Skip to main content
SpringerLink
Log in

The Muscarinic Receptors

  • Chapter
Principles and Methods in Receptor Binding

Part of the book series: NATO ASI Series ((NSSA,volume 72))

  • 70 Accesses

Abstract

Muscarinic receptors exist in both peripheral tissues and the central nervous system. Their activation is responsible for all the effects elicited by parasympathetic stimulation in the peripheral organs and modulate ganglionic transmission (Wallis, 1979). In the central nervous system muscarinic receptors are involved in many functions connected with the cognitive processes, sleep mechanism, motility, blood pressure and water intake regulation (Karczmar, 1981).

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
eBook
USD 16.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 16.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Alberts, P., Bartfai, T and Stjärne, L., 1982, The effects of atropine on 3H acetylcholine secretion from guinea—pig myenteric plexus evoked electrically or by high potassium, J. Physiol.(Lond.), 329: 93.

    Google Scholar 

  2. Aronstam, R.S., Triggle,D.J. and Eldefrawi, M.E., 1979, Structural and stereochemical requirements for muscarinic receptor binding, Mol. Pharmacol., 15: 227.

    CAS  Google Scholar 

  3. Bartus, R.T., Dean, R.L., Beer, B. and Lippa, A.S., 1982, The cholinergic hypothesis of geriatric memory disfunction, Science, 217: 408.

    CAS  Google Scholar 

  4. Beld, A.J. and Ariens, E.J., 1974, Stereospecific binding as a tool in attempts to localize and isolate muscarinic receptors, Eur. J. Pharmac., 25: 203.

    Google Scholar 

  5. Ben—Barak, J. and Dudai, Y., 1980, Scopolamine induces an increase in muscarinic receptor level in rat hippo—campus, Brain Res., 193: 309.

    Google Scholar 

  6. Birdsall, N.J.M.,and Hulme, E.C., 1976, Biochemical studies on muscarinic acetylcholine receptors, J. Neurochem., 27: 7.

    Article  Google Scholar 

  7. Birdsall, N.J.M., Burgen, A.S.V.,and Hulme, E.C., 1977, Correlation between the binding properties and pharmacological responses of muscarinic receptors, in: “Cholinergic mechanisms and psychopharmacology”, D.J. Jenden, ed., Plenum Press, New York.

    Google Scholar 

  8. Birdsall, N.J.M., Burgen, A.S.V.,and Hulme, E.C., 1978, The binding of agonists to brain muscarinic receptors, Mol. Pharmacol., 14: 723.

    CAS  Google Scholar 

  9. Bowen, D.M. and Marek, K.L., 1982, Evidence for the pharmacological similarity between central presynaptic muscarinic autoreceptors and postsynaptic muscarinic receptors, Br. J. Pharmac., 75: 367.

    Google Scholar 

  10. Brimblecombe, R.W., 1974, “Drug action on cholinergic systems”, The Macmillan Press, London.

    Google Scholar 

  11. Burgisser, E., De Lean, A.,and Lefkowitz, R.J., 1982, Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide, Proc. Natl. Acad. Sci. U.S.A., 79: 1732.

    Article  CAS  Google Scholar 

  12. Campbell, B.A., Lytle, L.D., and Fibiger, H.C., 1969, Ontogeny of adrenergic arousal and cholinergic inhibitory mechanisms in the rat, Science, 166: 635

    CAS  Google Scholar 

  13. Casamenti, F., Pedata,F., Corradetti, R., and Pepeu, G., 1980, Acetylcholine output from the cerebral cortex, choline uptake and muscarinic receptors in morphine—dependent freely—moving rats, Neuropharmacol.,19: 597.

    Google Scholar 

  14. Costa, L.G., Schwab, B.W., and Murphy, S.D., 1982, Differential alterations of cholinergic muscarinic receptors during chronic and acute tolerance to organophosphorus insecticides, Biochem. Pharmacol., 31: 3407.

    Google Scholar 

  15. Creese, I., Usdin, T.B., and Snyder, S.H., 1979, Dopamine receptor binding regulated by guanine nucleotides, Mol. Pharmacol., 16: 69.

