Use of radioactive 7alpha, 17alpha-dimethyl-19-nortestosterone (mibolerone) in the assay of androgen receptors
Tritiated 7alpha, 17alpha-dimethyl-19-nortestosterone (DMNT; mibolerone), a synthetic androgen stable to metabolic conversion in the rat ventral prostate, is an excellent radioactive ligand for the quantitation and characterization of androgen receptors in prostate, liver, and cultured cells. DMNT is more receptor-selective than 17alpha-methyl-17beta-hydroxy-estra-4,9,11-trien-3-one (R1881); DMNT interacts with glucocorticoid and progestin receptors much less strongly than R1881. Unlike 5alpha-dihydrotestosterone, DMNT does not bind tightly to testosterone-estradiol binding globulin of human serum. The hydroxylapatite-filter assay employed clearly distinguished between DMNT binding to androgen receptors of rat ventral prostate and interaction of DMNT with androgen binding protein of epididymides. The prostate cytosol (/sup 3/H)DMNT-receptor complex sediments in two forms (4 and 8 S) in a low salt medium. In 0.4 M KCl, both the prostate cytosol and nuclear (/sup 3/H)DMNT-receptor complexes migrated as 3-4 S components. The formation of both the cytosol and nuclear DMNT-receptor complexes is inhibited by antiandrogens and 17beta-estradiol.
- Research Organization:
- Univ. of Chicago, IL
- OSTI ID:
- 6005324
- Journal Information:
- Prostate (N.Y.); (United States), Vol. 5:6
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
ANDROGENS
BIOCHEMICAL REACTION KINETICS
ESTRADIOL
RECEPTORS
CELL CULTURES
COMPLEXES
LIVER
PROSTATE
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANDROSTANES
ANIMALS
BODY
DIGESTIVE SYSTEM
ESTRANES
ESTROGENS
GLANDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MALE GENITALS
MAMMALS
ORGANIC COMPOUNDS
ORGANS
REACTION KINETICS
RODENTS
STEROID HORMONES
STEROIDS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques