Jan 1, 1978

Characterization of the binding of a potent synthetic androgen, methyltrienolone, to human tissues

The Journal of Clinical Investigation
M MenonP C Walsh

Abstract

The potent synthetic androgen methytrienolone (R 1881), which does not bind to serum proteins, was utilized to characterize binding to receptors in human androgen responsive tissues. Cytosol extracts prepared from hypertrophic prostates (BPH) were utilized as the source of receptor for the initial studies. High affinity binding was detected in the cytosol of 29 of 30 samples of BPH (average number of binding sites, 45.8+/-4.7 fmol/mg of protein; dissociation constant, 0.9+/-0.2 nM). This binding had the characteristics of a receptor: heat lability, precipitability by 0-33% ammonium sulfate and by protamine sulfate, and 8S sedimentation coefficient. High affinity binding was also detected in cytosol prepared from seminal vesicle, epididymis, and genital skin but not in non-genital skin or muscle. However, similar binding was demonstrated in the cytosol of human uterus. The steroid specificities of binding to the cytosol of male tissues of accessory reproduction and of uterus were similar in that progestational agents were more effective competitors than natural androgens. Binding specificities in cytosol prepared from genital skin were distinctly different and were similar to those of ventral prostate from the castrated rat in t...Continue Reading

  • References13
  • Citations30

References

  • References13
  • Citations30

Citations

Mentioned in this Paper

Androgen Receptor
Dihydrotestosterone Assay
Exertion
Specimen Type - Genital
R-1881
Protamine Sulfate (USP)
Scrotum
Benign Neoplasm of Epididymis
Epididymis Disorders
Entire Uterus

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