Target Information

Target General Infomation
Target ID
T28893
Former ID
TTDS00002
Target Name
Muscarinic acetylcholine receptor M1
Gene Name
CHRM1
Synonyms
M1 receptor; CHRM1
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Anesthesia [ICD9: 338; ICD10: R20.0]
Abdominal stomach pain; Irritable bowel syndrome [ICD9:789.0, 338, 780, 564.1, 787.91; ICD10: R10, G89, R52, A09, K58, K59.1]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Excessive sweating; Stomach ulcer [ICD9:780.8; ICD10: R61, K25-K27]
Functional bowel syndrome; Irritable bowel syndrome [ICD10: K58]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Parkinson's disease [ICD9: 332; ICD10: G20]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
Parkinson's disease; Dystonia [ICD9:332; ICD10: G20, G24]
Parkinsonism; Extrapyramidal disorders secondary to neuroleptic drug therapy [ICD10: F06]
Schizophrenia; Dementia [ICD9: 290-294, 295; ICD10: F01-F07, F20]
Seborrhea [ICD10: L21]
Schizophrenia [ICD9: 295; ICD10: F20]
Schizophrenia; Schizoaffective disorders [ICD9: 295, 295.70; ICD10: F20, F25]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Visceral spasms [ICD10: R25.2]
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
T28893
UniProt ID
P11229
Sequence
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI
SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR
TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF
YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM
KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE
TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR
MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN
PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL
Drugs and Mode of Action
Drug(s) ACECLIDINE Drug Info Approved Glaucoma [539906], [551871]
Benztropine Drug Info Approved Parkinson's disease [538165], [542590]
Biperiden Drug Info Approved Parkinsonism; Extrapyramidal disorders secondary to neuroleptic drug therapy [551871]
Clidinium Drug Info Approved Abdominal stomach pain; Irritable bowel syndrome [540498], [550751], [551871]
Cycrimine Drug Info Approved Parkinson's disease [550740]
Dicyclomine Drug Info Approved Functional bowel syndrome; Irritable bowel syndrome [551871]
Diphemanil Methylsulfate Drug Info Approved Peptic ulcer [550746]
Fesoterodine fumarate Drug Info Approved Overactive bladder disorder [529941]
Glycopyrrolate Drug Info Approved Anesthesia [538189], [542483]
Metixene Drug Info Approved Parkinson's disease [542248], [550770]
Oxyphenonium Drug Info Approved Visceral spasms [551871]
Pirenzepine Drug Info Approved Peptic ulcer [535729], [540243]
Propantheline Drug Info Approved Excessive sweating; Stomach ulcer [538344], [540253], [551871]
SMT-D002 Drug Info Approved Seborrhea [551707]
Trihexyphenidyl Drug Info Approved Parkinson's disease; Dystonia [536923], [542338], [551871]
Darotropium + 642444 Drug Info Phase 3 Chronic obstructive pulmonary disease [523399]
Nebracetam Drug Info Phase 3 Parkinson's disease [526312]
(S)-oxybutynin Drug Info Phase 2 Urinary incontinence [525400]
FP-1097 Drug Info Phase 2 Urinary incontinence [547822]
N-DESMETHYLCLOZAPINE Drug Info Phase 2 Schizophrenia; Schizoaffective disorders [540289]
NGX-267 Drug Info Phase 2 Schizophrenia [522264]
SR-46559A Drug Info Phase 2 Cognitive disorders [544940]
Xanomeline tartrate Drug Info Phase 2 Parkinson's disease [531668]
AC-262271 Drug Info Phase 1 Glaucoma [549229]
Arecoline Drug Info Phase 1 Parkinson's disease [525796], [526115], [527244], [539971]
AZD-6088 Drug Info Phase 1 Neuropathic pain [522711], [542767]
GSK1034702 Drug Info Phase 1 Schizophrenia; Dementia [548788]
MCD-386 Drug Info Phase 1 Alzheimer disease [546687]
Thiopilocarpine Drug Info Phase 1 Cognitive disorders [526908]
Telenzepine Drug Info Discontinued in Preregistration Chronic obstructive pulmonary disease [544690]
