Inhibition of Nuclear Testosterone 5α-Reductase in Rat Ventral Prostate by Estrogens and Anti-Androgens

Shimazaki, Jun; Ohki, Yumiko; Koya, Atsushi; Shida, Keizo

doi:10.1507/endocrj1954.19.585

Cited by 20 publications

(4 citation statements)

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“…Steins et al(1974) reported that the binding rate with dihydrotestosterone of glandular type of the hypertrophic prostate was higher than that of the poor glandular type. In the present study, the proportion of glandular constituent in hypertrophic prostates was not correlated with binding affinity to dihydrotestosterone, and this might be due to the disparity of histological (Tveter, 1971;Shimazaki et al, 1972;Nozu and Tamaoki, 1975), and the present experiments also confirmed these results. Sch 13521 was a potent anti-androgen (Neri et al, 1972), but its mechanism of action was still disputable.…”

Section: Binding Capacity Of Acetone-dried Cytosolsupporting

confidence: 79%

Dihydrotestosterone-binding protein in cytosols of normal and hypertrophic human prostates, and influence of estrogens and anti-androgens on the binding.

et al. 1977

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Section: Binding Capacity Of Acetone-dried Cytosolsupporting

confidence: 79%

Dihydrotestosterone-binding protein in cytosols of normal and hypertrophic human prostates, and influence of estrogens and anti-androgens on the binding.

et al. 1977

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“…Mit einem 17a-östradiolhaltigen Haarwasser erreichten wir bei 63% unserer Patienten eine Besserung, während mit 17ß-östradiolhaltigen Haarwässern bei 58% der Patienten eine entsprechende Senkung der Telogenrate um mehr als 10% auftrat [9], Somit, falls die Hemmung der 5a-Reduktase der entscheidende Wirkungsmechanismus bei der lokalen Östro gentherapie ist, spielt die Östrogene Potenz der verschiedenen Derivate für ihre therapeutische Anwendung keine Rolle. Auch in vitro ist das Ausmass der Enzymhemmung von der Östrogenen Potenz der einzelnen Derivate offenbar unabhängig [8], Die Seborrhoea oleosa, die bei nur 7 Patienten der Behandlungsgruppe zurückging, ist lokaltherapeutisch offenbar schwer zu beeinflussen. Dies ha ben bereits Pochi und Strauss [5] dokumentiert: Mit 17ß-Östradiol konnte die Talgproduktion nicht gehemmt werden.…”

Section: Diskussionunclassified

Lokaltherapie der Alopecia androgenetica mit 17α-Östradiol

Orfanos

Vogels²

1980

Dermatology

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In a controlled, randomized double-blind study, 51 patients with androgenetic alopecia and increased hair loss (telogen rate > 20%) were treated by local application of hair lotions with and without 17α-estradiol (0.025%) for a period of at least 6 months. Before and after therapy trichograms were taken and evaluated under standardized conditions. In 63% of the treated patients a reduction of the amount of telogen hairs appeared, whereas in the control group the same reduction was found in only 37% of the cases. Similarly, in the treated group only 11% of the patients worsened, in contrast to 50% of the control group who showed an increased telogen rate (> 10%). The amount of growing anagen hairs and of seborrhea did not change significantly in both groups. Side effects were not seen. These findings indicate that hair lotions containing 17α-estradiol may have a therapeutic value in reducing androgenetic hair loss, if applied topically for a long period of time, similar to 17β-estradiol. However, no regrowth of new hair was found.

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“…on this enzyme is well known and has been documented several times (Lee et al 1973a,b;Shimazaki et al 1971Shimazaki et al , 1972. on this enzyme is well known and has been documented several times (Lee et al 1973a,b;Shimazaki et al 1971Shimazaki et al , 1972.…”

Section: Discussionmentioning

confidence: 95%

The EFFECT OF OESTRADIOL-3N-BIS-(2-CHLOROETHYL)CARBAMATE-17β-PHOSPHATE (ESTRACYT®) ON THE 5α-Reductase IN THE RAT VENTRAL PROSTATE

Høisæter¹

1975

Acta Endocrinologica

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The ventral prostate of the rat both after in vitro incubation and in vivo experiments was found to contain appreciable 5\g=a\-reductaseactivity, whilst a very low activity was registered in the diaphragm and liver. Neither Estracyt\s=r\ nor LEO275 (Estracyt\s=r\ without the phosphate group in position 17 of the oestradiol moiety) had an inhibitory effect on the enzyme activity after in vitro incubation but equivalent amounts of oestradiol-17\g=b\ and oestradiol-17\g=b\-phosphatesignificantly reduced 5\ g=a\ \ x=r eq-\ reductase activity. When Estracyt\s=r\ was injected in vivo no influence on activity was registered in "short term" experiments while a significant inhibition was found after "long term" treatment in vivo. Possible explanations for this "long term" effect of Estracyt\s=r\ on 5\g=a\-reductase activity are discussed.

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Inhibition of Nuclear Testosterone 5α-Reductase in Rat Ventral Prostate by Estrogens and Anti-Androgens

Cited by 20 publications

References 1 publication

Dihydrotestosterone-binding protein in cytosols of normal and hypertrophic human prostates, and influence of estrogens and anti-androgens on the binding.

Dihydrotestosterone-binding protein in cytosols of normal and hypertrophic human prostates, and influence of estrogens and anti-androgens on the binding.

Lokaltherapie der Alopecia androgenetica mit 17α-Östradiol

The EFFECT OF OESTRADIOL-3N-BIS-(2-CHLOROETHYL)CARBAMATE-17β-PHOSPHATE (ESTRACYT®) ON THE 5α-Reductase IN THE RAT VENTRAL PROSTATE

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