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Chemical Compound Review

MUSCARINE     [(2S,4R,5S)-4-hydroxy-5- methyl-oxolan-2...

Synonyms: Muscarin, Muskarin, muscarie, Lopac-M-104, CHEMBL12587, ...
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Disease relevance of MUSCARINE


Psychiatry related information on MUSCARINE


High impact information on MUSCARINE


Chemical compound and disease context of MUSCARINE


Biological context of MUSCARINE


Anatomical context of MUSCARINE


Associations of MUSCARINE with other chemical compounds

  • When a low dose of muscarine sufficient to inhibit IM, but not to elicit desensitization, was applied simultaneously with a desensitizing dose of SP, IM remained depressed and did not desensitize [26].
  • Only atropine and the m3-m4-selective muscarinic antagonist 4-diphenylacetoxy-4-methyl-piperidine (4-DAMP) reduce the response to muscarine, strongly suggesting that the m4 receptor is crucial for PNMT mRNA activation [27].
  • The production of [3H]inositol phosphates by VIP and muscarine occurred in calcium-free and EGTA medium [17].
  • Neither k nor n is affected when: (a) [Bis-Q] is varied between 5 and 100 microM; (b) [carbachol] is varied between 1 and 50 microM; (c) carbachol is replaced by other agonists (muscarine, acetylcholine, or acetyl-beta-methylcholine); or (d) the voltage is varied between the normal resting potential and a depolarization of 80 mV [28].
  • We now report that exposure of cultured cerebellar granule neurons, maintained under nondepolarizing conditions, to the muscarinic cholinergic receptor (mAchR) agonists carbachol and muscarine results in a concentration- and time-dependent inhibition of apoptosis [29].

Gene context of MUSCARINE

  • The muscarine-elicited depression of ACh release in normal junctions was completely abolished by pertussis toxin or methoctramine pretreatment, but was not affected by muscarinic toxin MT-3, thus indicating the involvement of the M2 mAChR [30].
  • The muscarine-induced increase of ACh release in AChE-deficient junctions was not affected by pertussis toxin, but was completely blocked by MT-7, a specific M1 mAChR antagonist [30].
  • In addition muscarine-enhanced sAPPalpha secretion and ERK1/2 activation were inhibited 60 and 80%, respectively, by micromolar concentrations of the phosphatidylinositol 3 kinase (PI-3K) inhibitor wortmannin [31].
  • 3. 10 muscarine receptor antagonists with differing relative affinities for M1, M2 and M3 receptors were introduced at 1 mumol/l to inhibit electrically-stimulated acid secretion [32].
  • The signalling pathways by which muscarine and epidermal growth factor (EGF) regulate the secretion of the alpha-secretase cleavage product (sAPPalpha) of the amyloid precursor protein (APP) were examined in the human neuroblastoma SH-SY5Y [31].

