Target Information

Target General Infomation
Target ID
T67684
Former ID
TTDS00004
Target Name
Muscarinic acetylcholine receptor M3
Gene Name
CHRM3
Synonyms
M3 receptor; CHRM3
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Diagnosing bronchial hyperreactivity [ICD10: W88]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Overactive bladder [ICD9: 596.51; ICD10: N32.81]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Obstructive lung diseases [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Postoperative nausea and vomiting [ICD10: R11]
Respiratory disease [ICD10: J00-J99]
Sjogren's syndrome [ICD9: 710.2; ICD10: M35.0]
Spasms; Pain [ICD9: 338,780; ICD10: R52, G89]
Seborrhea [ICD10: L21]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
The 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. Primary transducing effect is Pi turnover.
BioChemical Class
GPCR rhodopsin
Target Validation
T67684
UniProt ID
P20309
Sequence
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI
SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR
TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF
YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM
KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE
TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR
MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN
PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL
Structure
2CSA
Drugs and Mode of Action
Drug(s) ACECLIDINE Drug Info Approved Glaucoma [1], [2]
Cevimeline Drug Info Approved Sjogren's syndrome [3]
Darifenacin Drug Info Approved Overactive bladder disorder [4], [5], [6]
Ipratropium Drug Info Approved Obstructive lung diseases [7], [8]
LAS-34273 Drug Info Approved Chronic obstructive pulmonary disease [9], [10]
Methacholine Chloride Drug Info Approved Diagnosing bronchial hyperreactivity [2]
Methscopolamine Bromide Drug Info Approved Postoperative nausea and vomiting [2]
SMT-D002 Drug Info Approved Seborrhea [11]
Solifenacin Drug Info Approved Overactive bladder disorder [12], [13]
Succinylcholine Drug Info Approved Spasms; Pain [14], [15], [2]
Tiotropium Drug Info Approved Chronic obstructive pulmonary disease [5], [16]
Tolterodine Drug Info Approved Overactive bladder [2]
(R)-mequitazine (incontinence/respiratory disease), Pierre Fabre Drug Info Phase 2 Respiratory disease [17]
Tarafenacin Drug Info Phase 2 Overactive bladder disorder [18]
TRN-157 Drug Info Phase 2 Chronic obstructive pulmonary disease [19]
CHF 5407 Drug Info Phase 1 Chronic obstructive pulmonary disease [20]
Zamifenacin Drug Info Discontinued in Phase 3 Urinary incontinence [21]
PSD-506 Drug Info Discontinued in Phase 2 Overactive bladder disorder [22]
Revatropate Drug Info Discontinued in Phase 1 Chronic obstructive pulmonary disease [23]
Alvameline Drug Info Terminated Alzheimer disease [24]
Modulator (R)-mequitazine (incontinence/respiratory disease), Pierre Fabre Drug Info
Alvameline Drug Info [24]
CHF 5407 Drug Info
DAU-5750 Drug Info
DAU-5884 Drug Info
Ipratropium Drug Info
Methacholine Chloride Drug Info [25]
Methscopolamine Bromide Drug Info
PSD-506 Drug Info [26]
Revatropate Drug Info
Inhibitor 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info [27]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info [28]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info [29]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info [30]
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info [31]
3-(3-benzylamino)-piperidin-2-one Drug Info [32]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [31]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info [33]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [34]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info [31]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info [31]
7-Dimethylamino-hept-5-yn-2-one Drug Info [31]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [31]
A-987306 Drug Info [35]
ACECLIDINE Drug Info [36]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [37]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [38]
BRL-55473 Drug Info [39]
CREMASTRINE Drug Info [40]
FLUMEZAPINE Drug Info [41]
FM1-10 Drug Info [42]
FM1-43 Drug Info [42]
GNF-PF-5618 Drug Info [43]
ISOCLOZAPINE Drug Info [44]
ISOLOXAPINE Drug Info [45]
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info [31]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info [39]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info [39]
NOCARDIMICIN A Drug Info [43]
Nocardimicin C Drug Info [43]
Nocardimicin D Drug Info [43]
Nocardimicin F Drug Info [43]
Noccardimicin E Drug Info [43]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [38]
SULFOARECOLINE Drug Info [46]
UCB-101333-3 Drug Info [47]
Antagonist 3-(1-carbamoyl-1,1-diphenylmethyl)-1-(4-methoxyphenylethyl)pyrrolidine (APP) Drug Info [48]
4-DAMP Drug Info [49], [50]
AE-9C90CB Drug Info [51]
Darifenacin Drug Info [52]
guanylpirenzepine Drug Info [53]
hexahydrodifenidol Drug Info [54]
hexahydrosiladifenidol Drug Info [54]
LAS-34273 Drug Info [23]
lithocholylcholine Drug Info [55]
ML381 Drug Info [56]
Olterodine Drug Info [57]
Oxybutynine Drug Info [58]
p-F-HHSiD Drug Info [59]
PTAC Drug Info [57]
silahexocyclium Drug Info [54]
Solifenacin Drug Info [60]
Succinylcholine Drug Info [61], [62]
Tarafenacin Drug Info [63]
Tiotropium Drug Info [64]
Tolterodine Drug Info [65], [48]
tripitramine Drug Info [66]
TRN-157 Drug Info [51]
UH-AH 37 Drug Info [67]
VU0255035 Drug Info [68]
Zamifenacin Drug Info [69]
[3H]darifenacin Drug Info [70]
[3H]N-methyl scopolamine Drug Info [71]
[3H]QNB Drug Info [72]
[3H]tiotropium Drug Info [73]
Agonist arecaidine propargyl ester Drug Info [74]
Cevimeline Drug Info [75]
furtrethonium Drug Info [74]
J-104135 Drug Info [51]
McN-A-343 Drug Info [76]
methylfurmethide Drug Info [74]
NNC 11-1314 Drug Info [77]
NNC 11-1585 Drug Info [77]
NNC 11-1607 Drug Info [77]
oxotremorine-M Drug Info [74]
pentylthio-TZTP Drug Info [74]
SMT-D002 Drug Info [78]
Modulator (allosteric modulator) brucine Drug Info [79]
Go7874 Drug Info [80]
N-benzyl brucine Drug Info [79]
N-chloromethyl-brucine Drug Info [79]
thiochrome Drug Info [81]
vinburnine Drug Info [74]
WIN 51,708 Drug Info [82]
WIN 62,577 Drug Info [82]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Cholinergic synapse
Regulation of actin cytoskeleton
Insulin secretion
Salivary secretion
Gastric acid secretion
Pancreatic secretion
PANTHER Pathway Alzheimer disease-amyloid secretase pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Muscarinic acetylcholine receptor 1 and 3 signaling pathway
PathWhiz Pathway Gastric Acid Production
Reactome Muscarinic acetylcholine receptors
Acetylcholine regulates insulin secretion
G alpha (q) signalling events
WikiPathways Monoamine GPCRs
Calcium Regulation in the Cardiac Cell
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Integration of energy metabolism
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
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