In Vivo and in Vitro Studies on a Muscarinic Presynaptic Antagonist and Postsynaptic Agonist: BM-5

  • Ö. Nordström
  • A. Undén
  • V. Grimm
  • B. Frieder
  • H. Ladinsky
  • T. Bartfai
Part of the Advances in Behavioral Biology book series (ABBI, volume 30)


The oxotremorine analog, compound BM-5: N-methyl-N(1-methyl-4-pyrrolidino-2-butynyl)acetamide (11) (Fig. 1) has been studied with respect to its muscarinic actions (9, 11). Jenden and colleagues found that the compound inhibited oxotremorine induced tremor in mice (11) while it was a partial agonist producing contraction of the ileum (9, 11). In parallel studies we found that compound BM-5 behaved as a presynaptic antagonist enhancing the evoked release of acetylcholine from the myenteric plexus and from synaptosomes prepared from rat hippocampus (9). In other presumable postsynaptic tests, such as the atropine sensitive stimulation of cyclic 3’5’guanosine monophosphate (cGMP) synthesis in human lymphocytes — a noninnervated “postsynaptic model tissue” — or inhippocampal slices, compound BM-5 behaved as a muscarinic agonist since it enhanced cGMP synthesis (9).


Muscarinic Receptor Myenteric Plexus Memory Consolidation Guanosine Monophosphate Muscarinic Agonist 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Berrie, C.P., Birdsall, N.J.M., Burgen, A.S.V. and Hulme, E.C. (1979): Biochem. Biophys. Res. Commun. 87: 1000–1005.CrossRefGoogle Scholar
  2. 2.
    Birdsall,N.J.M. and Hulme, E.C. (1976): J. Neurochem. 27: 7–16.CrossRefGoogle Scholar
  3. 3.
    Consolo, S., Ladinsky, H. and Garattini, S. (1974): J. Pharm. Pharmacol. 26: 275–277.Google Scholar
  4. 4.
    Garattini, S., Forloni, G.L., Tirelli, S., Ladinsky,H. and Consolo, S. (1984): Psychopharmacology 82: 210–214.CrossRefGoogle Scholar
  5. 5.
    Hingtgen,J.N. and Aprison, M.H. (1976): In Biology of Cholinergic Function (eds.) A.M. Goldberg and I. Hanin, Raven Press, New York, pp. 515–566.Google Scholar
  6. 6.
    Kloog, Y., Egozi, Y. and Sokolovsky, M. (1979): FEBS Lett. 97: 265–268.CrossRefGoogle Scholar
  7. 7.
    Ladinsky, H. Consolo, S., Bianchi, S. andJori, A. (1976): Brain Res. 108: 351–361.CrossRefGoogle Scholar
  8. 8.
    Maayani, S., Egozi, Y., Pinchasi, I. and Sokolovsky, M. (1978): Biochem. Pharmacol. 27: 203–214.CrossRefGoogle Scholar
  9. 9.
    Nordström, 8., Alberts, P., Westlind, A., Unden, A. and Bartfai, T. (1983): Mol. Pharmacol. 24: 1–5.Google Scholar
  10. 10.
    Pradhan, S.N. and Dutta, S.N. (1971): Int. Rev. Neurobiol. 14:173–231.Google Scholar
  11. 11.
    Resul, B., Dahlbom, R., Ringdahl, B. and Jenden, D.J. (1983): Eur. J. Med. Chem. 17: 317–322.Google Scholar
  12. 12.
    Russell, R.W. (1977): In Cholinergic Mechanisms and Psychopharmacology (ed.) D.J. Jenden, Plenum Press, New York, pp. 709–731.Google Scholar
  13. 13.
    Saelens, J.K., Allen, M.P. and Simke, J.P. (1970): Arch. Int. Pharmacodyn. Ther. 186: 279–286.Google Scholar
  14. 14.
    Sokolovsky, M. and Bartfai, T. (1982): Trends Biochem. Sci. 6: 303–305.CrossRefGoogle Scholar
  15. 15.
    Stratton L.D. and Petranovich, L. (1963): Psychopharmacologia:5:47–54.Google Scholar
  16. 16.
    Takeyashu, K., Uchida, S., Noguchi, Y., Fujita, N., Saito, K., Hata, F. and Yoshida, H. (1979): Life Sci. 25: 585–592.CrossRefGoogle Scholar
  17. 17.
    Westlind, A., Grynfarb, M., Hedlund, B., Bartfai, T. and Fuxe, K. (1981): Brain Res. 225: 131–141.CrossRefGoogle Scholar
  18. 18.
    Whitehouse, J.M. (1964): J. Comp. Physiol. Psychol. 57: 13–15.CrossRefGoogle Scholar
  19. 19.
    Whitehouse, J.M. (1966): Psychopharmacologia 2: 183–188.CrossRefGoogle Scholar

Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • Ö. Nordström
    • 1
  • A. Undén
    • 1
  • V. Grimm
    • 2
  • B. Frieder
    • 2
  • H. Ladinsky
    • 3
  • T. Bartfai
    • 1
  1. 1.Department of BiochemistryArrhenius LaboratoryStockholmSweden
  2. 2.Isotope DepartmentWeizmann Institute of ScienceRehovotIsrael
  3. 3.Cholinergic NeuropharmacologyMario Negri Institute for Pharmacological ResearchMilanItaly

Personalised recommendations