Target Information
Target General Infomation | |||||
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Target ID |
T67684
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Former ID |
TTDS00004
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Target Name |
Muscarinic acetylcholine receptor M3
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Gene Name |
CHRM3
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Synonyms |
M3 receptor; CHRM3
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Target Type |
Successful
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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] | |||||
Obstructive lung diseases [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Overactive bladder [ICD9: 596.51; ICD10: N32.81] | |||||
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81] | |||||
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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T67684
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UniProt ID | |||||
Sequence |
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL |
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Structure |
2CSA
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Drugs and Mode of Action | |||||
Drug(s) | ACECLIDINE | Drug Info | Approved | Glaucoma | [539906], [551871] |
Cevimeline | Drug Info | Approved | Sjogren's syndrome | [535986] | |
Darifenacin | Drug Info | Approved | Overactive bladder disorder | [527466], [536361], [540188] | |
Ipratropium | Drug Info | Approved | Obstructive lung diseases | [536527], [540223] | |
LAS-34273 | Drug Info | Approved | Chronic obstructive pulmonary disease | [530127], [532210] | |
Methacholine Chloride | Drug Info | Approved | Diagnosing bronchial hyperreactivity | [551871] | |
Methscopolamine Bromide | Drug Info | Approved | Postoperative nausea and vomiting | [551871] | |
SMT-D002 | Drug Info | Approved | Seborrhea | [551707] | |
Solifenacin | Drug Info | Approved | Overactive bladder disorder | [538568], [542506] | |
Succinylcholine | Drug Info | Approved | Spasms; Pain | [538408], [540621], [551871] | |
Tiotropium | Drug Info | Approved | Chronic obstructive pulmonary disease | [536361], [540500] | |
Tolterodine | Drug Info | Approved | Overactive bladder | [551871] | |
(R)-mequitazine (incontinence/respiratory disease), Pierre Fabre | Drug Info | Phase 2 | Respiratory disease | [524448] | |
Tarafenacin | Drug Info | Phase 2 | Overactive bladder disorder | [523669] | |
TRN-157 | Drug Info | Phase 2 | Chronic obstructive pulmonary disease | [525108] | |
CHF 5407 | Drug Info | Phase 1 | Chronic obstructive pulmonary disease | [537130] | |
Zamifenacin | Drug Info | Discontinued in Phase 3 | Urinary incontinence | [545544] | |
PSD-506 | Drug Info | Discontinued in Phase 2 | Overactive bladder disorder | [548196] | |
Revatropate | Drug Info | Discontinued in Phase 1 | Chronic obstructive pulmonary disease | [536223] | |
Alvameline | Drug Info | Terminated | Alzheimer disease | [534674] | |
Modulator | (R)-mequitazine (incontinence/respiratory disease), Pierre Fabre | Drug Info | |||
Alvameline | Drug Info | [534674] | |||
CHF 5407 | Drug Info | ||||
DAU-5750 | Drug Info | ||||
DAU-5884 | Drug Info | ||||
Ipratropium | Drug Info | ||||
Methacholine Chloride | Drug Info | [526519] | |||
Methscopolamine Bromide | Drug Info | ||||
PSD-506 | Drug Info | [1572591] | |||
Revatropate | Drug Info | ||||
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-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] | |||
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] | |||
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester | Drug Info | [525826] | |||
BRL-55473 | Drug Info | [551234] | |||
CREMASTRINE | Drug Info | [527523] | |||
FLUMEZAPINE | Drug Info | [533165] | |||
FM1-10 | Drug Info | [529178] | |||
FM1-43 | Drug Info | [529178] | |||
GNF-PF-5618 | Drug Info | [527653] | |||
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] | |||
NOCARDIMICIN A | Drug Info | [527653] | |||
Nocardimicin C | Drug Info | [527653] | |||
Nocardimicin D | Drug Info | [527653] | |||
Nocardimicin F | Drug Info | [527653] | |||
Noccardimicin E | Drug Info | [527653] | |||
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester | Drug Info | [525826] | |||
SULFOARECOLINE | Drug Info | [533450] | |||
UCB-101333-3 | Drug Info | [528765] | |||
Antagonist | 3-(1-carbamoyl-1,1-diphenylmethyl)-1-(4-methoxyphenylethyl)pyrrolidine (APP) | Drug Info | [535903] | ||
4-DAMP | Drug Info | [535437], [537414] | |||
AE-9C90CB | Drug Info | [543432] | |||
Darifenacin | Drug Info | [537284] | |||
guanylpirenzepine | Drug Info | [534213] | |||