    Google Scholar 

  16. Ehlert, ?.J., Kokka, N., and Fairhurst, A.S., 1980, Altered H quinuclidinyl benzylate binding in the striatum following chronic cholinesterase inhibition with diisopropylfluorophosphate, Mol. Pharmacol., 17: 24.

    Google Scholar 

  17. Fozard, J.R. and Muscholl, E., 1972, Effects of several muscarinic agonists on cardiac performance and the release of noradrenaline from sympathetic nerves of the perfused rabbit heart, Br. J. Pharmac., 45: 616.

    Article  CAS  Google Scholar 

  18. Furchgott, R.F., 1978, Pharmacological characterization of receptors: its relation to radioligand—binding studies, Fedn. Proc., 37: 115.

    Google Scholar 

  19. Gazit, H., Silman, I., and Dudai, Y., 1979, Administration of an organophosphate causes a decrease in mus — carinic receptor level in rat brain, Brain Res., 174: 351.

    Article  PubMed  CAS  Google Scholar 

  20. Hammer, R., Berrie, C.P., Birdsall, N.J.M., Burgen, A. S.V., and Hulme, E.C., 1980, Pirenzepine distinguishes between different “subclasses of muscarinic receptors, Nature, 283: 90.

    CAS  Google Scholar 

  21. Hammer, R. and Giachetti, A., 1982, Muscarinic receptor subtypes: M1 and M. Biochemical and functional charac— terization, Life Seei., 31: 2991.

    Google Scholar 

  22. Hartzell, H.C., 1982, Physiological consequences of muscarinic receptor activation, Trends Pharmacol. Sci.

    Google Scholar 

  23. Heilbronn, E. and Bartfai, T., 1978, Muscarinic acetylcholine receptors, Progr. Neurobiol., 11: 171.

    Google Scholar 

  24. Heilbronn, E. and Bartfai, T., 1978, Muscarinic acetylcholine receptors, Progr. Neurobiol., 11: 171.

    Google Scholar 

  25. Hulme, E.C., Birdsall, N.J.M., Burgen, A.S.V., and Mehta, P., 1978, The binding of antagonists to brain muscarinic receptors, Mol. Pharmacol., 14: 737.

    PubMed  CAS  Google Scholar 

  26. Karczmar, A.G., 1981, Basic phenomena underlying novel use of cholinergic agents, anticholinesterases and precursors in neurological including peripheral and psychiatric diseases, in: “Cholinergic mechanisms”, G. Pepeu and H. Ladins y eds., Plenum Press, New York.

    Google Scholar 

  27. Kilbinger, H. and Wessler, I., 1980, Pre and post—synaptic effects of muscarinic agonists in the guinea—pig ileaum, Naunyn—Schmiedeberg’s Arch. Pharmacol., 314: 259.

    Article  CAS  Google Scholar 

  28. Kuhar, M.J. and Yamamura, H.I., 1975, Light autoradio—graphic localization of cholinergic muscarinic receptors in rat brain by specific binding of a potent antagonist, Nature, 253: 560.

    CAS  Google Scholar 

  29. Kuhar, M.J., Birdsall, N.J.M., Burgen, A.S.V. and Hulme, E.C., 1980, Ontogeny of muscarinic receptors in rat brain, Brain Res., 184: 375•

    Google Scholar 

  30. Kuo, J.F., 1974, Guanosine 3’ 5’- monophosphate—dependent protein kinases in mammalian tissues, Proc. Natl. Acad. Sci. U.S.A., 71: 4037.

    Google Scholar 

  31. Laduron, P., 1980, Axoplasmic transport of muscarinic receptors, Nature, 286: 287.

    CAS  Google Scholar 

  32. Laduron, P., Verwimp, M, and Leysen, J.E., 1979

    Google Scholar 

  33. Stereospecific in vitro binding of3H dexetimide to brain muscarinic receptors, J. Neurochem., 32: 421.

    Google Scholar 

  34. Lundberg, J.M., 1981, Evidence for coesistence of vasoactive intestinal polypeptide (VIP) and acetylcholine

    Google Scholar 

  35. in neurons of cat exocrine glands, Acta Physiol. Scand., Suppl. 496: 1.

    Google Scholar 

  36. Lundberg, J.M., Hedlund, B., and Bartfai, T., 1982, Vasoactive intestinal polypeptide enhances muscarinic ligand binding in cat submandibular salivary gland, Nature, 295: 147.

