|别名||4-雄烯-4-醇-3,17-二酮 ;福美司坦,4-羟基雄甾烷-4-烯-3,17-二酮;4-Hydroxy-4-androstene-3,17-dione Formestane|
|个人防护设备||Eyeshields,full-face particle respirator type N100 (US),Gloves,respirator cartridge type N100 (US),type P1 (EN143) respirator filter,type P3 (EN 143) respirator cartridges|
Formestane (Lentaron(R), 4-hydroxyandrostenedione) is a steroidal aromatase inhibitor used for treatment of advanced breast cancer. Clinically, it is administered as a depot form once fortnightly by i...Read More
Estrogens are known to be important in the growth of breast cancers in both pre- and postmenopausal women. The number of breast cancer patients with hormone-dependent disease increases with age, as do...Read More
Steroid hormones are essential for maintenance of pregnancy and fetal development. The expression and catalytic activity of the key steroidogenic enzymes involved in the production of progesterone and...Read More
Estrogen-dependent inhibition of dextrose-induced endoplasmic reticulum stress and superoxide generation in endothelial cells.
Increased oxidative stress and endoplasmic reticulum stress (ER stress) have been implicated in atherosclerosis. Estrogens have potent antioxidant activity but their effects on ER stress have not been...Read More
Aromatase is a key enzyme responsible for in vivo estrogen biosynthesis. Inhibition of the activity of the aromatase has become an alterative way for treatment of breast cancer. In this review, the st...Read More
The aromatase inhibitor formestane (4-hydroxy-androst-4-ene-3,17-dione, F) is prohibited in sports by the World Anti-Doping Agency (WADA). F possesses only weak androgenic properties and is presumed t...Read More
Early transcripts related to male development in chicken embryos and their expression profiles were examined. A total of 89 and 127 candidate male development transcripts that represented 83 known and...Read More
Combined inhibitory effect of formestane and herceptin on a subpopulation of CD44+/CD24low breast cancer cells.
In breast cancer, stromal cells surrounding cancer epithelial cells can influence phenotype by producing paracrine factors. Among many mediators of epithelial-stromal interactions, aromatase activity ...Read More
Cytochrome P450 (P450) enzymes regulate a variety of endogenous signaling molecules and play central roles in the metabolism of xenobiotics and drugs. We recently showed that an aryl alkyne serves as ...Read More
Testosterone reduces cumulative burying in female Wistar rats with minimal participation of estradiol.
Testosterone exerts anxiolytic effects, but the participation of its aromatase metabolic product estradiol is controversial. Therefore, we used the defensive burying paradigm in female Wistar rats to ...Read More
The detection of androstenedione abuse in sport: a mass spectrometry strategy to identify the 4-hydroxyandrostenedione metabolite.
Studies have shown that the administration of androstenedione (ADIONE) significantly increases the urinary ratio of testosterone glucuronide to epitestosterone glucuronide (T/E) - measured by gas chro...Read More
Resting intracellular calcium concentration, depolarizing Gamma-Aminobutyric Acid and possible role of local estradiol synthesis in the developing male and female hippocampus.
The maturation of the hippocampus is impacted by a multitude of factors, including the regulation of intracellular calcium levels. Depolarizing actions of Gamma-Aminobutyric Acid (GABA) can profoundly...Read More
Synthesis of 4-amino-4,6-androstadiene-3,17-dione 7, an analog of formestane used in breast cancer therapy as an aromatase inhibitor, from 4-acetoxy-4-androstene-3,17-dione 2 is described. This is the...Read More
The role of estrogen in the developmental appearance of sensory-motor behaviors in the zebrafish (Danio rerio): the characterization of the "listless" model.
The brain is a steroidogenic organ and is thus dependent on estrogen for many aspects of its development and maintenance in both males and females. The purpose of this study was to develop a model to ...Read More
Acute and chronic effects of testosterone and 4-hydroxyandrostenedione to the crustacean Daphnia magna.
Steroid compounds have been globally detected in surface waters. The ecological impacts of these biologically active chemicals are largely unknown. Toxicity of testosterone and 4-hydroxyandrostenedion...Read More
In vitro expansion of human breast cancer epithelial and mesenchymal stromal cells: optimization of a coculture model for personalized therapy approaches.
Molecularly targeted, customized therapies are designed based on the molecular portraits of cancer tissue. The efficacy of targeted therapy in individual patients depends on the contribution of single...Read More
The effects of aromatase inhibitors and selective estrogen receptor modulators on eye development in the zebrafish (Danio rerio).
It has been shown that the steroid hormone estrogen plays an important role in the development of the central nervous system. The purpose of these studies was to determine the effect of estrogen on ze...Read More
In male rats, the antidepressant-like effect of fluoxetine (FLX) and desipramine (DMI) in the forced swimming test (FST) is reduced by orchidectomy and partially restored by testosterone (T). It is un...Read More
Coadministration of the aromatase inhibitor formestane and an isopropanolic extract of black cohosh in a rat model of chemically induced mammary carcinoma.
Non-steroidal as well as steroidal aromatase inhibitors are currently being discussed as alternatives to tamoxifen in the first-line treatment of patients with hormone-dependent breast cancer. Many of...Read More
Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites
4-Hydroxyandrost-4-ene-3,17-dione is a second generation, irreversible aromatase inhibitor and commonly used as anti breast cancer medication for postmenopausal women. 4-Hydroxytestosterone is adverti...Read More
Aromatase destabilizer: novel action of exemestane, a food and drug administration-approved aromatase inhibitor.
Using Western blot as the major technique, we studied the effects of the three Food and Drug Administration (FDA)-approved aromatase inhibitors (AI) on aromatase protein stability in the aromatase-ove...Read More
Ghrelin, an endogenous ligand for the GH secretagogue receptor, is predominantly produced in the stomach. Little is known about the regulation mechanism of gastric ghrelin. Here, we report that estrog...Read More
Cyclooxygenase-2 directly regulates gene expression of P450 Cyp19 aromatase promoter regions pII, pI.3 and pI.7 and estradiol production in human breast tumor cells
The present studies evaluated the direct effects of the presence of human cyclooxygenase-2 (Cox-2) on gene expression of specific promoter regions of the P450 Cyp19 enzyme aromatase enzyme and its pro...Read More
Survival with aromatase inhibitors and inactivators versus standard hormonal therapy in advanced breast cancer: meta-analysis.
Aromatase inhibitors and inactivators have been extensively tested in patients with advanced breast cancer, but it is unclear whether they offer any survival benefits compared with standard hormonal t...Read More
Estrogen has been shown to have an important role in skeletal maturation in both males and females. The use of aromatase inhibitors may provide a means to delay skeletal maturation and increase final ...Read More
Effect of 4-hydroxyandrost-4-ene-3,17-dione (formestane) on the bile secretion and metabolism of 4-(14)C-cholesterol to bile acids.
4-Hydroxyandrost-4-ene-3,17-dione (formestane) is a selective aromatase inhibitor. It is indicated for postmenopausal patients with advanced breast cancer. The aim of the present study was to investig...Read More