hexahydrodifenidol | Drug Info | [533335] | |||
hexahydrosiladifenidol | Drug Info | [533335] | |||
LAS-34273 | Drug Info | [536223] | |||
lithocholylcholine | Drug Info | [526426] | |||
ML381 | Drug Info | [532729] | |||
Olterodine | Drug Info | [535327] | |||
Oxybutynine | Drug Info | [536612] | |||
p-F-HHSiD | Drug Info | [534185] | |||
PTAC | Drug Info | [535327] | |||
silahexocyclium | Drug Info | [533335] | |||
Solifenacin | Drug Info | [537339] | |||
Succinylcholine | Drug Info | [536941], [538090] | |||
Tarafenacin | Drug Info | [529966] | |||
Tiotropium | Drug Info | [536555] | |||
Tolterodine | Drug Info | [535660], [535903] | |||
tripitramine | Drug Info | [529575] | |||
TRN-157 | Drug Info | [543432] | |||
UH-AH 37 | Drug Info | [534670] | |||
VU0255035 | Drug Info | [530098] | |||
Zamifenacin | Drug Info | [535150] | |||
[3H]darifenacin | Drug Info | [534324] | |||
[3H]N-methyl scopolamine | Drug Info | [534769] | |||
[3H]QNB | Drug Info | [533454] | |||
[3H]tiotropium | Drug Info | [532246] | |||
Agonist | arecaidine propargyl ester | Drug Info | [534426] | ||
Cevimeline | Drug Info | [536701] | |||
furtrethonium | Drug Info | [534426] | |||
J-104135 | Drug Info | [543432] | |||
McN-A-343 | Drug Info | [533662] | |||
methylfurmethide | Drug Info | [534426] | |||
NNC 11-1314 | Drug Info | [526123] | |||
NNC 11-1585 | Drug Info | [526123] | |||
NNC 11-1607 | Drug Info | [526123] | |||
oxotremorine-M | Drug Info | [534426] | |||
pentylthio-TZTP | Drug Info | [534426] | |||
SMT-D002 | Drug Info | [527286] | |||
Modulator (allosteric modulator) | brucine | Drug Info | [534573] | ||
Go7874 | Drug Info | [525801] | |||
N-benzyl brucine | Drug Info | [534573] | |||
N-chloromethyl-brucine | Drug Info | [534573] | |||
thiochrome | Drug Info | [526926] | |||
vinburnine | Drug Info | [534426] | |||
WIN 51,708 | Drug Info | [526460] | |||
WIN 62,577 | Drug Info | [526460] | |||
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 | |||||
Ref 523669 | ClinicalTrials.gov (NCT01458197) A Phase 2 Study to Compare the Efficacy and Tolerability of Tarafenacin 0.2 mg and Tarafenacin 0.4 mg to Placebo in Patients Suffering From Overactive Bladder.. U.S. National Institutes of Health. | ||||
Ref 524448 | ClinicalTrials.gov (NCT01951222) Bronchodilator Properties and Safety in Asthma. U.S. National Institutes of Health. | ||||
Ref 525108 | ClinicalTrials.gov (NCT02382510) Multiple Ascending Dose Study of TRN-157 in Stable Mild and Moderate Asthmatics. U.S. National Institutes of Health. | ||||
Ref 530127 | Aclidinium bromide, a novel long-acting muscarinic M3 antagonist for the treatment of COPD. Curr Opin Investig Drugs. 2009 May;10(5):482-90. | ||||
Ref 534674 | In 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 535986 | Therapeutic effect of cevimeline on dry eye in patients with Sj??gren's syndrome: a randomized, double-blind clinical study. Am J Ophthalmol. 2004 Jul;138(1):6-17. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 537130 | Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94. | ||||
Ref 538408 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008453. | ||||
Ref 538568 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021518. | ||||
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 540188 | (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: 321). | ||||
Ref 540223 | (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: 325). | ||||
Ref 540500 | (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: 367). | ||||
Ref 540621 | (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: 4004). | ||||
Ref 542506 | (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: 7483). | ||||
Ref 545544 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003650) | ||||
Ref 525801 | Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site. Mol Pharmacol. 2000 Jul;58(1):194-207. | ||||
Ref 525826 | J 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 526123 | Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists. J Pharmacol Exp Ther. 2001 Sep;298(3):1260-8. | ||||
Ref 526426 | Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. J Pharmacol Exp Ther. 2002 Oct;303(1):29-35. | ||||
Ref 526460 | Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors. Mol Pharmacol. 2002 Dec;62(6):1492-505. | ||||
Ref 526519 | Muscarinic M3-receptors mediate cholinergic synergism of mitogenesis in airway smooth muscle. Am J Respir Cell Mol Biol. 2003 Feb;28(2):257-62. | ||||
Ref 526926 | Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity. Mol Pharmacol. 2004 Jan;65(1):257-66. | ||||
Ref 527029 | J 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 527286 | Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64. | ||||