    CAS  Google Scholar 

  37. Majocha, R. and Baldessarini, R.J., 1980, Increased muscarinic receptor binding in rat forebrain after scopolamine, European J. Pharmacol., 67: 327.

    CAS  Google Scholar 

  38. Matsuzawa, H. and Nirenberg, M., 1975, Receptor mediated shift in cGMP and cAMP levels in neuroblastoma cells, Proc. Natl. Acad. Sci. U.S.A., 72: 3472.

    Google Scholar 

  39. McKinney and Coyle, J.T., 1982, Regulation of neocortical muscarinic receptors: effect of drug treatment and lesions, J. Neurosci., 2: 97.

    Google Scholar 

  40. Mitchell, R.H. and Kirk, C.J., 1981, Why is phosphatidylinositol degraded in responses to stimulation of certain receptors ?, Trends Pharmacol. Sci., 2: 86.

    Google Scholar 

  41. Nordberg, A., Wahlström, G and Larsson, Ch., 1980, Increased number of muscarinic binding sites in brain following chronic barbiturate treatment to rat, Life Sci., 26: 231.

    Article  PubMed  CAS  Google Scholar 

  42. Nordström, 0. and Bartfai, T., 1980, Muscarinic auto—receptor regulates acetylcholine in rat hippocampus: in vitro evidence, Acta Physiol., 108: 347.

    Article  Google Scholar 

  43. Nordström, 0;, Alberts, P., Westlind, A., Unden, A., and Bartfai, T., 1983, Presynaptic antagonist — post—synaptic agonist at muscarinic cholinergic synapses:

    Google Scholar 

  44. N—methyl—N—(1—methyl-4—pyrrolidino-2—butynyl) acetamide, Mol. Pharmacol., in the press.

    Google Scholar 

  45. Parry, M. and Heathcote, B.V., 1982, A comparison of the effec of pirenzepine and atropine on gastric acid secretion, salivary secretion and pupil diameter in the rat. Life Sci., 31: 1465.

    Article  PubMed  CAS  Google Scholar 

  46. Patel, A.J., Smith, R.M., Kingsbury, A.E., Hunt, A., and Balazs, R., 1980, Effects of thyroid state on brain

    Google Scholar 

  47. development: muscarinic acetylcholine and GABA receptors, Brain Res., 198: 389.

    Google Scholar 

  48. Paton, W.D.M. and Rang, H.P., 1965, The uptake of atropine and related drugs by intestinal smooth muscle of the guinea—pig in relation to acetylcholine receptors, Proc. R. Soc. B, 163: 1.

    Google Scholar 

  49. Pedata, F., Slavikova, J., Kotas,A., and Pepeu, G., 1983, Acetylcholine release from rat cortical slices during postnatal development and aging, Neurobiol. Aging, in the press.

    Google Scholar 

  50. Polak, R.L. and Meeuws, M.M., 1966, The influence of atropine on the release and uptake of acetylcholine by the isolated cerebral cortex of the rat, Biochem. Pharmacol., 15: 989.

    Google Scholar 

  51. Putney, J.W. and Van De Walle, C., 1980, The relationship between muscarinic receptor binding and ion movements in rat parotid cells, J. Physiol. (Lond.), 299: 521.

    CAS  Google Scholar 

  52. Rosenberger,L.B.,Roeske, W.R., and Yamamura, H.I., 1979, The regulation of muscarinic receptors by guanine nucleotides in cardiac tissue, European J. Pharmacol., 56: 179.

    Google Scholar 

  53. Rosenberger, L.B., Yamamura, H.I., and Roeske, W.R., 1980 The regulation of cardiac muscarinic receptors by isoproterenol, European J. Pharmacol., 65: 129.

    Google Scholar 

  54. Siman, R.G. and Klein, W.L., 1981, Specificity of muscarinic acetylcholine receptor regulation by receptor activity, J. Neurochem., 37: 1099.

    Article  PubMed  CAS  Google Scholar 

  55. Siman, R.G., and Klein, W.L., 1979, Cholinergic activity regulates muscarinic receptors in central nervous system cultures, Proc, Natl. Acad. Sci. U.S.A., 76: 4141.

