Medroxyprogesterone acetate 是广泛使用的合成类固醇,与雄激素,孕酮及糖皮质激素受体均有作用。
产品描述
Medroxyprogesterone acetate is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.
体外活性
MPA和黄体酮显著减少海马中GAD水平,MPA和黄体酮明显增加内嗅皮质的GAD水平.MPA在老年卵巢切除大鼠中,损害水面上旋臂迷宫延迟记忆保留,并加剧Morris水迷宫的隔夜遗忘.
体内活性
Medroxyprogesterone acetate(MPA)减少人乳腺癌细胞中IL-6和PTHrP的分泌。MPA在KTC-2细胞中,以剂量依赖的方式减少IL-6和PTHrP的分泌和表达。MPA和地塞米松在M-1细胞中,剂量依赖性增加α-ENaC的启动子驱动的萤光素酶活性,这不受Org31710抑制,这表明MPA调节的α-ENaC与PR无关。MPA和地塞米松在M-1和Madin-Darby狗肾-C7细胞中,剂量依赖性增加α-ENaC的和SGK1的mRNA,但黄体酮无此作用。0.1 nM MPA明显增强体外特异性免疫球蛋白G抗体的产生,该作用似乎涉及孕激素与PRG受体的相互作用。MPA抑制3- hydroxyste-固醇脱氢酶,参与THP和DHP之间的可逆转换,因此,可能会影响到大脑中DHP和THP的作用。
Cas No.
71-58-9
分子式
C24H34O4
分子量
386.532
别名
Metigestrona;安宫黄体酮;Medroxyprogesterone (acetate);Farlutin;Medroxyprogesterone 17-acetate;Provera;醋酸甲羟孕酮;NSC-26386
储存和溶解度
DMSO:10 mg/mL (25.9 mM)
Ethanol:10 mg/mL (25.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years