Target Information

Target General Infomation
Target ID
T50918
Former ID
TTDS00006
Target Name
Muscarinic acetylcholine receptor M5
Gene Name
CHRM4
Synonyms
M5 receptor; CHRM4
Target Type
Successful
Disease Acquired nystagmus [ICD9: 379.5; ICD10: H55]
Alzheimer disease [ICD9: 331; ICD10: G30]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Bronchodilator [ICD9: 493; ICD10: J45]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cough [ICD9: 786.2; ICD10: R05]
Central and peripheral nervous diseases [ICD10: G96.9]
Dysuria; Urgency; Nocturia; Suprapubic pain [ICD10: R300, R35]
Depression [ICD9: 311; ICD10: F30-F39]
Gastrointestinal disease [ICD10: K00-K93]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Gastric motility disorder; Spasm [ICD9:728.85; ICD10: K22.4, R25.2]
Hypertension [ICD9: 401; ICD10: I10-I16]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Moderate and severe psychomotor agitation [ICD code not available]
Overactive bladder disorder; Spasm [ICD9:188, 596.51, 728.85; ICD10: C67, N32.81, R25.2]
Organophosphate poisoning [ICD9: 989.3; ICD10: T60.0]
Poison intoxication [ICD10: T36-T50]
Peptic ulcer disease; Irritable bowel syndrome; Pancreatitis; Gastritis [ICD10: K58, K85, K86, K29.0-K29.7]
Parkinson's disease [ICD9: 332; ICD10: G20]
Produce mydriasis and cycloplegia for diagnostic purposes [ICD10: H57.04]
Peptic ulcer; Gastrointestinal disease [ICD9:531-534; ICD10: K25-K27, K00-K93]
Peptic ulcer; Uveitis [ICD9:531-534, 364; ICD10: K25-K27, H20]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Schizophrenia [ICD9: 295; ICD10: F20]
Urinary retention [ICD9: 788.2; ICD10: R33]
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
T50918
UniProt ID
P08173
Sequence
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
Drugs and Mode of Action
Drug(s) ACECLIDINE Drug Info Approved Glaucoma [1], [2]
Anisodine Drug Info Approved Central and peripheral nervous diseases [2]
Anisotropine Methylbromide Drug Info Approved Peptic ulcer [3], [2]
Atropine Drug Info Approved Organophosphate poisoning [4], [5]
Bethanechol Drug Info Approved Urinary retention [6], [7]
Cimetropium bromide Drug Info Approved Gastric motility disorder; Spasm [2]
Cryptenamine Acetates Drug Info Approved Hypertension [2]
Cyclopentolate Drug Info Approved Produce mydriasis and cycloplegia for diagnostic purposes [2]
Flavoxate Drug Info Approved Dysuria; Urgency; Nocturia; Suprapubic pain [2]
Flutropium bromide Drug Info Approved Cough [2]
Homatropine Methylbromide Drug Info Approved Peptic ulcer; Uveitis [8], [2]
Hyoscyamine Drug Info Approved Gastrointestinal disease [9]
Ispaghula Drug Info Approved Irritable bowel syndrome [9]
Mebeverine Drug Info Approved Irritable bowel syndrome [9]
Mepenzolate Drug Info Approved Peptic ulcer; Gastrointestinal disease [10], [2]
Methantheline Drug Info Approved Peptic ulcer disease; Irritable bowel syndrome; Pancreatitis; Gastritis [2]
Oxitropium bromide Drug Info Approved Bronchodilator [2]
Oxyphencyclimine Drug Info Approved Peptic ulcer [11], [12], [2]
Pilocarpine Drug Info Approved Glaucoma [13], [14]
Procyclidine Drug Info Approved Parkinson's disease [15], [16]
Promazine Drug Info Approved Moderate and severe psychomotor agitation [2]
Tridihexethyl Drug Info Approved Acquired nystagmus [17]
Trospium Drug Info Approved Overactive bladder disorder; Spasm [18], [19], [20], [21], [2]
Umeclidinium Drug Info Approved Chronic obstructive pulmonary disease [22], [23]
Hyoscine Drug Info Phase 4 Discovery agent [24]
L-651582 Drug Info Phase 3 Solid tumours [25]
OrM3 Drug Info Phase 2b Chronic obstructive pulmonary disease [26]
GSK233705 Drug Info Phase 2 Chronic obstructive pulmonary disease [26]
Atropine Drug Info Phase 1 Poison intoxication [27], [5], [2]
Org-23366 Drug Info Preclinical Schizophrenia [28]
Benactyzine Drug Info Withdrawn from market Depression [29]
RS 86 Drug Info Terminated Alzheimer disease [30]
Inhibitor 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info [31]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info [32]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info [33]
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info [34]
3-(3-benzylamino)-piperidin-2-one Drug Info [35]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [34]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info [36]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [37]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info [34]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info [34]
7-Dimethylamino-hept-5-yn-2-one Drug Info [34]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [34]
ACECLIDINE Drug Info [38]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [39]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [39]
BRL-55473 Drug Info [40]
CREMASTRINE Drug Info [41]
FLUMEZAPINE Drug Info [42]
FM1-10 Drug Info [43]
FM1-43 Drug Info [43]
GNF-PF-5618 Drug Info [44]
ISOCLOZAPINE Drug Info [45]
ISOLOXAPINE Drug Info [46]
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info [34]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info [40]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info [40]
PF-3409409 Drug Info [47]
SULFOARECOLINE Drug Info [48]
VU0119498 Drug Info [49]
VU0238429 Drug Info [49]
Modulator Anisodine Drug Info [50]
Cimetropium bromide Drug Info [51], [52]
Cryptenamine Acetates Drug Info [53]
Flutropium bromide Drug Info [52]
L-651582 Drug Info [25]
Oxitropium bromide Drug Info [52]
Umeclidinium Drug Info [22]
Binder Anisotropine Methylbromide Drug Info [54]
Oxyphencyclimine Drug Info [55]
Promazine Drug Info [56]
Tridihexethyl Drug Info [57]
Antagonist Aprophen Drug Info [58], [59]
Atropine Drug Info [60], [61], [62], [59]
Benactyzine Drug Info [59]
Cyclopentolate Drug Info [63]
Flavoxate Drug Info [64]
GSK233705 Drug Info [26]
Homatropine Methylbromide Drug Info [65]
Hyoscine Drug Info [66]
Hyoscyamine Drug Info [67]
Ispaghula Drug Info [9]
Mebeverine Drug Info [9]
Mepenzolate Drug Info [68]
Methantheline Drug Info [69]
Org-23366 Drug Info [28]
OrM3 Drug Info [26]
Procyclidine Drug Info [70]
Trospium Drug Info [65]
Agonist Bethanechol Drug Info [71], [72], [73]
Muscarine Drug Info [60]
Pilocarpine Drug Info [74], [75]
RS 86 Drug Info [76]
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
PANTHER Pathway Alzheimer disease-amyloid secretase pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Reactome Muscarinic acetylcholine receptors
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
GPCR ligand binding
GPCR downstream signaling
References
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