Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00003

Target Information
NameMuscarinic acetylcholine receptor M2    
Type of targetSuccessful target    
SynonymsM2 receptor    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
[ICD9: 338   ICD10: R52]
Autoimmune cardiomyopathy[3]
Bronchoconstriction (cold air-induced)
[ICD9: 493   ICD10: J45]
Chronic obstructive pulmonary disease, unspecified
[ICD9: 460-519, 490-492, 494-496   ICD10: J00-J99, J40-J44, J47]
[ICD9: 991.6   ICD10: T68]
Neurogenic bladder
[ICD9: 188   ICD10: C67]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
Tremor, unspecified
[ICD9: 781.0   ICD10: R25.1]
Drug(s)Gallamine TriethiodideApprovedStabilize muscle contractions[7]
MethylscopolamineApprovedPeptic ulcer disease[8]
ScopolamineApprovedNausea and Addiction[9][10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
Regulation of actin cytoskeleton
UniProt IDP08172
PDB Structure1LUB; 3UON.    
FunctionThe muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins.    
Related US Patent6,288,068
Target ValidationClick to Find Target Validation Information.    
1,1-diphenyl-2- (3-tropanyl)ethanol[12]
1-Methyl-1- (4-pyrrolidin-1-yl-but-2-ynyl)-urea[13]
2- (4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione[15]
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime[16]
3- (3-benzylamino)-piperidin-2-one[17]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[19]
6-Dimethylamino-2-methyl-hex-4-ynal oxime[16]
7-Dimethylamino-hept-5-yn-2-one oxime[16]
7-Pyrrolidin-1-yl-hept-5-yn-2-one oxime[16]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester[22]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester[24]
N- (4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide[16]
N-methoxyquinuclidine-3-carboximidoyl chloride[23]
N-methoxyquinuclidine-3-carboximidoyl fluoride[23]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester[24]
Tiotropium Bromide[35]
Antagonist (R)-4-[2-[3-[37][3]
Gallamine Triethiodide[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Psychosis of Alzheimer's disease is associated with elevated muscarinic M2 binding in the cortex. Neurology. 2001 Sep 11;57(5):805-11. To Reference
Ref 2Evaluation of muscarinic agonist-induced analgesia in muscarinic acetylcholine receptor knockout mice. Mol Pharmacol. 2002 Nov;62(5):1084-93. To Reference
Ref 3Beneficial effect of muscarinic-2 antagonist on dilated cardiomyopathy induced by autoimmune mechanism against muscarinic-2 receptor. J Cardiovasc Pharmacol. 2001 Oct;38 Suppl 1:S43-9. To Reference
Ref 4Function of pulmonary neuronal M(2) muscarinic receptors in stable chronic obstructive pulmonary disease. Am J Respir Crit Care Med. 2001 May;163(6):1320-5. To Reference
Ref 5Generation and pharmacological analysis of M2 and M4 muscarinic receptor knockout mice. Life Sci. 2001 Apr 27;68(22-23):2457-66. To Reference
Ref 6The effects of the antagonists of muscarinic acetylcholine receptor subtypes in rat brain on urinary bladder contraction. Nippon Hinyokika Gakkai Zasshi. 2002 Mar;93(3):427-34. To Reference
Ref 7Cholinergic regulation of the corpora allata in adult male loreyi leafworm Mythimna loreyi. Arch Insect Biochem Physiol. 2002 Apr;49(4):215-24. To Reference
Ref 8Methylacridinium and its Cholinergic Properties. Neurotox Res. 2009 Jun 30. [Epub ahead of print] To Reference
Ref 9The amygdala modulates morphine-induced state-dependent memory retrieval via muscarinic acetylcholine receptors. Neuroscience. 2009 May 5;160(2):255-63. Epub 2009 Mar 9. To Reference
Ref 10Midbrain acetylcholine and glutamate receptors modulate accumbal dopamine release. Neuroreport. 2008 Jun 11;19(9):991-5. To Reference
Ref 11J Med Chem. 1989 May;32(5):1057-62.Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist. To Reference
Ref 12Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2. Epub 2009 Jul 8.Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD. To Reference
Ref 13J Med Chem. 1992 Aug 21;35(17):3270-9.Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. To Reference
Ref 14J Med Chem. 1998 Oct 22;41(22):4181-5.Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone. To Reference
Ref 15Bioorg. Med. Chem. Lett. 7(8):979-984 (1997) To Reference
Ref 16Bioorg. Med. Chem. Lett. 2(8):803-808 (1992) To Reference
Ref 17J Med Chem. 2007 Apr 19;50(8):1925-32. Epub 2007 Mar 17.Designing active template molecules by combining computational de novo design and human chemist's expertise. To Reference
Ref 18J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives. To Reference
Ref 19J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 20J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 21J Med Chem. 1993 Apr 2;36(7):842-7.Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. To Reference
Ref 22J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. To Reference
Ref 23Bioorg. Med. Chem. Lett. 2(8):791-796 (1992) To Reference
Ref 24J Med Chem. 2000 Jun 29;43(13):2514-22.6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. To Reference
Ref 25J Med Chem. 1991 Oct;34(10):2984-9.Muscarinic receptor binding profile of para-substituted caramiphen analogues. To Reference
Ref 26J Med Chem. 1989 Dec;32(12):2573-82.Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. To Reference
Ref 27Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist. To Reference
Ref 28J Nat Prod. 2005 Jul;68(7):1061-5.Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. To Reference
Ref 29Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70.Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations. To Reference
Ref 30J Med Chem. 1990 Feb;33(2):809-14.Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. To Reference
Ref 31J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. To Reference
Ref 32J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. To Reference
Ref 33J Med Chem. 2002 Dec 5;45(25):5415-8.Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists. To Reference
Ref 34J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. To Reference
Ref 35J Med Chem. 2009 Aug 27;52(16):5076-92.Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide). To Reference
Ref 36Bioorg. Med. Chem. Lett. 2(8):809-814 (1992) To Reference
Ref 37Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. To Reference


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