Ref 527344 | J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives. | ||||
Ref 527523 | J Nat Prod. 2005 Apr;68(4):572-3.Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata. | ||||
Ref 527653 | J 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 528735 | J 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 528765 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3077-80. Epub 2007 Mar 19.Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives. | ||||
Ref 529178 | Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist. | ||||
Ref 529575 | Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics. Bioorg Med Chem. 2008 Aug 1;16(15):7311-20. | ||||
Ref 529789 | J 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 529966 | In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009 Mar;156(5):807-17. | ||||
Ref 530098 | A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol Pharmacol. 2009 Aug;76(2):356-68. | ||||
Ref 530266 | Bioorg 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 530313 | J Med Chem. 1990 Feb;33(2):809-14.Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. | ||||
Ref 531079 | J 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 532246 | Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. | ||||
Ref 532729 | Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe. ChemMedChem. 2014 Aug;9(8):1677-82. | ||||
Ref 533165 | J 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 533335 | Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol. 1989 Apr;35(4):469-76. | ||||
Ref 533345 | J 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 533450 | J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. | ||||
Ref 533454 | Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. | ||||
Ref 533577 | J 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 533662 | Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists. Br J Pharmacol. 1995 Mar;114(6):1241-9. | ||||
Ref 534044 | J 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 534185 | Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung. Biochem Pharmacol. 1996 Aug 23;52(4):643-58. | ||||
Ref 534213 | Binding of the labelled muscarinic toxin 125I-MT1 to rat brain muscarinic M1 receptors. Eur J Pharmacol. 1996 Jun 3;305(1-3):187-92. | ||||
Ref 534324 | Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors. J Recept Signal Transduct Res. 1997 Jan-May;17(1-3):177-84. | ||||
Ref 534426 | Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol. 1997 Jul;52(1):172-9. | ||||
Ref 534573 | Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies. Mol Pharmacol. 1998 Mar;53(3):573-89. | ||||
Ref 534645 | J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. | ||||
Ref 534670 | Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists. Eur J Pharmacol. 1998 May 22;349(2-3):285-92. | ||||
Ref 534674 | In 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 534723 | J 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 534769 | Interaction of neuromuscular blocking drugs with recombinant human m1-m5 muscarinic receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Nov;125(5):1088-94. | ||||
Ref 535150 | Drug treatment options for irritable bowel syndrome: managing for success. Drugs Aging. 2001;18(3):201-11. | ||||
Ref 535327 | Which muscarinic receptor is important in the bladder? World J Urol. 2001 Nov;19(5):299-306. | ||||
Ref 535437 | The effects of the antagonists of muscarinic acetylcholine receptor subtypes in rat brain on urinary bladder contraction. Nippon Hinyokika Gakkai Zasshi. 2002 Mar;93(3):427-34. | ||||
Ref 535660 | Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | ||||
Ref 535903 | Signal transduction underlying carbachol-induced contraction of human urinary bladder. J Pharmacol Exp Ther. 2004 Jun;309(3):1148-53. Epub 2004 Feb 9. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536555 | DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. | ||||
Ref 536612 | Generation of an agonistic binding site for blockers of the M(3) muscarinic acetylcholine receptor. Biochem J. 2008 May 15;412(1):103-12. | ||||
Ref 536701 | Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist. Am J Physiol Gastrointest Liver Physiol. 2008 Jul;295(1):G112-G123. Epub 2008 May 1. | ||||
Ref 536941 | The involvement of histaminic and muscarinic receptors in the bronchoconstriction induced by myorelaxant administration in sensitized rabbits. Anesth Analg. 2008 Dec;107(6):1899-906. | ||||
Ref 537284 | M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor. Pharmacol Res. 2009 May;59(5):300-5. Epub 2009 Feb 5. | ||||
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