Mifepristone

Description

Simple description:
Product Name: Mifepristone
CAS: 84371-65-3
Melting point 195-198 ° C
Specific rotation D20+138.5 ° (c=0.5 in chloroform)
Boiling point 544.13 ° C (rough estimate)
Density 1.0731 (rough estimate)
Refractive index 1.6290 (estimate)
Storage conditions 2-8 ° C
Solubility in DMSO (up to 40 mg/ml) or Ethanol (up to 20 mg/ml)
Yellow solid

The pharmacological action of mifepristone, also known as antiprogesterone, cypermethrin, Xiyin, Hanzhuting, Smian, and Minasterone, is an antiprogesterone drug. It was first developed by Roussel Ulsf in France in the early 1980s as a new type of anti fertility drug acting at the receptor level. It has no Progestogen, androgen, and estrogen activities. It was first listed in France in 1988. It mainly acts on endometrial Progesterone receptor, can bind with Progesterone receptor and Glucocorticoid receptor, and has high affinity. Its affinity for endometrial Progesterone receptor is 5 times stronger than progesterone. It has no obvious effect on the level of cortisol chemobook at Effective dose, and can produce strong anti progesterone effect, denature decidua and chorionic tissue of pregnancy, release endogenous Prostaglandin, and cause Uterine contraction, At the same time, it can reduce the production of Human chorionic gonadotropin and dissolve the corpus luteum, thus causing embryo abortion. Because the drug can not induce enough uterine activity, it has a high rate of incomplete abortion when used solely for anti early pregnancy, but can increase the sensitivity of the uterus to Prostaglandin, so the addition of small doses of Prostaglandin can not only reduce the adverse reactions of Prostaglandin, but also significantly increase the rate of complete abortion. In addition, mifepristone also has the effect of softening and expanding the cervix.

Biological activity and mechanism Mifepristone has strong anti progesterone activity. Animal experiments show that the binding force of Mifepristone to Progesterone receptor is 3-5 times higher than that of progesterone. Mifepristone mainly acts on the endometrium, competing with endogenous progesterone at the molecular level to bind receptors, producing strong anti progesterone effect, and producing the following physiological activities: 1. Competitively occupying the Progesterone receptor in decidua, causing withdrawal of progesterone effect, degeneration and death of decidual tissue, secondary damage and stripping of villi, causing the decline of HCGChemicalbook level and luteolysis. The mechanism is that mifepristone can directly act on syncytiotrophoblast, causing a dose-dependent decline in the rate of HCG, HPL and P production. 2. Promote the release of endogenous Prostaglandin, resulting in Uterine contraction. 3. At the same time, it also acts on the anterior pituitary lobe of the hypothalamus, promoting a decrease in FSH and LH, luteal lysis, and ultimately leading to pregnancy failure and miscarriage that relies on the maintenance of the corpus luteum. 4. Acting on the cervix, it softens and expands, facilitating the expulsion of the embryo sac and decidua.

Usage: Anti early pregnancy in 7 weeks

 

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