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 Alzheimer disease [ICD9: 331; ICD10: G30]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Acquired nystagmus [ICD9: 379.5; ICD10: H55]
Bronchodilator [ICD9: 493; ICD10: J45]
Central and peripheral nervous diseases [ICD10: G96.9]
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47]
Cough [ICD9: 786.2; ICD10: R05]
Depression [ICD9: 311; ICD10: F30-F39]
Dysuria; Urgency; Nocturia; Suprapubic pain [ICD10: R300, R35]
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 [539906], [551871]
Anisodine Drug Info Approved Central and peripheral nervous diseases [551871]
Anisotropine Methylbromide Drug Info Approved Peptic ulcer [538465], [551871]
Atropine Drug Info Approved Organophosphate poisoning [538234], [540179]
Bethanechol Drug Info Approved Urinary retention [538184], [539981]
Cimetropium bromide Drug Info Approved Gastric motility disorder; Spasm [551871]
Cryptenamine Acetates Drug Info Approved Hypertension [551871]
Cyclopentolate Drug Info Approved Produce mydriasis and cycloplegia for diagnostic purposes [551871]
Flavoxate Drug Info Approved Dysuria; Urgency; Nocturia; Suprapubic pain [551871]
Flutropium bromide Drug Info Approved Cough [551871]
Homatropine Methylbromide Drug Info Approved Peptic ulcer; Uveitis [538361], [551871]
Hyoscyamine Drug Info Approved Gastrointestinal disease [536224]
Ispaghula Drug Info Approved Irritable bowel syndrome [536224]
Mebeverine Drug Info Approved Irritable bowel syndrome [536224]
Mepenzolate Drug Info Approved Peptic ulcer; Gastrointestinal disease [538434], [551871]
Methantheline Drug Info Approved Peptic ulcer disease; Irritable bowel syndrome; Pancreatitis; Gastritis [551871]
Oxitropium bromide Drug Info Approved Bronchodilator [551871]
Oxyphencyclimine Drug Info Approved Peptic ulcer [542274], [550780], [551871]
Pilocarpine Drug Info Approved Glaucoma [538550], [540051]
Procyclidine Drug Info Approved Parkinson's disease [538423], [542300]
Promazine Drug Info Approved Moderate and severe psychomotor agitation [551871]
Tridihexethyl Drug Info Approved Acquired nystagmus [538420]
Trospium Drug Info Approved Overactive bladder disorder; Spasm [527466], [528278], [538569], [542503], [551871]
Umeclidinium Drug Info Approved Chronic obstructive pulmonary disease [542375], [550101]
Hyoscine Drug Info Phase 4 Discovery agent [524694]
L-651582 Drug Info Phase 3 Solid tumours [528019]
OrM3 Drug Info Phase 2b Chronic obstructive pulmonary disease [537130]
GSK233705 Drug Info Phase 2 Chronic obstructive pulmonary disease [537130]
Atropine Drug Info Phase 1 Poison intoxication [534497], [540179], [551871]
Org-23366 Drug Info Preclinical Schizophrenia [536463]
Benactyzine Drug Info Withdrawn from market Depression [526766]
RS 86 Drug Info Terminated Alzheimer disease [544694]
Inhibitor 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info [533345]
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]
ACECLIDINE Drug Info [534044]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info [525826]
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]
PF-3409409 Drug Info [530265]
SULFOARECOLINE Drug Info [533450]
VU0119498 Drug Info [530133]
VU0238429 Drug Info [530133]
Modulator Anisodine Drug Info [533488]
Cimetropium bromide Drug Info [528603], [536361]
Cryptenamine Acetates Drug Info [556264]
Flutropium bromide Drug Info [536361]
L-651582 Drug Info [528019]
Oxitropium bromide Drug Info [536361]
Umeclidinium Drug Info [542375]
Binder Anisotropine Methylbromide Drug Info [535825]
Oxyphencyclimine Drug Info [535829]
Promazine Drug Info [537711]
Tridihexethyl Drug Info [537342]
Antagonist Aprophen Drug Info [536212], [537749]
Atropine Drug Info [535437], [537455], [537469], [537749]
Benactyzine Drug Info [537749]
Cyclopentolate Drug Info [537401]
Flavoxate Drug Info [537993]
GSK233705 Drug Info [537130]
Homatropine Methylbromide Drug Info [536284]
Hyoscine Drug Info [538039]
Hyoscyamine Drug Info [537734]
Ispaghula Drug Info [536224]
Mebeverine Drug Info [536224]
Mepenzolate Drug Info [537843]
Methantheline Drug Info [537027]
Org-23366 Drug Info [536463]
OrM3 Drug Info [537130]
Procyclidine Drug Info [535950]
Trospium Drug Info [536284]
Agonist Bethanechol Drug Info [536978], [536985], [537156]
Muscarine Drug Info [535437]
Pilocarpine Drug Info [537264], [537370]
RS 86 Drug Info [537751]
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
Ref 524694ClinicalTrials.gov (NCT02098889) Safety Study of Hyoscine N Butyl Bromide in Active Management of Labor. U.S. National Institutes of Health.
Ref 526766Benactyzine as an aid in treatment of anxiety states; preliminary report. Br Med J. 1957 Feb 9;1(5014):306-10.
Ref 5274662004 approvals: the demise of the blockbuster. Nat Rev Drug Discov. 2005 Feb;4(2):93-4.
Ref 528019The antiproliferative and antimetastatic compound L651582 inhibits muscarinic acetylcholine receptor-stimulated calcium influx and arachidonic acid release. J Pharmacol Exp Ther. 1991 Jun;257(3):967-71.
