Neurochemical Research

, Volume 11, Issue 11, pp 1565–1569 | Cite as

Azidomorphine is an agonist of high-affinity opioid receptor binding sites

  • Katalin Horváth
  • Mária Wollemann
Original Articles


Azidomorphine at low concentration (10−9 M) inhibits the high-affinity binding site of labeled naloxone in rat brain membrane preparations. In the presence of Na+ and guanine nucleotides the displacement curves of azidomorphine are increased toward high concentrations, whereas Mg2+ ions decrease the IC50 values; This demonstrates the agonist behavior of azidomorphine in binding experiments. When compared with morphine, azidomorphine displayed five-fold lower IC50 values. Based on the presented results, azidomorphine appears to be a good candidate for photoaffinity labeling of opiate receptors.


Morphine Guanine Naloxone Receptor Binding Opioid Receptor 
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.
    Knoll, J. 1979. Azidomorphine: a new family of potent analgesics with low dependence capacity. Prog. Neuro-Psychopharmacol. 3:95–108.Google Scholar
  2. 2.
    Knoll, J. 1973. Azidomorphine and Rymazolium an approach to the ideal analgesic. Pharmacol. Res. Commun. 5:175–185.Google Scholar
  3. 3.
    Knoll, J., Fürst, S., andKeleman, K. 1973. The pharmacology of azidomorphine and azidocodeine. J. Pharm. Pharmacol. 25:929–939.Google Scholar
  4. 4.
    Knoll, J., Fürst, S., andVizi, E. S. 1973. Kinetic parameters of a new narcotic agonist azidomorphine. Pharmacology 10:154–162.Google Scholar
  5. 5.
    Tóth, G., Krámer, M., Sirokmán, F., Borsodi, A., andRónai, A. J. 1982. Preparation of [7,8,19,20-3H]naloxone of high specific activity. Labeled Comp. and Radiopharm. 19:1021–1030.Google Scholar
  6. 6.
    Tóth, G., Kramer, M., Szücs, M., Benyhe, S., andSirokmán, F. 1982. Preparation of [1,7,8-3H]dihydromorphine of high molar activity and its application in opiate receptor binding experiments. Radiochem. Radioanal. Lett. 56:209–216.Google Scholar
  7. 7.
    Bognár, R., andMakleit, S. 1968. Conversion of tosyl and mesyl derivatives of the morphine group. II. Aminomorphides and aminocodides. Acta Chim. Acad. Sci. Hung. 58:203–205.Google Scholar
  8. 8.
    Pasternak, G. W., Wilson, H. A., andSnyder, S. H. 1975. Differential effects of protein-modifying reagents on receptor binding of opiate agonists and antagonists. Mol. Pharmacol. 11:340–351.Google Scholar
  9. 9.
    Peterson, G. L. 1977. A simplification of the protein assay method of Lowry et al. which is more generally applicable. Anal. Biochem. 83:346–356.Google Scholar
  10. 10.
    Zhang, A. Z., Pasternak, G. W. 1981. Opiates and enkephalins: a common binding site mediates their analgesic actions in rats. Life Sci. 29:843–851.Google Scholar
  11. 11.
    Knoll, J., andZsilla, G. 1974. Possible mechanism of the low tolerance capacity of azidomorphine and azidocodeine. Biochem. Pharmacol. 23:745–750.Google Scholar

Copyright information

© Plenum Publishing Corporation 1986

Authors and Affiliations

  • Katalin Horváth
    • 1
  • Mária Wollemann
    • 1
  1. 1.Institute of Biochemistry Biological ResearchCenter of Hungarian Academy of SciencesSzegedHungary

Personalised recommendations