الوصف
Eplerenone CAS 107724-20-9 Quick Details
| الاسم الكيميائي: | Eplerenone |
| اسم آخر: | (7α,11α,17α)-9,11-Epoxy-17-hydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylicacidγ-lactoneMethylester; Eplerenone cas 107724-20-9 |
| CAS: | 107724-20-9 |
| EINECS: | 600-850-8 |
| النوع: | Pharmaceuticals, pesticides, dye intermediates; Pharmaceutical raw materials |
| الصيغة الجزيئية: | C24H30O6 |
| الوزن الجزيئي: | 414.49 |
Eplerenone CAS 107724-20-9 Chemical Properties
| نقطة الانصهار | 241-243°C |
| ألفا | D +5° (c = 0.437 in chloroform) |
| نقطة الغليان | 597.9±50.0 °C(Predicted) |
| الكثافة | 1.31±0.1 g/cm3(Predicted) |
| درجة حرارة التخزين. | Store at RT |
| قابلية الذوبان | DMSO: soluble2mg/mL, clear (warmed) |
| النموذج | المسحوق |
| اللون | white to beige |
What is Eplerenone?
Eplerenone is utilized alone or in mix with various other drugs to treat hypertension. Eplerenone comes from a course of medicines called mineralocorticoid receptor villains. It works by blocking the activity of aldosterone, an all-natural compound in the body that can elevate blood pressure.
Eplerenone, an aldosterone receptor villain similar to spironolactone, has been revealed to create continual boosts in plasma renin and product aldosterone, which is consistent with the unfavorable governing comments of hindering aldosterone on renin secretion. The resulting rise in plasma renin activity and also aldosterone distributing degrees did not conquer the effects of eplerenone. Compared to its binding to recombinant human glucocorticoid, progesterone and also androgen receptors, eplerenone uniquely binds to recombinant human mineralocorticoid receptors.
Eplerenone is a new type of careful aldosterone receptor antagonist. It was approved by the State Fda for professional application in 2002. The pure product is white or white like crystal, and its aldosterone antagonistic effect is more powerful than spironolactone, and its fondness for androgen and progesterone receptors is very low. The adverse responses are little. It has a certain result on the therapy of hypertension, cardiac arrest and myocardial infarction, with less negative reactions and excellent resistance, It is a good substitute for spironolactone. For serious hypertension that can not be controlled by multiple antihypertensive drugs, the enhancement of eplerenone can dramatically lower blood pressure, particularly systolic high blood pressure. With angiotensin converting enzyme prevention (ACEI) and β The mix of receptor blockers can enhance the lifestyle as well as decrease the death of individuals with serious cardiac arrest as well as coronary infarction.
Eplerenone Uses
- Eplerenone selectively acts on aldosterone receptors and is highly selective for mineralocorticoid receptors, but has less effect on androgen and progesterone receptors, and its affinity for mineralocorticoids is 15-20% of that of spironolactone. It has a 500-fold smaller affinity for androgen and progesterone receptors than spironolactone, so there are fewer sex hormone-related adverse reactions.
- Eplerenone can reduce hypertension C, because aldosterone may play an important role in the pathophysiological process of obesity hypertension, so eplerenone also has a good antihypertensive effect on diet-induced obesity-related hypertension; In addition, eplerenone can significantly reduce glomerular ultrafiltration, thereby reducing proteinuria in hypertensive patients, and this renoprotective effect is more pronounced in hypertensive patients with diabetes.
- Eplerenone is not an inhibitor of CYP1A2, CYP3A4, CYP2C19, CYP2C9, or CYP2D6, and does not inhibit diclofenac, methylphenidate, losartan, amiodarone, dexamethasone, phenytoin, phenacetin, Dextromethorphan, metoprolol, tolbutamide, amlodipine, astemizole, cisapride, diazepam, 17-ethinyl estradiol, fluoxetine, lovastatin, methylprednisone Metabolism of drugs such as dragon, midazolam, nifedipine, glyburide and warfarin.
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