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)


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.


Ascorbic Acid Liver Microsome Reactive Intermediate Complete System Covalent Binding 
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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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