エストラジオールシピオナート

外観

白色～ほとんど白色粉末～結晶

効能

月経障害治療薬, エストロゲン受容体作動薬

化学的特性

Estradiol cypionate is a White to Off-White Solid. It is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of estradiol cypionate in ethanol is approximately 20 mg/ml and approximately 15 mg/ml in DMSO and DMF.

使用

Estradiol Cypionate is the cypionate salt form of estradiol, the most potent, naturally produced estrogen. Estradiol Cypionate is present in injectable contraceptive formulations. Used in hormone replacement therapy with potential for improving cognition in post-menopausal women.

定義

ChEBI: Estradiol 17beta-cyclopentylpropionate is a steroid ester. It inhibits ET-1 synthesis via estrogen receptor.

副作用

The side effects of estradiol cypionate are the same as those of estradiol. The side effects of Estradiol Cypionate include breast tenderness and enlargement, nausea, vomiting, bloating, edema, headache, migraine, and melasma. High-dose estrogen therapy with estradiol cypionate injections may also cause an increased risk of thromboembolism, changes in blood lipid profile, increased insulin resistance, and increased levels of prolactin.

安全性プロファイル

An experimental teratogen. Other experimental reproductive effects. A steroid. When heated to decomposition it emits acrid smoke and fumes.

Mode of action

Estradiol cypionate diffuses through the cell membrane and binds to and subsequently activates the nuclear estrogen receptor found in the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated complex binds to the estrogen response element on the DNA and activates the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics.