Affinity and Efficacy of Oxotremorine Analogs at Ileal Muscarinic Receptors

  • B. Ringdahl
Part of the Advances in Behavioral Biology book series (ABBI, volume 30)


The pharmacological activity of a muscarinic agonist, as measured for example by contractile responses in smooth muscle preparations, is a function of both its affinity for the receptor and its efficacy in producing a stimulus that leads to a response (26). Because of the existence in many tissues of a receptor reserve for muscarinic agonists, ED50 values for pharmacological responses often are poor estimates of affinities. More satisfactory estimates of agonist affinities may be obtained from receptor binding studies. Although the relationship between binding parameters and ED50 values of muscarinic agonists is not yet fully understood, radioligand binding techniques have given valuable information on the structural demands for agonist binding at the muscarinic receptor (3, 12). In contrast, the structural features of muscarinic agonists that cause them to activate the receptor are less readily assessed.


Muscarinic Receptor Partial Agonist Receptor Occupancy Relative Efficacy Muscarinic Agonist 
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  1. 1.
    Ariens, E.J. (1979): Trends Pharmacol. Sci. 1: 11–15.CrossRefGoogle Scholar
  2. 2.
    Besse, J.C. and Furchgott, R.F. (1976): J. Pharmacol. Exp. Ther. 197:66–78.Google Scholar
  3. 3.
    Birdsall, N.J.M., Burgen, A.S.V. and Hulme, E.C. (1978): Mol. Pharmacol. 14: 723–736.Google Scholar
  4. 4.
    Burgen, A.S.V. (1981): Fed. Proc. 40: 2723–2728.Google Scholar
  5. 5.
    Dahlbom, R. (1981): In Cholinergic Mechanisms: Phylogenetic Aspects, Central and Peripheral Synapses, and Clinical Significance (eds) G. Pepeu and H. Ladinsky, Plenum Press, New York, pp. 621–638.Google Scholar
  6. 6.
    Dahlbom, R., Jenden, D.J., Resul, B. and Ringdahl, B. (1982): Brit. J. Pharmacol. 76: 299–304.Google Scholar
  7. 7.
    Ehlert, F.J., Kokka, N. and Fairhurst, A.S. (1980): Biochem. Pharmacol. 29: 1391–1397.CrossRefGoogle Scholar
  8. 8.
    El-Fakahany, E. and Richelson, E. (1981): Mol. Pharmacol. 20: 519–525.Google Scholar
  9. 9.
    Fisher, S.K., Klinger, P.D. and Agranoff, B.W. (1983): J. Biol. Chem. 258: 7358–7363.Google Scholar
  10. 10.
    Furchgott, R.F. (1966): Adv. Drug Res. 3: 21–55.Google Scholar
  11. 11.
    Furchgott, R.F. and Bursztyn, P. (1967): Ann. N.Y. Acad. Sci. 144: 882–899.CrossRefGoogle Scholar
  12. 12.
    Jim, K., Bolger, G.T., Triggle, D.J. and Lambrecht, G. (1982): Can. J. Physiol. Pharmacol. 60: 1707–1714.CrossRefGoogle Scholar
  13. 13.
    Michell, R.H. and Kirk, C.J. (1981): Trends Pharmacol. Sci. 2: 86–89.CrossRefGoogle Scholar
  14. 14.
    Nordström, O., Alberts, P., Westlind, A., Unden, A. and Bartfai, T. (1983): Mol. Pharmacol. 24: 1–5.Google Scholar
  15. 15.
    Resul, B., Dahlbom, R., Ringdahl, B. and Jenden, D.J. (1982): Eur. J. Med. Chem. 17: 317–322.Google Scholar
  16. 16.
    Resul, B., Ringdahl, B., Dahlbom, R. and Jenden, D.J. (1983): Eur. J. Pharmacol. 87: 387–396.CrossRefGoogle Scholar
  17. 17.
    Ringdahl, B. (1984): J. Pharmacol. Exp. Ther. 229: 199–206.Google Scholar
  18. 18.
    Ringdahl, B. (1984): Brit. J. Pharmacol. 82: 269–274.Google Scholar
  19. 19.
    Ringdahl, B. (1985): J. Pharmacol. Exp. Ther. 232: 67–73.Google Scholar
  20. 20.
    Ringdahl, B. and Jenden, D.J. (1983): Mol. Pharmacol. 23: 17–25.Google Scholar
  21. 21.
    Ringdahl, B. and Jenden, D.J. (1983): Life Sci. 32: 2401–2413.CrossRefGoogle Scholar
  22. 22.
    Ringdahl, B., Resul, B., Jenden, D.J. and Dahlbom, R. (1982): Eur. J. Pharmacol. 85: 79–83.CrossRefGoogle Scholar
  23. 23.
    Ruffolo, R.R., Jr. (1982): J. Auton. Pharmacol. 2: 277–295.CrossRefGoogle Scholar
  24. 24.
    Sastry, B.V.R. and Cheng, H.C. (1972): J. Pharmacol. Exp. Ther. 180: 326–339.Google Scholar
  25. 25.
    Siegel, H. and Triggle, D.J. (1982): Life Sci. 30: 1645–1652.CrossRefGoogle Scholar
  26. 26.
    Stephenson, R.P. (1956): Brit. J. Pharmacol. 11: 379–393.Google Scholar
  27. 27.
    Takeyasu, K., Uchida, S., Wada, A., Maruno, M., Lai, R.T., Hata, F. and Yoshida, H. (1979): Life Sci. 25: 1761–1772.CrossRefGoogle Scholar
  28. 28.
    Waud, D.R. (1969): J. Pharmacol. Exp. Ther. 170: 117–122.Google Scholar
  29. 29.
    Yamamura, H.I. and Snyder, S.H. (1974): Mol. Pharmacol. 10: 861–867.Google Scholar

Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • B. Ringdahl
    • 1
  1. 1.Department of Pharmacology School of MedicineUniversity of CaliforniaLos AngelesUSA

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