Analytical, diagnostic and therapeutic context of MUSCARINE


  1. Optical recordings of the effects of cholinergic ligands on neurons in the ganglion cell layer of mammalian retina. Baldridge, W.H. J. Neurosci. (1996) [Pubmed]
  2. Bradykinin and muscarine induce Ca(2+)-dependent oscillations of membrane potential in rat glioma cells indicating a rhythmic Ca2+ release from internal stores: thapsigargin and 2,5-di(tert-butyl)-1, 4-benzohydroquinone deplete InsP3-sensitive Ca2+ stores in glioma and in neuroblastoma-glioma hybrid cells. Reiser, G., Cesar, M., Binmöller, F.J. Exp. Cell Res. (1992) [Pubmed]
  3. Pharmacological and functional characterization of muscarinic receptors in the frog pars intermedia. Garnier, M., Lamacz, M., Galas, L., Lenglet, S., Tonon, M.C., Vaudry, H. Endocrinology (1998) [Pubmed]
  4. Hypoxia and cyanide induce depolarization and catecholamine release in dispersed guinea-pig chromaffin cells. Inoue, M., Fujishiro, N., Imanaga, I. J. Physiol. (Lond.) (1998) [Pubmed]
  5. Inhibition of N-type Ca2+ channel currents in human neuroblastoma (SH-SY5Y) cells by muscarine via stimulation of M3 receptors. Reeve, H.L., Vaughan, P.F., Peers, C. Neuropharmacology (1995) [Pubmed]
  6. Loss of M2 muscarine receptors in the cerebral cortex in Alzheimer's disease and experimental cholinergic denervation. Mash, D.C., Flynn, D.D., Potter, L.T. Science (1985) [Pubmed]
  7. Pharmacological restoration of scopolamine-impaired memory. Petkov, V.V., Vuglenova, Y. Acta physiologica et pharmacologica Bulgarica. (1985) [Pubmed]
  8. Phorbol ester facilitates 45Ca accumulation and catecholamine secretion by nicotine and excess K+ but not by muscarine in rat adrenal medulla. Wakade, A.R., Malhotra, R.K., Wakade, T.D. Nature (1986) [Pubmed]
  9. Muscarinic depression of long-term potentiation in CA3 hippocampal neurons. Williams, S., Johnston, D. Science (1988) [Pubmed]
  10. Muscarinic induction of hippocampal gamma oscillations requires coupling of the M1 receptor to two mixed cation currents. Fisahn, A., Yamada, M., Duttaroy, A., Gan, J.W., Deng, C.X., McBain, C.J., Wess, J. Neuron (2002) [Pubmed]
  11. Selective reduction of one mode of M-channel gating by muscarine in sympathetic neurons. Marrion, N.V. Neuron (1993) [Pubmed]
  12. Muscarinic Ca2+ responses resistant to muscarinic antagonists at perisynaptic Schwann cells of the frog neuromuscular junction. Robitaille, R., Jahromi, B.S., Charlton, M.P. J. Physiol. (Lond.) (1997) [Pubmed]
  13. Enhancement of GABA-activated current by muscarine in rat dorsal root ganglion neurons. Hu, H.Z., Shao, M., Li, Z.W. Neuroscience (1999) [Pubmed]
  14. Distinct muscarinic receptors enhance spontaneous GABA release and inhibit electrically evoked GABAergic synaptic transmission in the chick lateral spiriform nucleus. Guo, J., Chiappinelli, V.A. Neuroscience (2001) [Pubmed]
  15. Muscarine inhibits omega-conotoxin-sensitive calcium channels in a voltage- and time-dependent mode in the human neuroblastoma cell line SH-SY5Y. Toselli, M., Perin, P., Taglietti, V. J. Neurophysiol. (1995) [Pubmed]
  16. ERK1 and ERK2, two microtubule-associated protein 2 kinases, mediate the phosphorylation of tyrosine hydroxylase at serine-31 in situ. Haycock, J.W., Ahn, N.G., Cobb, M.H., Krebs, E.G. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  17. Vasoactive intestinal polypeptide and muscarine mobilize intracellular Ca2+ through breakdown of phosphoinositides to induce catecholamine secretion. Role of IP3 in exocytosis. Malhotra, R.K., Wakade, T.D., Wakade, A.R. J. Biol. Chem. (1988) [Pubmed]
  18. Muscarinic receptor stimulation induces translocation of an alpha-synuclein oligomer from plasma membrane to a light vesicle fraction in cytoplasm. Leng, Y., Chase, T.N., Bennett, M.C. J. Biol. Chem. (2001) [Pubmed]
  19. Role of muscarinic receptor subtypes in the constriction of peripheral airways: studies on receptor-deficient mice. Struckmann, N., Schwering, S., Wiegand, S., Gschnell, A., Yamada, M., Kummer, W., Wess, J., Haberberger, R.V. Mol. Pharmacol. (2003) [Pubmed]
