Role of dihydrotestosterone in androgen action

  title={Role of dihydrotestosterone in androgen action},
  author={Jean D. Wilson},
  journal={The Prostate},
Androgen action differs from that of most hormones in that testosterone, the major androgen secreted from the testes and the most abundant androgen in the circulation of men, is not the principal androgen within target cells. Indeed, abundant evidence indicates that most androgen actions are mediated by the 5α‐reduced metabolite dihydrotestosterone that is formed in target tissues. The conversion of testosterone to dihydrotestosterone is mediated by two isoenzymes; mutations in the steroid 5… 

Regulation of androgen action.

Safety aspects of androgen treatment with 5α‐dihydrotestosterone

Safety concerns regarding androgen treatment with DHT are similar to those of treatment with testosterone, while the effects of DHT on the prostate are likely to be less biopotent.

The Androgen Receptor, Androgen Insensitivity, and Prostate Cancer

In mammals, two steroids, testosterone and its 5α-reduced metabolite 5 α-dihydrotestosterone (5α-DHT) serve as the principal circulating androgens.

Androgen Regulation of 5α-Reductase Isoenzymes in Prostate Cancer: Implications for Prostate Cancer Prevention

It is found that androgen regulates the mRNA level of 5α-reductase isoenzymes in a cell type–specific manner, that regulation occurs at the transcriptional level, and that AR is necessary for this regulation.

Plasma levels of dihydrotestosterone remain in the normal range in men treated with long‐acting parenteral testosterone undecanoate

Treatment with testosterone undecanoate generates physiological levels of DHT, and the resulting plasma DHT levels in 122 hypogonadal men treated with a novel testosterone treatment modality were investigated.

Androgen Biosynthesis And Degradation

Androgens are important male sex steroid hormones that exert many physiological functions leading to the male characteristics and other phenotypes. The major circulating androgen is testosterone (T)

Molecular Biology of the Androgen Receptor: From Molecular Understanding to the Clinic

The most important findings about the AR and the androgen signaling pathway are summarized to improve the understanding of prostate diseases and novel treatment strategies that may be useful in the clinic.



Testosterone at high concentrations interacts with the human androgen receptor similarly to dihydrotestosterone.

The results suggest that the weaker androgenic potency of testosterone compared to that of dihydrotestosterone resides in its weaker interaction with the androgen receptor, most clearly demonstrable as an increase in the dissociation rate of testosterone from the receptor.

Selective Retention of Dihydrotestosterone by Prostatic Nuclei

Nuclear chromatin of prostate, but not other tissues which are insensitive to androgen, contains an androgen receptor which can selectively retain dihydrotestosterone (DHT, 5α-androstane-17β-ol-3-one)—the most potent endogenous androgen for the growth of ventral prostate of rat13,14.

Steroid 5 alpha-reductase 2 deficiency.

It is imperative to establish whether defects in steroid 5 alpha-reductase 2, perhaps in the heterozygous state, are responsible for a portion of cases of sporadic hypospadias, to determine whether 5alpha- reductase plays a role in progesterone action in women, and to elucidate the relation between androgen action and gender role behavior.

Metabolism of testosterone by the human prostate.

In vitro studies on rat-ventral and monkey-caudal prostate minces have shown that a 10 -7 M concentration of testosterone significantly accelerates incorporation of amino acids into protein and of acetate into fatty acids and citric acid.

The Effect of a 5α;-Reductase Inhibitor on Androgen Mediated Growth of the Dog Prostate

The administration of testosterone cypionate to castrated male dogs caused a doubling of prostate weight within 4 weeks and an increase in the content of testosterone and dihydrotestosterone in the prostate, and results suggest that dihydratestosterone formation plays a role in prostatic growth.

The pathogenesis of benign prostatic hyperplasia.

  • J. D. Wilson
  • Medicine, Biology
    The American journal of medicine
  • 1980

Deletion of steroid 5α-reductase 2 gene in male pseudohermaphroditism

The results verify the existence of at least two 5α-reductases in man and provide insight into a fundamental hormone-mediated event in male sexual differentiation.

Comparison of the metabolites formed in rat prostate following the in vivo administration of seven natural androgens.

The incorporation of radioactivity by rat prostate has been measured following administration of seven tritium-labeled natural androgens to separate groups of castrated functionally hepatectomized rats and dihydrotestosterone consistently was found to be the major metabolite.