Darotropium Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [525365]
Declopramide Drug Info Discontinued in Phase 2 Inflammatory bowel disease [546239]
Rispenzepine Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [545564]
Talsaclidine fumarate Drug Info Discontinued in Phase 2 Alzheimer disease [545043]
YM-796 Drug Info Discontinued in Phase 2 Cognitive disorders [539895], [544855]
PD-151832 Drug Info Discontinued in Phase 1/2 Parkinson's disease [546217]
ITAMELINE Drug Info Discontinued in Phase 1 Cognitive disorders [545662]
Sabcomeline Drug Info Discontinued in Phase 1 Discovery agent [540062], [545592]
SDZ-210-086 Drug Info Discontinued in Phase 1 Cognitive disorders [544969]
TAZOMELINE Drug Info Discontinued in Phase 1 Cognitive disorders [546138]
AC-260584 Drug Info Terminated Schizophrenia [540298], [547460]
Alvameline Drug Info Terminated Alzheimer disease [534674]
HIMBACINE Drug Info Terminated Discovery agent [540212], [546219]
WAY-132983 Drug Info Terminated Discovery agent [546686]
Antagonist (S)-oxybutynin Drug Info [530541]
Benztropine Drug Info [536453], [536690]
Biperiden Drug Info [535016]
Clidinium Drug Info [537371]
Dicyclomine Drug Info [537482], [537630]
FP-1097 Drug Info [549828]
Glycopyrrolate Drug Info [535754], [536471]
Oxyphenonium Drug Info [534888]
Pirenzepine Drug Info [535794], [537295]
Propantheline Drug Info [536001]
Rispenzepine Drug Info [537849]
Trihexyphenidyl Drug Info [536802]
Inhibitor 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info [533345]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info [530266]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info [527029]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info [534723]
2-(4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione Drug Info [551341]
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info [551235]
3-(3-benzylamino)-piperidin-2-one Drug Info [528735]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [551235]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info [527344]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info [528473]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info [551235]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info [551235]
7-Dimethylamino-hept-5-yn-2-one Drug Info [551235]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [551235]
A-987306 Drug Info [529789]
ACECLIDINE Drug Info [534044]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [534645]
AMINOBENZTROPINE Drug Info [534349]
Arecoline Drug Info [551393]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [525826]
Bo(15)PZ Drug Info [527889]
BRL-55473 Drug Info [551234]
CARAMIPEN Drug Info [529957]
CREMASTRINE Drug Info [527523]
DIFLUOROBENZTROPINE Drug Info [528473]
FLUMEZAPINE Drug Info [533165]
FM1-10 Drug Info [529178]
FM1-43 Drug Info [529178]
GNF-PF-5618 Drug Info [527653]
HIMBACINE Drug Info [527126]
ISOCLOZAPINE Drug Info [530313]
ISOLOXAPINE Drug Info [533577]
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info [551235]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info [551234]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info [551234]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [525826]
R-dimethindene Drug Info [530300]
RR(17)PZ Drug Info [527889]
SULFOARECOLINE Drug Info [533450]
Agonist AC-260584 Drug Info [537030]
AC-262271 Drug Info [550343]
AC-42 Drug Info [537030]
AF150(S) Drug Info [535833], [536601]
AZD-6088 Drug Info [544266]
BQCA Drug Info [540839]
Darotropium Drug Info [550963]
Darotropium + 642444 Drug Info [550963]
GSK1034702 Drug Info [550963]
ITAMELINE Drug Info [551871]
LY-593039 Drug Info [537030]
MCD-386 Drug Info [527660]
Nebracetam Drug Info [530866]
NGX-267 Drug Info [537030]
PD-151832 Drug Info [551871]
Sabcomeline Drug Info [537030]
SDZ-210-086 Drug Info [533965]