  20. The contribution of TWIK-related acid-sensitive K+-containing channels to the function of dorsal lateral geniculate thalamocortical relay neurons. Meuth, S.G., Aller, M.I., Munsch, T., Schuhmacher, T., Seidenbecher, T., Meuth, P., Kleinschnitz, C., Pape, H.C., Wiendl, H., Wisden, W., Budde, T. Mol. Pharmacol. (2006) [Pubmed]
  21. Inflammatory modulation of muscarinic receptor activation in canine ileal circular muscle cells. Shi, X.Z., Sarna, S.K. Gastroenterology (1997) [Pubmed]
  22. Different effects of N-ethylmaleimide on M1 and M2 muscarine receptors in rat brain. Flynn, D.D., Potter, L.T. Proc. Natl. Acad. Sci. U.S.A. (1985) [Pubmed]
  23. [Ca2+]i elevations detected by BK channels during Ca2+ influx and muscarine-mediated release of Ca2+ from intracellular stores in rat chromaffin cells. Prakriya, M., Solaro, C.R., Lingle, C.J. J. Neurosci. (1996) [Pubmed]
  24. Substance P: ionic basis for depolarizing responses of mouse spinal cord neurons in cell culture. Nowak, L.M., Macdonald, R.L. J. Neurosci. (1982) [Pubmed]
  25. Muscarine hyperpolarizes a subpopulation of neurons by activating an M2 muscarinic receptor in rat nucleus raphe magnus in vitro. Pan, Z.Z., Williams, J.T. J. Neurosci. (1994) [Pubmed]
  26. Desensitization of the inhibition of the M-current in sympathetic neurons: effects of ATP analogs, polyanions, and multiple agonist applications. Simmons, M.A., Becker, J.B., Mather, R.J. Neuron (1990) [Pubmed]
  27. A single transmitter regulates gene expression through two separate mechanisms: cholinergic regulation of phenylethanolamine N-methyltransferase mRNA via nicotinic and muscarinic pathways. Evinger, M.J., Ernsberger, P., Regunathan, S., Joh, T.H., Reis, D.J. J. Neurosci. (1994) [Pubmed]
  28. A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart. Nargeot, J., Lester, H.A., Birdsall, N.J., Stockton, J., Wassermann, N.H., Erlanger, B.F. J. Gen. Physiol. (1982) [Pubmed]
  29. Activation of muscarinic cholinergic receptors blocks apoptosis of cultured cerebellar granule neurons. Yan, G.M., Lin, S.Z., Irwin, R.P., Paul, S.M. Mol. Pharmacol. (1995) [Pubmed]
  30. Regulation of acetylcholine release by muscarinic receptors at the mouse neuromuscular junction depends on the activity of acetylcholinesterase. Minic, J., Molgó, J., Karlsson, E., Krejci, E. Eur. J. Neurosci. (2002) [Pubmed]
  31. Muscarine enhances soluble amyloid precursor protein secretion in human neuroblastoma SH-SY5Y by a pathway dependent on protein kinase C(alpha), src-tyrosine kinase and extracellular signal-regulated kinase but not phospholipase C. Canet-Aviles, R.M., Anderton, M., Hooper, N.M., Turner, A.J., Vaughan, P.F. Brain Res. Mol. Brain Res. (2002) [Pubmed]
  32. Telenzepine inhibits electrically-stimulated, acetylcholine plus histamine-mediated acid secretion in the mouse isolated stomach by blockade of M1 muscarine receptors. Kromer, W., Baron, E., Boer, R., Eltze, M. Naunyn Schmiedebergs Arch. Pharmacol. (1991) [Pubmed]
  33. Cross-communication between acetylcholine and VIP in controlling catecholamine secretion by affecting cAMP, inositol triphosphate, protein kinase C, and calcium in rat adrenal medulla. Malhotra, R.K., Wakade, T.D., Wakade, A.R. J. Neurosci. (1989) [Pubmed]
  34. Muscarine inhibits high-threshold calcium currents with two distinct modes in rat embryonic hippocampal neurons. Toselli, M., Taglietti, V. J. Physiol. (Lond.) (1995) [Pubmed]
  35. Acetylcholine released from guinea-pig submucosal neurones dilates arterioles by releasing nitric oxide from endothelium. Andriantsitohaina, R., Surprenant, A. J. Physiol. (Lond.) (1992) [Pubmed]
  36. Changes in potassium channel activity following axotomy of B-cells in bullfrog sympathetic ganglion. Jassar, B.S., Pennefather, P.S., Smith, P.A. J. Physiol. (Lond.) (1994) [Pubmed]
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