08172
- Version: 01-August-2011
Alternate Names:

1129 Entrez Gene Id

P08172 Uniprot Accession

ACM2_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Transmembrane Helix Count 6

Publications:
PharmGKB: CHRM2
- Version: 18-August-2020
Alternate Names:

PA111 PharmGKB ID

Gene Info:

Publications:

Mobascher A et al., 2010, Association of a variant in the muscarinic acetylcholine receptor 2 gene (CHRM2) with nicotine addiction., Am J Med Genet B Neuropsychiatr Genet
DTC: CHRM2
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Schmitz J et al., 2014, Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity., J Med Chem
ChemblInteractions: CHRM2
- Version: chembl_23
Alternate Names:

CHRM2 GENE_SYMBOL

Muscarinic acetylcholine receptor M2 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000181072
- Version: 31-May-2017
Alternate Names:

ENSG00000181072 Gene Symbol

CHRM2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: CHRM2
- Version: 27-Jun-2013
Alternate Names:

1129 Gene ID

HM2 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Muscarinic acetylcholine receptor M2
- Version: 2020.06.01
Alternate Names:

CHRM2 TTD Gene Abbreviation

T46185 TTD Target ID

Gene Info:

Publications:

Trial Name	AA-2010
Novel drug target	Established target
Trial Name	AP-1034,Anturol

Trial Name	rocuronium bromide,Esmeron, Zemuron, Eslax
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	Muscarinic acetylcholine receptor M2 antagonist
Trial Name	inhaled atropine

Trial Name	ipratropium bromide + albuterol sulfate,DuoNeb
Novel drug target	Established target

Trial Name	Solifenacin succinate, YM-905,Vesicare
Novel drug target	Established target

Trial Name	THVD-201
Novel drug target	Established target
Trial Name	tolterodine extended release capsules,Detrol LA

Trial Name	tiotropium bromide,Spiriva
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	Muscarinic acetylcholine receptor M2 agonist

Trial Name	Silenor (SO-101)
Novel drug target	Established target

Mechanism of Interaction	Muscarinic acetylcholine receptor antagonist
Direct Interaction	yes

partial agonist (activating)
antagonist (inhibitory)

Trial Name	ALKS 3831
Trial Name	OREX-003, olanzapine plus zonisamide SR
Trial Name	Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

CHRM2	Display Id
MUSCARINIC ACETYLCHOLINE RECEPTOR M2. [SOURCE:UNIPROT/SWISSPROT;ACC:P08172]	Description
ENSG00000181072	Ensembl Gene Id

P08172	Uniprot Accession
MUSCARINIC ACETYLCHOLINE RECEPTOR M2	Uniprot Protein Name
CHRM2	Uniprot Gene Name

1129	Entrez Gene Id
P08172	Uniprot Accession
ACM2_HUMAN	Uniprot Id

CHRM2 Gene Record

CHRM2 1129 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17139284 17016423 9523819

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25051097

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8050463 9059856 10530931 12185001 9454790 10497897 1863523 9851542

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2027917 1426023 2253700 20624420 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name AA-2010 Novel drug target Established target Trial Name AP-1034,Anturol

PMIDs: 19446545 15963006 17222678 16188951 20590605 7620236

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 19002123 3247311 17016423 17139284 10858873

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: partial agonist (activating) antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 9523819

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 15627430 11752352

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 1426023 3247303 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12948933 15485827 15333678 16181410 12505062

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name rocuronium bromide,Esmeron, Zemuron, Eslax Novel drug target Established target

PMIDs: 20400785 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist Trial Name inhaled atropine

PMIDs: 7855217 16188951 16248990 17087737 17588565 15333678

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name ipratropium bromide + albuterol sulfate,DuoNeb Novel drug target Established target

PMIDs: 30085570 15987237 28546381

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 4152054 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Solifenacin succinate, YM-905,Vesicare Novel drug target Established target

PMIDs: 19029429 20590605

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name THVD-201 Novel drug target Established target Trial Name tolterodine extended release capsules,Detrol LA

PMIDs: 19168050 11193006 16188951 14769832

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name tiotropium bromide,Spiriva Novel drug target Established target

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423 9523819

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
25051097

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8050463 9059856 10530931 12185001 9454790 10497897 1863523 9851542

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2027917 1426023 2253700 20624420 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name AA-2010

Novel drug target Established target

Trial Name AP-1034,Anturol

PMIDs:
19446545 15963006 17222678 16188951 20590605 7620236

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
19002123 3247311 17016423 17139284 10858873

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

partial agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 9523819

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
15627430 11752352

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
1426023 3247303 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12948933 15485827 15333678 16181410 12505062

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name rocuronium bromide,Esmeron, Zemuron, Eslax

Novel drug target Established target

PMIDs:
20400785 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Trial Name inhaled atropine

PMIDs:
7855217 16188951 16248990 17087737 17588565 15333678

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name ipratropium bromide + albuterol sulfate,DuoNeb

Novel drug target Established target

PMIDs:
30085570 15987237 28546381

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
4152054 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
19029429 20590605

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name THVD-201

Novel drug target Established target

Trial Name tolterodine extended release capsules,Detrol LA

PMIDs:
19168050 11193006 16188951 14769832

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tiotropium bromide,Spiriva

Novel drug target Established target

PMIDs:
10188785 12582447

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M2 antagonist

Direct Interaction yes