SMT-D002 Drug Info [527286]
SR-46559A Drug Info [551871]
Talsaclidine fumarate Drug Info [535511], [537030]
TAZOMELINE Drug Info [551871]
Thiopilocarpine Drug Info [526908]
WAY-132983 Drug Info [535511], [537030]
Xanomeline tartrate Drug Info [537030], [538104]
Modulator Alvameline Drug Info [534674]
DAU-5750 Drug Info
DAU-5884 Drug Info
DAU-6202 Drug Info
Declopramide Drug Info [525463]
Diphemanil Methylsulfate Drug Info [556264]
Fesoterodine fumarate Drug Info [551871]
hexocyclium Drug Info
Metixene Drug Info
N-DESMETHYLCLOZAPINE Drug Info
Telenzepine Drug Info [533879]
YM-796 Drug Info
Binder Cycrimine Drug Info [537692]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
PI3K-Akt signaling pathway
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
Muscarinic acetylcholine receptor 1 and 3 signaling 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
Secretion of Hydrochloric Acid in Parietal Cells
GPCR ligand binding
GPCR downstream signaling
References
Ref 522264ClinicalTrials.gov (NCT00637793) Study of NGX267 Oral Capsules in Patients With Xerostomia Associated With Sjorgren's Syndrome. U.S. National Institutes of Health.
Ref 522711ClinicalTrials.gov (NCT00931541) AZD6088 Single Ascending Dose Study. U.S. National Institutes of Health.
Ref 523399ClinicalTrials.gov (NCT01316900) 24-week Trial Comparing GSK573719/GW642444 With GW642444 and With Tiotropium in Chronic Obstructive Pulmonary Disease. U.S. National Institutes of Health.
Ref 525365Medicinal chemistry and therapeutic potential of muscarinic M3 antagonists. Med Res Rev. 2009 Nov;29(6):867-902.
Ref 525400A phase 2, randomized, double-blind, efficacy and safety study of oxybutynin vaginal ring for alleviation of overactive bladder symptoms in women. J Urol. 2014 Apr;191(4):1014-21.
Ref 525796Arecoline excites rat locus coeruleus neurons by activating the M2-muscarinic receptor. Chin J Physiol. 2000 Mar 31;43(1):23-8.
Ref 526115M1 receptor activation is a requirement for arecoline analgesia. Farmaco. 2001 May-Jul;56(5-7):383-5.
Ref 526312Nefiracetam ameliorates associative learning impairment in the scopolamine-injected older rabbit. Med Sci Monit. 2002 Apr;8(4):BR105-12.
Ref 526908SDZ ENS 163, a selective muscarinic M1 receptor agonist, facilitates the induction of long-term potentiation in rat hippocampal slices. Eur J Pharmacol. 1992 Nov 3;222(1):21-5.
Ref 527244Arecoline excites the colonic smooth muscle motility via M3 receptor in rabbits. Chin J Physiol. 2004 Jun 30;47(2):89-94.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 531668The M1/M4 preferring agonist xanomeline is analgesic in rodent models of chronic inflammatory and neuropathic pain via central site of action. Pain. 2011 Dec;152(12):2852-60.
Ref 534674In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro. Psychopharmacology (Berl). 1998 Jun;137(3):233-40.
Ref 535729Autonomic modulation during acute myocardial ischemia by low-dose pirenzepine in conscious dogs with a healed myocardial infarction: a comparison with beta-adrenergic blockade. J Cardiovasc Pharmacol. 2003 May;41(5):671-7.
Ref 536923Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
Ref 538165FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040103.
Ref 538189FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040568.
Ref 538344FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080927.
Ref 539895(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. (Ligand id: 287).
Ref 539906(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. (Ligand id: 288).
Ref 539971(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. (Ligand id: 296).
Ref 540062(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. (Ligand id: 306).
Ref 540212(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. (Ligand id: 324).
Ref 540243(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. (Ligand id: 328).
