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In Vitro Covalent Binding of 14C-Mibolerone to Rat Liver Microsomes

  • P. S. Jaglan
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 197)

Abstract

Mibolerone (17-Hydroxy-7,17-dimethylestr-4-en-3-one; 7α-17αdimethyl-19-nortestosterone) is being marketed by The Upjohn Company for the inhibition of estrus in bitches. The aim of this study was to determine the extent of covalent binding of mibolerone to rat liver microsomes. Liver microsomes were obtained from Control and phenobarbitol-treated female Fisher rats, and were incubated with 14C-mibolerone at 37°C for 10 minutes. No covalent binding to macromolecules was observed when 14C-mibolerone was incubated with rat liver microsomes. Under identical conditions, 14C-estradiol was covalently bound to macromolecules. Slightly higher covalent binding of estradiol was observed with microsomes from phenobarbitol-treated rats. Ascorbic acid and glutathione inhibited covalent binding of estradiol to macromolecules in the in vitro microsomal system.

Keywords

Ascorbic Acid Liver Microsome Reactive Intermediate Complete System Covalent Binding 
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.

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References

  1. 1.
    J. A. Miller, Cancer Res., 30, 559–576 (1970).PubMedGoogle Scholar
  2. 2.
    E. C. Miller and J. A. Miller, Pharmacol. Rev., 18, 805–838 (1966).PubMedGoogle Scholar
  3. 3.
    P. N. Magee and J. M. Barnes, Adv. Cancer Res., 10, 163–246 (1967).PubMedCrossRefGoogle Scholar
  4. 4.
    R. O. Recknagel, Pharmacol. Rev., 19, 145–208 (1967).PubMedGoogle Scholar
  5. 5.
    G. J. Traiger and G. L. J. Plaa, Pharmacol. Exp. Therap., 183, 481 (1972).Google Scholar
  6. 6.
    J. R. Mitchell, D. J. Jollow, J. R. Gillette, and B. B. Brodie, Drug Metab. Dispos., 1, 418–423 (1973).PubMedGoogle Scholar
  7. 7.
    J. R. Gillette, J. R. Mitchell, and B. B. Brodie, Ann. Rev. Pharmacol., 14, 271–288 (1974).CrossRefGoogle Scholar
  8. 8.
    J. R. Mitchell, D. J. Jollow, and J. R. Gillette, Israel J. Med. Sci., 10, 339–345 (1974).Google Scholar
  9. 9.
    J. R. Mitchell and D. J. Jollow, Israel J. Med. Sci., 10, 312–318 (1974).Google Scholar
  10. 10.
    J. R. Mitchell and D. J. Jollow, Gastroenterology, 68, 392–410 (1975).PubMedGoogle Scholar
  11. 11.
    D. M. Jerina and J. W. Daly, Science, 185, 573–582 (1974).PubMedCrossRefGoogle Scholar
  12. 12.
    S. D. Nelson, M. R. Boyd, and J. R. Mitchell, Drug Metabolism Concepts: ACS Symposium Series, 44, 155–185 (1977).CrossRefGoogle Scholar
  13. 13.
    S. D. Nelson, J. R. Mitchell, E. Dybing, and H. A. Sasame, Biochem. Biophys. Res. Comm., 70, 1157–1165 (1976).PubMedCrossRefGoogle Scholar
  14. 14.
    O. H. Lowry, N. J. Rosenbrough, A. Farr, and R. Randall, J. Biol. Chem., 193, 265–271 (1951).PubMedGoogle Scholar
  15. 15.
    N. Nishikimi, Biochem. Biophys. Res. Comm., 63, 463–468 (1975).PubMedCrossRefGoogle Scholar
  16. 16.
    T. R. Tephly, C. Webb, P. Trussler, F. Kniffer, E. Hasegawa, and W. Pipor, Drug Metab. Dispos., 1, 259–266 (1973).PubMedGoogle Scholar

Copyright information

© Plenum Press, New York 1986

Authors and Affiliations

  • P. S. Jaglan
    • 1
  1. 1.Biochemistry and Residue AnalysisThe Upjohn CompanyKalamazooUSA

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