In vitro binding of 16-methylated C18 and C19 steroid derivatives to the androgen receptor

Istvan Toth, Imre Faredin, Eszter Mesko, J. Wölfling, G. Schneider

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The binding of androgens and structurally related analogues to the androgen receptor was studied. The in vitro experiments were carried out with cytosol of castrated rat prostate, using [3H]R1881 (methyltrienolone) as radioligand. The binding parameters measured were Kd=1.25 × 10-10 m and Bmax=111 fmol (mg protein)-1. Ligand specificity was confirmed by competition experiments with known androgen, oestrogen and progestogen ligands. The receptor binding of substituted steroids was studied. The RBAs (relative binding affinities) of our recently synthetized 16-alkyl steroids were low. The only exception was the 17β-hydroxy-16β-methylestr-4-en-3-one, which exhibited the remarkable RBA of 22.9%.

Original languageEnglish
Pages (from-to)217-221
Number of pages5
JournalPharmacological Research
Volume32
Issue number4
DOIs
Publication statusPublished - 1995

Fingerprint

Metribolone
Androgen Receptors
Androgens
Steroids
Ligands
Progestins
Cytosol
Prostate
Estrogens
Proteins
In Vitro Techniques

Keywords

  • 16-alkyl steroids
  • androgen receptor binding

ASJC Scopus subject areas

  • Pharmacology

Cite this

In vitro binding of 16-methylated C18 and C19 steroid derivatives to the androgen receptor. / Toth, Istvan; Faredin, Imre; Mesko, Eszter; Wölfling, J.; Schneider, G.

In: Pharmacological Research, Vol. 32, No. 4, 1995, p. 217-221.

Research output: Contribution to journalArticle

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