Ref 540253(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. (Ligand id: 329).
Ref 540289(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. (Ligand id: 333).
Ref 540298(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. (Ligand id: 334).
Ref 540498(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. (Ligand id: 366).
Ref 542248(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. (Ligand id: 7232).
Ref 542338(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. (Ligand id: 7315).
Ref 542483(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. (Ligand id: 7459).
Ref 542590(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. (Ligand id: 7601).
Ref 542767(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. (Ligand id: 7822).
Ref 544690Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000603)
Ref 544855Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001332)
Ref 544940Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001599)
Ref 544969Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001734)
Ref 545043Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001956)
Ref 545564Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003718)
Ref 545592Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003824)
Ref 545662Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004062)
Ref 546138Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006554)
Ref 546217Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006926)
Ref 546219Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006949)
Ref 546239Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007055)
Ref 546686Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009638)
Ref 546687Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009639)
Ref 547460Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016553)
Ref 547822Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019662)
Ref 548788Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028844)
Ref 549229Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033965)
Ref 550740Drug information of Cycrimine, 2008. eduDrugs.
Ref 550746Drug information of Diphemanil Methylsulfate, 2008. eduDrugs.
Ref 550751Drug information of Clidinium, 2008. eduDrugs.
Ref 550770Drug information of Metixene, 2008. eduDrugs.
Ref 551707Clinical pipeline report, company report or official report of Summit.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525463Pharmacokinetics and central nervous system toxicity of declopramide (3-chloroprocainamide) in rats and mice. Anticancer Drugs. 1999 Jan;10(1):79-88.
Ref 525826J 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.
Ref 526908SDZ ENS 163, a selective muscarinic M1 receptor agonist, facilitates the induction of long-term potentiation in rat hippocampal slices. Eur J Pharmacol. 1992 Nov 3;222(1):21-5.
Ref 527029J 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.
Ref 527126Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70.Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Ref 527286Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
Ref 527344J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
Ref 527523J Nat Prod. 2005 Apr;68(4):572-3.Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.
Ref 527653J 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.
Ref 527660The processing of the selective M1 agonist CDD-0102-J by human hepatic drug metabolizing enzymes. Am J Ther. 2005 Jul-Aug;12(4):300-5.
Ref 527889J Med Chem. 2005 Dec 1;48(24):7847-59.On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.
Ref 528473J Med Chem. 2006 Oct 19;49(21):6391-9.Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
Ref 528735J 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.
Ref 529178Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist.
Ref 529789J 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.
Ref 529957J Med Chem. 1991 Oct;34(10):2984-9.Muscarinic receptor binding profile of para-substituted caramiphen analogues.
Ref 530266Bioorg 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.
Ref 530300J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Ref 530313J Med Chem. 1990 Feb;33(2):809-14.Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
Ref 530541Enantiomers of oxybutynin: in vitro pharmacological characterization at M1, M2 and M3 muscarinic receptors and in vivo effects on urinary bladder contraction, mydriasis and salivary secretion in guinea pigs. J Pharmacol Exp Ther. 1991 Feb;256(2):562-7.
Ref 530866Effects of nebracetam (WEB 1881 FU), a novel nootropic, as a M1-muscarinic agonist. Jpn J Pharmacol. 1991 Jan;55(1):177-80.
Ref 531079J 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.
Ref 533165J 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.
Ref 533345J Med Chem. 1989 May;32(5):1057-62.Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
Ref 533450J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Ref 533577J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.
Ref 533879Effect of telenzepine, an M1-selective muscarinic receptor antagonist, in patients with nocturnal asthma. Pulm Pharmacol. 1994 Apr;7(2):91-7.
Ref 533965Influence of the cholinergic agonist SDZ 210-086 on sleep in healthy subjects. Neuropsychopharmacology. 1993 Nov;9(3):225-32.
Ref 534044J 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.
Ref 534349J Med Chem. 1997 Mar 14;40(6):851-7.3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.
Ref 534645J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Ref 534674In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro. Psychopharmacology (Berl). 1998 Jun;137(3):233-40.
