VI. EFFECTS OF THE ANTI-ANDROGEN TSAA-291 AND ITS RELATED COMPOUNDS ON THE IN VITRO FORMATION OF 5α-DHT-Receptor COMPLEX IN THE CYTOSOL OF RAT VENTRAL PROSTATES

Sudo, Katsuichi; Yoshida, Kentaroh; Nakayama, Ryo

doi:10.1530/acta.0.092s082

Cited by 6 publications

(2 citation statements)

References 7 publications

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“…Further, the binding was effectively replaced by such androgens and antiandrogens as 5a-DHT, 19-nortestosterone, TSAA-29 1 and cyproterone acetate. The number of bind¬ ing sites for TSAA-291 calculated by Scatchard analysis was comparable to the estimate for 5CX-DHT (Sudo et al 1979b). In addition, the maximally displaced level of the binding caused by unlabelled TSAA-291 was equal to that caused by unlabelled 5a-DHT (Fig.…”

Section: Discussionsupporting

confidence: 65%

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Specific interaction of radioactive anti-androgen TSAA-291 with androgen receptor in rat prostates

Sudo

Yoshida

Nakayama

1982

Acta Endocrinologica

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A steroidal anti-androgen TSSA-291 ( 16\ g=b\ \ x=r eq-\ ethyl-17\g=b\-hydroxy-4-oestren-3-one) bound to a macromolecular component in the cytosol of rat ventral prostates with high affinity (Kd = 5.0 \m=x\10\m=-\9 m) and in a saturable manner. The number of binding sites was comparable to that for 5\g=a\-dihydrotestosterone( 5\ g=a\ \ x=r eq-\ DHT).[3H]TSAA-291 binding was effectively displaced by unlabelled 5\g=a\-DHT,19-nortestosterone and cyproterone acetate but to a lesser degree by corticosterone. Glycerol density-gradient centrifugation analysis revealed that the sedimentation coefficeint of the [ 3H] \ x=r eq-\ TSAA-291-macromolecule complex was 3\p=n-\4.5 S. However, when the unlabelled cytosol was fractionated by glycerol density-gradient centrifugation before the binding of [3H]TSAA-291 was examined, specific binding of [3H]TSAA-291 was observed in fractions corresponding to 8\p=n-\10 S. Binding of the [3H]TSAA-291-macromolecules complex to prostatic nuclei and DNA-cellulose was considerably less than binding by the [3H]5\g=a\-DHT\x=req-\ macromolecule complex. Instability of the TSAA-291 binding component on heat treatment before and after complex formation was also revealed and the results are discussed in terms of the anti-androgenic activity of TSAA-291.

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Section: Discussionsupporting

confidence: 65%

“…At least three experiments were repeated for each centrifu¬ gation pattern. Details of the centrifugation procedure were as described previously (Sudo et al 1979b). …”

Section: Methodsmentioning

confidence: 99%

Specific interaction of radioactive anti-androgen TSAA-291 with androgen receptor in rat prostates

Sudo

Yoshida

Nakayama

1982

Acta Endocrinologica

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Biochemical difference between ventral and dorsolateral prostates: Effects of castration and administration of the antiandrogen 16β‐ethyl‐17β‐hydroxy‐4‐oestren‐3‐one on SDS‐electrophoretic patterns of subcellular proteins from rat prostates

1984

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Protein species in the cytosol, postnuclear particulate, and nuclear fractions from the ventral and dorsolateral prostates of rats castrated or injected with antiandrogen, 16 beta-ethyl-17 beta-hydroxy-4- oestren -3-one ( EHOO ), were analyzed by SDS-polyacrylamide gel electrophoresis. The effects of EHOO injection on the contents of the most abundant species in all three fractions of ventral prostate were similar to the effects of castration, but the effects of EHOO and castration were only similar on the nuclear fraction in the dorsolateral prostate. The most sensitive species to castration in the three subcellular fractions of dorsolateral prostate were the same as those to EHOO injections; this was not the case for the cytosol and nuclear fractions in the ventral prostate.

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Antiandrogenic treatment of benign prostatic hyperplasia: a placebo controlled trial

et al. 1989

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In a randomized triple-blind multicentre study, injections with the anti-androgenic agent oxendolone were compared with placebo in the treatment of benign prostatic hyperplasia. Thirty patients were treated with weekly injections of oxendolone 200 mg during a 3 months' period, and 30 patients were allocated to placebo treatment. During oxendolone treatment the maximum urinary flow rate increased statistically significantly (from 6.8 ml/s to 8.2 ml/s). However compared to placebo, the oxendolone effect was statistically insignificant. A slight but statistically significant improvement of the symptoms "sensation of retention", "urgency" and "frequency", was observed following oxendolone treatment, but an almost identical effect was seen in the placebo group. Following either treatment no change was observed in the residual urine volumes, in prostatic volume as measured by transrectal ultrasonotomography, or in any other therapeutic parameters. Conservative treatment of benign prostatic hyperplasia with the antiandrogen oxendolone in a dose of 200 mg a week cannot be recommended for clinical use.

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VI. EFFECTS OF THE ANTI-ANDROGEN TSAA-291 AND ITS RELATED COMPOUNDS ON THE IN VITRO FORMATION OF 5α-DHT-Receptor COMPLEX IN THE CYTOSOL OF RAT VENTRAL PROSTATES

Cited by 6 publications

References 7 publications

Specific interaction of radioactive anti-androgen TSAA-291 with androgen receptor in rat prostates

Specific interaction of radioactive anti-androgen TSAA-291 with androgen receptor in rat prostates

Biochemical difference between ventral and dorsolateral prostates: Effects of castration and administration of the antiandrogen 16β‐ethyl‐17β‐hydroxy‐4‐oestren‐3‐one on SDS‐electrophoretic patterns of subcellular proteins from rat prostates

Antiandrogenic treatment of benign prostatic hyperplasia: a placebo controlled trial

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