Chlormadinone acetate

Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders^[1][2][3]. In Vitro:Chlormadinone acetate binds to the human progesterone receptor in MCF-7 cell cytosol with a K_i value of 2.5 nM^[1].
Chlormadinone acetate binds to the human androgen receptor in LNCaP cell cytosol with a K_i value of 3.8 nM^[1].
Chlormadinone acetate binds to the human glucocorticoid receptor in IM-9 cell cytosol with a K_i value of 16 nM^[1]. In Vivo:Chlormadinone acetate (5-45 μg/kg; p.o.; daily; for 5 consecutive days) exhibits dose-dependent progestomimetic activity in β-estradiol-pretreated rabbits. At an oral dose of 45 μg/kg, it significantly increases uterine weight and induces near-maximal endometrial transformation^[1].
Chlormadinone acetate (4.64-21.5 mg/kg; p.o.; once daily; for 7 consecutive days) exhibits dose-dependent antiandrogenic activity in testosterone-treated castrated rats^[1].
Chlormadinone acetate (21.5-100 mg/kg; p.o.; once daily; for 6 consecutive days) exhibits dose-dependent glucocorticoid activity in immature rats^[1].