No loss of estrogenic or anti-estrogenic activity after demethylation of droloxifene (3-OH-Tamoxifen)
✍ Scribed by R. Löser; K. Seibel; U. Eppenberger
- Book ID
- 102278764
- Publisher
- John Wiley and Sons
- Year
- 1985
- Tongue
- French
- Weight
- 254 KB
- Volume
- 36
- Category
- Article
- ISSN
- 0020-7136
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✦ Synopsis
The bindin affinity of 3-OH-Tamoxifen (Droloxifene or DR8L) and N-demethyl-droloxifene (ND-DROL) to the cystosolic estrogen receptor of rabbit uteri was 10 times higher than that of Tamoxifen. Both compounds exhibited similar stimulation (estrogenic effect) and inhibition (anti-estrogenic effect) of uterine growth of immature female rats. 3H-Uridine incorporation into the RNA of MCF-7 and ZR-75 cells as a measure of anti-estrogenic activity was equally inhibited by concentrations of 0.05 -1.0 pmolll of both compounds. Thus, the pharmacological properties of DROL were not changed by N-demethylation.