Ref 534723J 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.
Ref 534888Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
Ref 535016Evaluation of in vivo binding properties of 3H-NMPB and 3H-QNB in mouse brain. J Neural Transm. 1999;106(7-8):583-92.
Ref 535511Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine. Psychopharmacology (Berl). 2002 Jul;162(3):292-300. Epub 2002 May 29.
Ref 535754A pharmacological profile of glycopyrrolate: interactions at the muscarinic acetylcholine receptor. Gen Pharmacol. 1992 Nov;23(6):1165-70.
Ref 535794The effect of muscarinic receptor blockers on non-specific bronchial reactivity in patients with bronchial asthma. Pneumonol Alergol Pol. 1992;60(11-12):32-6.
Ref 535833M1 muscarinic agonists can modulate some of the hallmarks in Alzheimer's disease: implications in future therapy. J Mol Neurosci. 2003;20(3):349-56.
Ref 536001Involvement of the peripheral cholinergic muscarinic system in the compensatory ovarian hypertrophy in the rat. Exp Biol Med (Maywood). 2004 Sep;229(8):793-805.
Ref 536453Muscarinic preferential M(1) receptor antagonists enhance the discriminative-stimulus effects of cocaine in rats. Pharmacol Biochem Behav. 2007 Oct;87(4):400-4. Epub 2007 Jun 2.
Ref 536471Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701. Epub 2007 Aug 8.
Ref 536601M1 muscarinic agonists target major hallmarks of Alzheimer's disease--an update. Curr Alzheimer Res. 2007 Dec;4(5):577-80.
Ref 536690Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60. Epub 2008 Jan 20.
Ref 536802The role of M1 muscarinic cholinergic receptors in the discriminative stimulus properties of N-desmethylclozapine and the atypical antipsychotic drug clozapine in rats. Psychopharmacology (Berl). 2009 Apr;203(2):295-301. Epub 2008 Aug 7.
Ref 537030Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists. Eur J Pharmacol. 2009 Mar 1;605(1-3):53-6. Epub 2009 Jan 11.
Ref 537295Negative crosstalk between M1 and M2 muscarinic autoreceptors involves endogenous adenosine activating A1 receptors at the rat motor endplate. Neurosci Lett. 2009 Aug 14;459(3):127-31. Epub 2009 May7.
Ref 537371Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
Ref 537482Fustin flavonoid attenuates beta-amyloid (1-42)-induced learning impairment. J Neurosci Res. 2009 Jun 16.
Ref 537630Characterization of undifferentiated muscarinic thyroid cells in Fisher rats.. Endocrinol Nutr. 2009 Mar;56(3):106-11. Epub 2009 May 18.
Ref 537692Capillary gas chromatography of trihexyphenidyl, procyclidine and cycrimine in biological fluids. J Chromatogr. 1989 Sep 29;494:135-42.
Ref 537849Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea. Am J Respir Crit Care Med. 1995 Sep;152(3):872-8.
Ref 538104On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor. Mol Pharmacol. 1998 Jun;53(6):1120-30.
Ref 540839(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. (Ligand id: 5436).
Ref 544266Evaluation of an Innovative Population Pharmacokinetic-Based Design for Behavioral Pharmacodynamic Endpoints. AAPS J. 2012 December; 14(4): 657-663.
Ref 549828Clinical pipeline report, company report or official report of FemmePharma.
Ref 550343Phase I clinical trial of muscarinic agonist (AC-262271) for treating glaucoma. Acadia Pharmaceuticals.
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551234A novel and selective class of azabicyclic muscarinic agonists incorporating an N-methoxy imidoyl halide or nitrile functionality, Bioorg. Med. Chem. Lett. 2(8):791-796 (1992).
Ref 551235Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5, Bioorg. Med. Chem. Lett. 2(8):803-808 (1992).
Ref 551341Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives, Bioorg. Med. Chem. Lett. 7(8):979-984 (1997).
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.