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IARC Monographs on the Evaluation of... Dec 1979
Review
Topics: Animals; Carcinogens; Chemical Phenomena; Chemistry; Cricetinae; Dogs; Female; Haplorhini; Humans; Male; Mestranol; Mice; Pregnancy; Rats; Teratogens
PubMed: 120834
DOI: No ID Found -
Acta Poloniae Pharmaceutica 1994The aim of this study was to investigate the effect of mestranol on pharmacokinetics of paracetamol. The study was carried out on 20 female rabbits. Paracetamol was...
The aim of this study was to investigate the effect of mestranol on pharmacokinetics of paracetamol. The study was carried out on 20 female rabbits. Paracetamol was administered to rabbits intragastrically at a dose of 50 mg/kg b.w. One group of animals was given mestranol intragastrically 0.1 mg once daily during 2 months. The method of Routh A. et al. was used to paracetamol concentration assay. Blood for the assays was collected within 24 hours after drug administration, prior to the study as well as 1 month and 2 months after continuous mestranol administration. The two compartment open model was used for calculations. The study revealed an increase in AUC and paracetamol half-life as well as decrease in the total body clearance. We conclude that there is an interaction between mestranol and paracetamol leading to a decrease in total body paracetamol clearance.
Topics: Acetaminophen; Animals; Drug Interactions; Female; Mestranol; Metabolic Clearance Rate; Rabbits
PubMed: 7863788
DOI: No ID Found -
Ceskoslovenska Farmacie Dec 1966
Topics: Chemistry, Pharmaceutical; Mestranol
PubMed: 5980772
DOI: No ID Found -
Acta Endocrinologica Aug 1969
Topics: Carbon Isotopes; Female; Humans; Lactation; Lynestrenol; Mestranol; Milk, Human; Pregnancy
PubMed: 5409087
DOI: 10.1530/acta.0.0610665 -
Xenobiotica; the Fate of Foreign... Sep 1972
Topics: Animals; Body Water; Brain; Carbon Isotopes; Ethinyl Estradiol; Feces; Female; Injections, Intraperitoneal; Injections, Intravenous; Liver; Lung; Mestranol; Mice; Rats; Tritium
PubMed: 4649044
DOI: 10.3109/00498257209111077 -
Journal of the American Geriatrics... Oct 1966
Topics: Adult; Climacteric; Female; Humans; Menopause; Mestranol; Middle Aged; Norethynodrel; Vaginal Smears; White People
PubMed: 5924635
DOI: 10.1111/j.1532-5415.1966.tb02880.x -
ChemMedChem Jan 2017Anticancer structure-activity relationship studies on aminosteroid (5α-androstane) derivatives have emerged with a promising lead candidate: RM-133...
Anticancer structure-activity relationship studies on aminosteroid (5α-androstane) derivatives have emerged with a promising lead candidate: RM-133 (2β-[1-(quinoline-2-carbonyl)pyrrolidine-2-carbonyl]-N-piperazine-5α-androstane-3α,17β-diol), which possesses high in vitro and in vivo activities against several cancer cells, and selectivity over normal cells. However, the relatively weak metabolic stability of RM-133 has been a drawback to its progression toward clinical trials. We investigated the replacement of the androstane backbone by a more stable mestranol moiety. The resulting compound, called RM-581 ({4-[17α-ethynyl-17β-hydroxy-3-methoxyestra-1,3,5(10)-trien-2-yl]piperazin-1-yl}[(2S)-1-(quinolin-2-ylcarbonyl)pyrrolidin-2-yl]methanone), was synthesized efficiently in only five steps from commercially available estrone. In comparison with RM-133, RM-581 was found to be twice as metabolically stable, retains potent cytotoxic activity in breast cancer MCF-7 cell culture, and fully blocks tumor growth in a mouse xenograft model of breast cancer. Advantageously, the selectivity over normal cells has been increased with this estrane version of RM-133. In fact, RM-581 showed a better selectivity index (15.3 vs. 3.0) for breast cancer MCF-7 cells over normal breast MCF-10A cells, and was found to be nontoxic toward primary human kidney proximal tubule cells at doses reaching 50 μm.
Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Design; Female; Humans; MCF-7 Cells; Mestranol; Mice; Mice, Nude; Transplantation, Heterologous
PubMed: 28060448
DOI: 10.1002/cmdc.201600482 -
Steroids Feb 1985The 1H- and 13C-nmr spectra of mestranol were assigned with the help of a 2 D-J-resolved, a 2D spin echo J-correlated (SECSY) and a 2D 1H-13C hetero-shift correlation...
The 1H- and 13C-nmr spectra of mestranol were assigned with the help of a 2 D-J-resolved, a 2D spin echo J-correlated (SECSY) and a 2D 1H-13C hetero-shift correlation experiment. The analysis of the spectra facilitated the identification of some of the photodecomposition products of mestranol. It was shown that, upon irradiation with UV-B light in water-ethanol (1:1, v/v), products are formed by oxidation of rings B and C of the steroid.
Topics: Carbon Isotopes; Magnetic Resonance Spectroscopy; Mestranol; Photochemistry; Protons; Salmonella typhimurium
PubMed: 3003971
DOI: 10.1016/0039-128x(85)90040-6 -
Quaderni Di Clinica Ostetrica E... Sep 1969
Comparative Study Review
Topics: Adrenal Glands; Blood Coagulation; Contraceptives, Oral; Endometrium; Ethinyl Estradiol; Female; Glucose Tolerance Test; Humans; Lipids; Liver; Mestranol; Nausea; Ovulation; Thyroid Gland
PubMed: 4926507
DOI: No ID Found -
American Journal of Obstetrics and... May 1970
Topics: Administration, Oral; Animals; Blood Platelets; Contraceptives, Oral; Drug Synergism; Endotoxins; Female; Mestranol; Norethynodrel; Plasminogen; Pregnancy; Pregnancy, Animal; Rats; Shwartzman Phenomenon; Thromboembolism
PubMed: 5462439
DOI: 10.1016/0002-9378(70)90587-9