Target Information

Target General Infomation
Target ID
T79961
Former ID
TTDI01755
Target Name
Acetylcholine receptor
Gene Name
CHRM5
Synonyms
CHRM1; Muscarinic acetylcholine receptor M1; CHRM5
Target Type
Successful
Disease Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Amnesia [ICD10: F04]
Brain diseases [ICD10: G00-G99]
Central and peripheral nervous diseases [ICD10: G96.9]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Colitis [ICD9: 556.9; ICD10: K50-K52]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Myasthenia gravis [ICD9: 358; ICD10: G70.0]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Stomach ulcer [ICD10: K25-K27]
Schizophrenia [ICD9: 295; ICD10: F20]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
BioChemical Class
GPCR rhodopsin
UniProt ID
P08912
Sequence
MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQ
LKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMN
LLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPL
DECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAE
KRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQL
TTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPN
YLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNP
NPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLG
YWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP
Structure
1Y5P; 1Y5T; 1Y6C
Drugs and Mode of Action
Drug(s) Belladonna Drug Info Approved Colitis [551871]
Butylscopolamine Drug Info Approved Dysmenorrhea [551871]
Choline alfoscerate Drug Info Approved Amnesia [551871]
Emepronium Drug Info Approved Urinary incontinence [551871]
Prifinium Drug Info Approved Irritable bowel syndrome [551871]
Propiverine Drug Info Approved Urinary incontinence [551871]
Pramiracetam Drug Info Approved (orphan drug) Brain diseases [551871]
Dexpirronium Drug Info Phase 1 Chronic obstructive pulmonary disease [548759]
BMS-181168 Drug Info Discontinued in Phase 2 Cognitive disorders [544848]
DDP-200 Drug Info Discontinued in Phase 2 Urinary incontinence [547888]
FK-584 Drug Info Discontinued in Phase 2 Central and peripheral nervous diseases [546161]
AM-831 Drug Info Discontinued in Phase 1 Schizophrenia [547459]
SU-740 Drug Info Terminated Stomach ulcer [545835]
Blocker (channel blocker) A-867744 Drug Info [530093]
NS1738 Drug Info [528946]
Antagonist alpha-conotoxin AuIB Drug Info [543844]
alpha-conotoxin GI Drug Info [543844]
alpha-conotoxin PnIA Drug Info [543844]
Dexpirronium Drug Info [543844]
Propiverine Drug Info [525517], [551871]
Agonist AM-831 Drug Info [550322]
[125I]epibatidine Drug Info [543844]
[3H]cytisine Drug Info [543844]
[3H]epibatidine Drug Info [543844]
Modulator Belladonna Drug Info [530253], [551871]
BHT-3034 Drug Info [543844]
BMS-181168 Drug Info [534294]
Butylscopolamine Drug Info [533864], [551871]
Choline alfoscerate Drug Info [543844]
CRTX-070 Drug Info [543844]
DDP-200 Drug Info [550848]
Emepronium Drug Info [533659], [551871]
FK-584 Drug Info [550892]
JWB-1-84-1 Drug Info [543844]
Pramiracetam Drug Info [550025], [551871]
Prifinium Drug Info [533658], [551871]
Recombinant botulinum toxin Drug Info [543844]
SU-740 Drug Info [551752]
Topical anticholinergics Drug Info [543844]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Reactome Muscarinic acetylcholine receptors
Acetylcholine regulates insulin secretion
Highly sodium permeable acetylcholine nicotinic receptors
Highly calcium permeable postsynaptic nicotinic acetylcholine receptors
WikiPathways Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
References
Ref 544848Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001318)
Ref 545835Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004989)
Ref 546161Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006686)
Ref 547459Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016551)
Ref 547888Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020170)
Ref 548759Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028438)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525517Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 1999;64(25):2351-8.
Ref 528946An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307. Epub 2007 Jul 11.
Ref 530093J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. Epub 2009 Apr 23.In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Ref 530253Plasma level of atropine after accidental ingestion of Atropa belladonna. Clin Toxicol (Phila). 2009 Jul;47(6):602-4.
Ref 533658Ligand binding properties of muscarinic acetylcholine receptor subtypes (m1-m5) expressed in baculovirus-infected insect cells. J Pharmacol Exp Ther. 1995 Jul;274(1):378-84.
Ref 533659Classification of the presynaptic muscarinic receptor subtype that regulates 3H-acetylcholine secretion in the guinea pig urinary bladder in vitro. J Pharmacol Exp Ther. 1995 Jul;274(1):458-68.
Ref 533864Comparison of pharmacological effects of L- and DL-n-butyl-scopolamine in rat uterus. Yao Xue Xue Bao. 1994;29(1):24-7.
Ref 534294Efficacy and safety of BMY 21,502 in Alzheimer disease. Ann Pharmacother. 1996 Dec;30(12):1376-80.
Ref 543844(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 467).
Ref 550025Some neurochemical properties of pramiracetam (CI-879), a new cognition-enhancing agent. Article first published online: 5 OCT 2004.
Ref 550322Clinical pipeline report, company report or official report of Avarx.
Ref 550848CA patent application no. 753057, Sustained release oral dosage forms of an r-baclofen prodrug.
Ref 550892US patent application no. 2005,0261,328, Pharmaceutical composition comprising beta-3-adrenoceptor-agonists and antimuscarinic agents.
Ref 551752SU-840, a novel synthetic flavonoid derivative of sophoradin, with potent gastroprotective and ulcer healing activity. Journal of physiology and pharmacology. 49:1 1998 Mar pg 83-98
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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