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Use of radioactive 7alpha, 17alpha-dimethyl-19-nortestosterone (mibolerone) in the assay of androgen receptors

Journal Article · · Prostate (N.Y.); (United States)
OSTI ID:6005324
;
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), Journal Name: Prostate (N.Y.); (United States) Vol. 5:6; ISSN PRSTD
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANDROGENS
ANDROSTANES
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CELL CULTURES
COMPLEXES
DIGESTIVE SYSTEM
ESTRADIOL
ESTRANES
ESTROGENS
GLANDS
HORMONES
HYDROXY COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIVER
MALE GENITALS
MAMMALS
ORGANIC COMPOUNDS
ORGANS
PROSTATE
RATS
REACTION KINETICS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES