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]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
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 [1], [2]
Benztropine Drug Info Approved Parkinson's disease [3], [4]
Biperiden Drug Info Approved Parkinsonism; Extrapyramidal disorders secondary to neuroleptic drug therapy [2]
Clidinium Drug Info Approved Abdominal stomach pain; Irritable bowel syndrome [5], [6], [2]
Cycrimine Drug Info Approved Parkinson's disease [7]
Dicyclomine Drug Info Approved Functional bowel syndrome; Irritable bowel syndrome [2]
Diphemanil Methylsulfate Drug Info Approved Peptic ulcer [8]
Fesoterodine fumarate Drug Info Approved Overactive bladder disorder [9]
Glycopyrrolate Drug Info Approved Anesthesia [10], [11]
Metixene Drug Info Approved Parkinson's disease [12], [13]
Oxyphenonium Drug Info Approved Visceral spasms [2]
Pirenzepine Drug Info Approved Peptic ulcer [14], [15]
Propantheline Drug Info Approved Excessive sweating; Stomach ulcer [16], [17], [2]
SMT-D002 Drug Info Approved Seborrhea [18]
Trihexyphenidyl Drug Info Approved Parkinson's disease; Dystonia [19], [20], [2]
Darotropium + 642444 Drug Info Phase 3 Chronic obstructive pulmonary disease [21]
Nebracetam Drug Info Phase 3 Parkinson's disease [22]
(S)-oxybutynin Drug Info Phase 2 Urinary incontinence [23]
FP-1097 Drug Info Phase 2 Urinary incontinence [24]
N-DESMETHYLCLOZAPINE Drug Info Phase 2 Schizophrenia; Schizoaffective disorders [25]
NGX-267 Drug Info Phase 2 Schizophrenia [26]
SR-46559A Drug Info Phase 2 Cognitive disorders [27]
Xanomeline tartrate Drug Info Phase 2 Parkinson's disease [28]
AC-262271 Drug Info Phase 1 Glaucoma [29]
Arecoline Drug Info Phase 1 Parkinson's disease [30], [31], [32], [33]
AZD-6088 Drug Info Phase 1 Neuropathic pain [34], [35]
GSK1034702 Drug Info Phase 1 Schizophrenia; Dementia [36]
MCD-386 Drug Info Phase 1 Alzheimer disease [37]
Thiopilocarpine Drug Info Phase 1 Cognitive disorders [38]
Telenzepine Drug Info Discontinued in Preregistration Chronic obstructive pulmonary disease [39]
Darotropium Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [40]
Declopramide Drug Info Discontinued in Phase 2 Inflammatory bowel disease [41]
Rispenzepine Drug Info Discontinued in Phase 2 Chronic obstructive pulmonary disease [42]
Talsaclidine fumarate Drug Info Discontinued in Phase 2 Alzheimer disease [43]
YM-796 Drug Info Discontinued in Phase 2 Cognitive disorders [44], [45]
PD-151832 Drug Info Discontinued in Phase 1/2 Parkinson's disease [46]
ITAMELINE Drug Info Discontinued in Phase 1 Cognitive disorders [47]
Sabcomeline Drug Info Discontinued in Phase 1 Discovery agent [48], [49]
SDZ-210-086 Drug Info Discontinued in Phase 1 Cognitive disorders [50]
TAZOMELINE Drug Info Discontinued in Phase 1 Cognitive disorders [51]
AC-260584 Drug Info Terminated Schizophrenia [52], [53]
Alvameline Drug Info Terminated Alzheimer disease [54]
HIMBACINE Drug Info Terminated Discovery agent [55], [56]
WAY-132983 Drug Info Terminated Discovery agent [57]
Antagonist (S)-oxybutynin Drug Info [58]
Benztropine Drug Info [59], [60]
Biperiden Drug Info [61]
Clidinium Drug Info [62]
Dicyclomine Drug Info [63], [64]
FP-1097 Drug Info [65]
Glycopyrrolate Drug Info [66], [67]
Oxyphenonium Drug Info [68]
Pirenzepine Drug Info [69], [70]
Propantheline Drug Info [71]
Rispenzepine Drug Info [72]
Trihexyphenidyl Drug Info [73]
Inhibitor 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info [74]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info [75]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info [76]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info [77]
2-(4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione Drug Info [78]
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info [79]
3-(3-benzylamino)-piperidin-2-one Drug Info [80]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [79]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info [81]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info [82]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [83]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info [79]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info [79]
7-Dimethylamino-hept-5-yn-2-one Drug Info [79]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info [79]
A-987306 Drug Info [84]
ACECLIDINE Drug Info [85]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [86]
AMINOBENZTROPINE Drug Info [87]
Arecoline Drug Info [88]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [89]
Bo(15)PZ Drug Info [90]
BRL-55473 Drug Info [91]
CARAMIPEN Drug Info [92]
CREMASTRINE Drug Info [93]
DIFLUOROBENZTROPINE Drug Info [82]
FLUMEZAPINE Drug Info [94]
FM1-10 Drug Info [95]
FM1-43 Drug Info [95]
GNF-PF-5618 Drug Info [96]
HIMBACINE Drug Info [97]
ISOCLOZAPINE Drug Info [98]
ISOLOXAPINE Drug Info [99]
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info [79]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info [91]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info [91]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [89]
R-dimethindene Drug Info [100]
RR(17)PZ Drug Info [90]
SULFOARECOLINE Drug Info [101]
Agonist AC-260584 Drug Info [102]
AC-262271 Drug Info [103]
AC-42 Drug Info [102]
AF150(S) Drug Info [104], [105]
AZD-6088 Drug Info [106]
BQCA Drug Info [107]
Darotropium Drug Info [108]
Darotropium + 642444 Drug Info [108]
GSK1034702 Drug Info [108]
ITAMELINE Drug Info [2]
LY-593039 Drug Info [102]
MCD-386 Drug Info [109]
Nebracetam Drug Info [110]
NGX-267 Drug Info [102]
PD-151832 Drug Info [2]
Sabcomeline Drug Info [102]
SDZ-210-086 Drug Info [111]
SMT-D002 Drug Info [112]
SR-46559A Drug Info [2]
Talsaclidine fumarate Drug Info [113], [102]
TAZOMELINE Drug Info [2]
Thiopilocarpine Drug Info [38]
WAY-132983 Drug Info [113], [102]
Xanomeline tartrate Drug Info [102], [114]
Modulator Alvameline Drug Info [54]
DAU-5750 Drug Info
DAU-5884 Drug Info
DAU-6202 Drug Info
Declopramide Drug Info [115]
Diphemanil Methylsulfate Drug Info [116]
Fesoterodine fumarate Drug Info [2]
hexocyclium Drug Info
Metixene Drug Info
N-DESMETHYLCLOZAPINE Drug Info
Telenzepine Drug Info [117]
YM-796 Drug Info
Binder Cycrimine Drug Info [118]
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 1(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 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040103.
REF 4(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 5(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 6Drug information of Clidinium, 2008. eduDrugs.
REF 7Drug information of Cycrimine, 2008. eduDrugs.
REF 8Drug information of Diphemanil Methylsulfate, 2008. eduDrugs.
REF 92008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
REF 10FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040568.
REF 11(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 12(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 13Drug information of Metixene, 2008. eduDrugs.
REF 14Autonomic 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 15(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 16FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080927.
REF 17(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 18Clinical pipeline report, company report or official report of Summit.
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REF 20(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 21ClinicalTrials.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 22Nefiracetam ameliorates associative learning impairment in the scopolamine-injected older rabbit. Med Sci Monit. 2002 Apr;8(4):BR105-12.
REF 23A 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 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019662)
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REF 26ClinicalTrials.gov (NCT00637793) Study of NGX267 Oral Capsules in Patients With Xerostomia Associated With Sjorgren's Syndrome. U.S. National Institutes of Health.
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001599)
REF 28The 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 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033965)
REF 30Arecoline excites rat locus coeruleus neurons by activating the M2-muscarinic receptor. Chin J Physiol. 2000 Mar 31;43(1):23-8.
REF 31M1 receptor activation is a requirement for arecoline analgesia. Farmaco. 2001 May-Jul;56(5-7):383-5.
REF 32Arecoline excites the colonic smooth muscle motility via M3 receptor in rabbits. Chin J Physiol. 2004 Jun 30;47(2):89-94.
REF 33(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 34ClinicalTrials.gov (NCT00931541) AZD6088 Single Ascending Dose Study. U.S. National Institutes of Health.
REF 35(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 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028844)
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009639)
REF 38SDZ 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 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000603)
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REF 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007055)
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003718)
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001956)
REF 44(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 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001332)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006926)
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004062)
REF 48(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 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003824)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001734)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006554)
REF 52(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 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016553)
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REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006949)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009638)
REF 58Enantiomers 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 59Muscarinic 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 60Formulation and biopharmaceutical evaluation of transdermal patch containing benztropine. Int J Pharm. 2008 Jun 5;357(1-2):55-60. Epub 2008 Jan 20.
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REF 62Accidental acute clidinium toxicity. Emerg Med J. 2009 Jun;26(6):460.
REF 63Fustin flavonoid attenuates beta-amyloid (1-42)-induced learning impairment. J Neurosci Res. 2009 Jun 16.
REF 64Characterization of undifferentiated muscarinic thyroid cells in Fisher rats.. Endocrinol Nutr. 2009 Mar;56(3):106-11. Epub 2009 May 18.
REF 65Clinical pipeline report, company report or official report of FemmePharma.
REF 66A pharmacological profile of glycopyrrolate: interactions at the muscarinic acetylcholine receptor. Gen Pharmacol. 1992 Nov;23(6):1165-70.
REF 67Autonomic cardiovascular control during a novel pharmacologic alternative to ganglionic blockade. Clin Pharmacol Ther. 2008 May;83(5):692-701. Epub 2007 Aug 8.
REF 68Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999 Aug;88(8):759-62.
REF 69The 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 70Negative 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 71Involvement 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 72Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea. Am J Respir Crit Care Med. 1995 Sep;152(3):872-8.
REF 73The 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 74J 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 75Bioorg 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 76J 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 77J 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 78Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives, Bioorg. Med. Chem. Lett. 7(8):979-984 (1997).
REF 79Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5, Bioorg. Med. Chem. Lett. 2(8):803-808 (1992).
REF 80J 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 81J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
REF 82J 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 83J 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 84J 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 85J 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 86J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
REF 87J 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.
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