    Article  CAS  Google Scholar 

  56. Snyder, S.H., Chang, K.J., Kuhar, M.J., and Yamamura, H.I., 1975, Biochemical identification of the mammalian muscarinic cholinergic receptor, Fedn. Proc., 34: 1915.

    Google Scholar 

  57. Sokolovsky, M., Gurwitz, D., and Galron, R., 1980, Muscarinic receptor binding in mouse brain: regulation by guanine nucleotides, Biochem. Biophys. Res. Comm., 94: 487.

    CAS  Google Scholar 

  58. Szelenyi, I., 1982, Does pirenzepine distinguish between “subtypes” of muscarinic receptors ?, Br. J. Pharmac., 77: 567.

    Article  CAS  Google Scholar 

  59. Szerb, J.C. and Somogyi, C.T., 1973, Depression of acetylcholine release in cerebral cortical slices by cholinesterase inhibition and by oxotremorine, Nature, 241: 121.

    CAS  Google Scholar 

  60. Wallis, D.I., 1979, The apparent multiplicity of ganglionic receptors, in:“Trends in autonomic pharmacology”, I, Kalsner ed., Urban and Schwarzenberg, Baltimore.

    Google Scholar 

  61. Wamsley, J.K., Zarbin, M.A., and Kuhar, M.J., 1981, Muscarinic cholinergic receptors flow in the sciatic nerve, Brain Res., 217: 155.

    CAS  Google Scholar 

  62. Waser, P.G., 1961, Chemistry and pharmacology of muscarine, muscarone and related compounds, Pharmacol. Rev., 13: 465.

    CAS  Google Scholar 

  63. Wastek, G.J. and Yamamura, H.I., 1978, Biochemical characterization of the muscarinic cholinergic receptor in human brain: alteration in Huntington’s disease, Mol. Pharmacol., 14: 768.

    PubMed  CAS  Google Scholar 

  64. Wastek, G.J., Lopez, J.R.,and Richelson, E., 1981, Demonstration of a muscarinic mediated cyclic GMPdependent hyperpolarization of the vembrane potential of mouse neuroblastoma cells using H tetraphenylphosphonium, Mol. Pharmacol., 19: 15.

    Google Scholar 

  65. Watson, M., Roeske, W.R., and Yamamura, H.I., 1982, H pirenzepine selectively identifies a high affinity population of muscarinic cholinergic receptors in the rat cerebral cortex, Life Sci. 31: 2019.

    Article  PubMed  CAS  Google Scholar 

  66. Yamamura, H.I. and Snyder, S.H., 1974, Muscarinic cholinergic binding in rat brain, Proc. Natl. Acad. S.i. U.S.A., 71: 1725.

    Google Scholar 

  67. Yamamura, H.Z., Kuhar, M.J., Greenberg, D., and Snyder, S.H., 1974, Muscarinic cholinergic receptor binding: regional distribution in monkey brain, Brain Res., 66: 541.

    Article  CAS  Google Scholar 

  68. Zarbin, M.A., Wamsley, J.K., and Kuhar, M.J., 1982, Axonal transport of muscarinic cholinergic receptors in rat vagus nerve: high and low affinity agonist receptors move in opposite directions and differ in nucleotide sensitivity, J. Neurosci., 2: 934.

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Pharmacology, University of Florence, Viale Morgagni 65, 50134, Florence, Italy

    Giancarlo Pepeu & Ileana Marconcini Pepeu

Authors
  1. Giancarlo Pepeu
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Ileana Marconcini Pepeu
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. Institute of Pharmacology and Pharacognosy, University of Urbino, Urbino, Italy

    F. Cattabeni

  2. Institute of Pharmacology and Pharmacognosy, University of Milan, Milan, Italy

    S. Nicosia

Rights and permissions

Reprints and permissions

Copyright information

© 1984 Springer Science+Business Media New York

About this chapter

Cite this chapter

Pepeu, G., Pepeu, I.M. (1984). The Muscarinic Receptors. In: Cattabeni, F., Nicosia, S. (eds) Principles and Methods in Receptor Binding. NATO ASI Series, vol 72. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-1577-4_5

Download citation

  • DOI: https://doi.org/10.1007/978-1-4757-1577-4_5

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4757-1579-8

  • Online ISBN: 978-1-4757-1577-4

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation