A new triphenylethylene compound, Fc-1157a. I: Hormonal effects

The basic pharmacological and biochemical properties of a new antiestrogen, Fc-1157a, are described. Fc-1157a is bound specifically and with high affinity to estrogen receptors. The binding is competitive with estradiol. Fc-1157a treatment induces translocation of estrogen receptors from cytoplasm t...

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Bibliographic Details
Published in:Cancer chemotherapy and pharmacology 1986-06, Vol.17 (2), p.103-108
Main Authors: KALLIO, S, KANGAS, L, BLANCO, G, JOHANSSON, R, KARJALAINEN, A, PERILA, M, PIPPO, I, SUNDQUIST, H, SODERVALL, M, TOIVOLA, R
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Biological and medical sciences
Biological Transport - drug effects
Cell Nucleus - metabolism
Cytosol - metabolism
Estradiol - pharmacology
Estrogen Antagonists
Female
General aspects
Medical sciences
Mice
Ovariectomy
Pharmacology. Drug treatments
Rats
Receptors, Estrogen - drug effects
Receptors, Estrogen - metabolism
Receptors, Progesterone - metabolism
Tamoxifen - analogs & derivatives
Tamoxifen - pharmacology
Toremifene
Uterus - drug effects
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Summary:The basic pharmacological and biochemical properties of a new antiestrogen, Fc-1157a, are described. Fc-1157a is bound specifically and with high affinity to estrogen receptors. The binding is competitive with estradiol. Fc-1157a treatment induces translocation of estrogen receptors from cytoplasm to nucleus. The turnover rate of nuclear estrogen receptors is markedly lower than with estradiol, but is more rapid than after tamoxifen. Fc-1157a is an almost pure antiestrogen in rat uterus, but has intrinsic estrogenic activity in mouse uterus. In animal experiments Fc-1157a has shown antitumor properties, which are described in the companion paper.
ISSN:0344-5704
1432-0843
DOI:10.1007/BF00306736