Ref 528278Trospium chloride: the European experience. Expert Opin Pharmacother. 2006 Jul;7(10):1373-80.
Ref 534497Potentiation and inhibition of neuronal nicotinic receptors by atropine: competitive and noncompetitive effects. Mol Pharmacol. 1997 Nov;52(5):886-95.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 537130Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94.
Ref 538184FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040518.
Ref 538234FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071295.
Ref 538361FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 086310.
Ref 538420FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009489.
Ref 538423FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009818.
Ref 538434FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010679.
Ref 538465FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 013428.
Ref 538550FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020619.
Ref 538569FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021595.
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 539981(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: 297).
Ref 540051(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: 305).
Ref 540179(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: 320).
Ref 542274(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: 7256).
Ref 542300(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: 7280).
Ref 542375(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: 7354).
Ref 542503(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: 7480).
Ref 544694Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000634)
Ref 550101Clinical pipeline report, company report or official report of GlaxoSmithKline.
Ref 550780Drug information of Oxyphencyclimine, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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 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 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 528019The antiproliferative and antimetastatic compound L651582 inhibits muscarinic acetylcholine receptor-stimulated calcium influx and arachidonic acid release. J Pharmacol Exp Ther. 1991 Jun;257(3):967-71.
Ref 528603Scopolamine in Brugmansia suaveolens (Solanaceae): defense, allocation, costs, and induced response. J Chem Ecol. 2007 Feb;33(2):297-309.
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 530133J Med Chem. 2009 Jun 11;52(11):3445-8.Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Ref 530265Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. Epub 2009 Jul 2.Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
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 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 533488Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
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 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 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 535437The 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 535825Anisotropine methylbromide: a new antispasmodic for gastrointestinal disorders. Curr Ther Res Clin Exp. 1963 May;5:213-8.
Ref 535829Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors. Eur J Pharmacol. 1992 Sep 1;227(1):33-42.
Ref 535950Protection against soman-induced seizures in rats: relationship among doses of prophylactics, soman, and adjuncts. Toxicol Appl Pharmacol. 2004 May 1;196(3):327-36.
Ref 536212M1 muscarinic antagonists interact with sigma recognition sites. Life Sci. 1991;49(17):1229-35.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536284Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
Ref 536361Natural 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 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536978Postoperative analgesia induced by intrathecal neostigmine or bethanechol in rats. Clin Exp Pharmacol Physiol. 2009 Jul;36(7):648-54. Epub 2008 Nov 28.
Ref 536985Morphine increases acetylcholine release in the trigeminal nuclear complex. Sleep. 2008 Dec 1;31(12):1629-37.
Ref 537027Anticholinergics for urinary symptoms in multiple sclerosis. Cochrane Database Syst Rev. 2009 Jan 21;(1):CD004193.
Ref 537130Emerging drugs in chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2009 Mar;14(1):181-94.
Ref 537156Loss of Ca-mediated ion transport during colitis correlates with reduced ion transport responses to a Ca-activated K channel opener. Br J Pharmacol. 2009 Apr;156(7):1085-97. Epub 2009 Mar 9.
Ref 537264Muscarinic activation attenuates abnormal processing of beta-amyloid precursor protein induced by cobalt chloride-mimetic hypoxia in retinal ganglion cells. Biochem Biophys Res Commun. 2009 Jun 19;384(1):110-3. Epub 2009 Apr 22.
Ref 537342Effect of anticholinergic agents upon acquired nystagmus: a double-blind study of trihexyphenidyl and tridihexethyl chloride. Neurology. 1991 Nov;41(11):1737-41.
Ref 537370Retinoic acid prevents virus-induced airway hyperreactivity and M2 receptor dysfunction via anti-inflammatory and antiviral effects. Am J Physiol Lung Cell Mol Physiol. 2009 Aug;297(2):L340-6. Epub 2009 May 22.
Ref 537401High spatial resolution studies of muscarinic neuroeffector junctions in mouse isolated vas deferens. Neuroscience. 2009 May 29.
Ref 537455Loss of M2 muscarinic receptor function inhibits development of hypoxic bradycardia and alters cardiac beta-adrenergic sensitivity in larval zebrafish (Danio rerio). Am J Physiol Regul Integr Comp Physiol. 2009 Aug;297(2):R412-20. Epub 2009 Jun 10.
Ref 537469Additive Protective Effects of Donepezil and Nicotine Against Salsolinol-Induced Cytotoxicity in SH-SY5Y Cells. Neurotox Res. 2009 Mar 20.
Ref 537711Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites. Life Sci. 1988;43(5):405-12.
Ref 537734Reconstitution of the purified porcine atrial muscarinic acetylcholine receptor with purified porcine atrial inhibitory guanine nucleotide binding protein. Biochemistry. 1987 Dec 15;26(25):8175-82.
Ref 537749The muscarinic antagonists aprophen and benactyzine are noncompetitive inhibitors of the nicotinic acetylcholine receptor. Mol Pharmacol. 1987 Nov;32(5):678-85.
Ref 537751The pharmacological assessment of RS 86 (2-ethyl-8-methyl-2,8-diazaspiro-[4,5]-decan-1,3-dion hydrobromide). A potent, specific muscarinic acetylcholine receptor agonist. Eur J Pharmacol. 1986 Jun 5;125(1):45-62.
Ref 537843Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker. J Ethnopharmacol. 1995 Mar;45(3):215-22.
Ref 537993Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res. 1996 Jul 15;727(1-2):91-8.
Ref 538039Comparison of the effects of a selective muscarinic receptor antagonist and hyoscine (scopolamine) on motion sickness, skin conductance and heart rate. Br J Clin Pharmacol. 1997 Jun;43(6):633-7.
Ref 542375(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: 7354).
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 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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