Drospirenone

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Chemical Structure| 67392-87-4 同义名 : 屈螺酮 ，二氢螺利酮 ;Dihydrospirorenone;ZK 30595;Dehydrospirorenone;Drospirenonum;Drospirenona;67392-87-4;1,2-dihydro Spirorenone;ZK 3059
CAS号 : 67392-87-4
货号 : A689592
分子式 : C24H30O3
纯度 : 99+%
分子量 : 366.493
MDL号 : MFCD00867350
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Progesterone receptor
描述 Drospirenone is a novel progestin under clinical development that is similar to the natural hormone progesterone, combining potent progestogenic with antimineralocorticoid and antiandrogenic activities. Drospirenone displayed high affinity to PR (progesterone receptor) and MR (mineralocorticoid receptor) and low binding to AR (androgen receptor), similar to progesterone. Drospirenone showed considerable antimineralocorticoid activity and weak mineralocorticoid activity[3]. Drospirenone acts on the renin-angiotensin-aldosterone system (RAAS), which prevents excessive sodium loss and regulates blood pressure. The antialdosterone properties exhibited by drospirenone promote sodium excretion and prevent water retention, conferring potential blood pressure benefits[4]. The lowest effective dose of drospirenone for reduction in BP (blood pressure) is 2mg, a dose that is also protective of the uterus in women treated with estrogen therapy. In addition to effectively relieving menopausal symptoms and lowering BP, drospirenone reduces bodyweight and lipoprotein concentrations[5]. The combination of 17beta-estradiol with drospirenone offers a safe and effective medication for decreasing bone turnover and preventing postmenopausal bone loss in postmenopausal women[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00185328 Postmenopause Phase 4 Completed - -
NCT00442689 Polycystic Ovary Syndrome ... 展开 >> Metabolic Syndrome 收起 << Not Applicable Completed - United States, Illinois ... 展开 >> Northwestern Memorial Hospital Chicago, Illinois, United States, 60611 收起 <<
NCT00442689 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.64mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]Fuhrmann U, Krattenmacher R, et al. The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception. 1996 Oct;54(4):243-51.

[2]Muhn P, Krattenmacher R, et al. Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Pharmacological characterization in animal models. Contraception. 1995 Feb;51(2):99-110.

[3]Fuhrmann U, Krattenmacher R, Slater EP, Fritzemeier KH. The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception. 1996 Oct;54(4):243-51

[4]Genazzani AR, Mannella P, Simoncini T. Drospirenone and its antialdosterone properties. Climacteric. 2007 Feb;10 Suppl 1:11-8

[5]Mallareddy M, Hanes V, White WB. Drospirenone, a new progestogen, for postmenopausal women with hypertension. Drugs Aging. 2007;24(6):453-66

[6]Christiansen C. Effects of drospirenone/estrogen combinations on bone metabolism. Climacteric. 2005 Oct;8 Suppl 3:35-41