Mifepristone Chemical Properties
- Melting point:
- D20 +138.5° (c = 0.5 in chloroform)
- Boiling point:
- 544.13°C (rough estimate)
- 1.0731 (rough estimate)
- refractive index
- 1.6290 (estimate)
- storage temp.
- Yellow solid
- Water Solubility
- 474.8ug/L(22.5 ºC)
- CAS DataBase Reference
- 84371-65-3(CAS DataBase Reference)
Mifepristone Usage And Synthesis
Mifepristone is a kind of antagonist of the progestational and glucocorticoid hormone. It is mainly used for the treatment of hypercortisolism in patients with nonpituitary cushing syndrome. During the treatment of Cushing’s syndrome, mifepristone takes effect through interfering with the binding of cortisol to its receptor. It reduces the effects of excess cortisol (e.g., high blood sugar levels) without causing decreased cortisol production. It can also be used to end a pregnancy. Its inhibition on progesterone can induce bleeding during the luteal phase and in early pregnancy.
Mifepristone is an orally-active progesterone and glucocorticoid receptor antagonist indicated for use as a post-coital contraceptive. In addition to being an abortifacient, mifepristone is reported to be effective in the treatment of ocular hypertension; its potential therapeutic effect in hormone-dependent tumors is currently under investigation.
Pale Yellow Solid
glutamate uptake inhibitor, AMPA blocker
A progesterone and glucocorticoid antagonist, suppresses VEGF production.
A progesterone receptor antagonist with partial agonist activity. Abortifacient.
Mifepristone is a progesterone receptor antagonist that has a high affinity for glucocorticoid receptors and little agonist effect.This drug has recently been approved for use in the United States for the treatment of hypercortisolism. At high doses, mifepristone blocks negative feedback of the hypothalamic–pituitary axis, thereby increasing endogenous corticotrophin and cortisol levels. Because mifepristone exerts its effects at the receptor level and not by altering glucocorticoid production, elevated serum cortisol and corticotrophin levels may not accurately reflect the effectiveness of the therapeutic regimen. Mifepristone does not inhibit cortisol binding to the mineralocorticoid receptor, so that the resulting corticotrophin disinhibition may cause potassium depletion. Thus, administration of a mineralocorticoid receptor antagonist such as spironolactone may be indicated with mifepristone. Hypoadrenalism, nausea, and drowsiness have been reported during prolonged administration of mifepristone.
World Health Organization (WHO)
Mifepristone, an antiprogesterone used in combination with a prostaglandin for the termination of early pregnancy, was introduced in 1990. Use of the combination has been associated with episodes of coronary spasm that are attributed to administration of the prostaglandin and which have resulted in several cases of cardiac infarction and ventricular fibrillation. At least one of these incidents has been fatal.
Selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors in vitro and in vivo . Is a silent antagonist at PR and has a higher affinity than progesterone. Has higher affinity for GR than dexamethasone.
- mifepristone methochloride
- N-DESMETHYL MIFEPRISTONE,N-Demethyl Mifepristone
- Didemethyl Mifepristone,DIDESMETHYL MIFEPRISTONE,N-Didesmethyl Mifepristone
- 22-Hydroxy Mifepristone-d6
- Estr-9-en-3-one, 11-[4-(dimethylamino)phenyl]-5,17-dihydroxy-17-(1-propynyl)-, cyclic 1,2-ethanediyl acetal, (5a,11b,17b)-
- RU486 (Mifepristone)
- MIFEPRISTONE, [N-METHYL-3H]
- RU-486 (MIFEPRISTONE), [N-METHYL-3H]
- HYDROXY MIFEPRISTONE,22-Hydroxy Mifepristone
- CHLOROPHOSPHONAZO III
- 010-82848833- ;010-82848833-