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In vitro covalent binding of /sup 14/C-mibolerone to rat liver microsomes

Journal Article · · Adv. Exp. Med. Biol.; (United States)

Mibolerone (17-Hydroxy-7,17-dimethylestr-4-en-3-one; 7 alpha-17 alpha dimethyl-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 /sup 14/C-mibolerone at 37/sup 0/C for 10 minutes. No covalent binding to macromolecules was observed when /sup 14/C-mibolerone was incubated with rat liver microsomes. Under identical conditions, /sup 14/C-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.

Research Organization:
Upjohn Co., Kalamazoo, MI
OSTI ID:
7189188
Journal Information:
Adv. Exp. Med. Biol.; (United States), Journal Name: Adv. Exp. Med. Biol.; (United States); ISSN AEMBA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANESTHETICS
ANIMALS
ANTICONVULSANTS
AZINES
BARBITURATES
BODY
CARBON 14 COMPOUNDS
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM DEPRESSANTS
CHEMICAL BONDS
DIGESTIVE SYSTEM
DRUGS
ESTRADIOL
ESTRANES
ESTROGENS
GLANDS
HETEROCYCLIC COMPOUNDS
HORMONE ANTAGONISTS
HORMONES
HYDROXY COMPOUNDS
HYPNOTICS AND SEDATIVES
IN VITRO
INHIBITION
LABELLED COMPOUNDS
LIVER
MAMMALS
MEMBRANE PROTEINS
MICROSOMES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANOIDS
ORGANS
PHENOBARBITAL
PROTEINS
PYRIMIDINES
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
TRITIUM COMPOUNDS
VERTEBRATES