Clomiphene

Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) is an orally active ovulation-inducing agent. Clomiphene binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene ameliorates memory impairment in PCOS models. Clomiphene mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer^[1][2][3][4]. In Vitro:Clomiphene (citrate) (1.0-5.0 μg/mL; 18 h) significantly increases hyperploidy and diploidy in cultured mouse germinal vesicle-stage oocytes, while reducing the proportion of metaphase I oocytes, indicating accelerated oocyte maturation^[1].
Clomiphene (citrate) (10-50 μM) increases cytosolic free calcium levels in PC3 human prostate cancer cells with an EC₅₀ of approximately 30 μM^[4].
Clomiphene (citrate) (50 μM; 2-30 min) induces time-dependent mild cytotoxicity in PC3 human prostate cancer cells, reducing viability by 10-50% over 2-15 minutes of incubation with no further decrease after 15 minutes^[4]. In Vivo:Clomiphene (citrate) (25-100 mg/kg; i.p.; 3 doses over 4 hours) induces a significant 1.5% hyperploidy rate in mouse oocytes in vivo at the highest dose, while lower doses increase premature centromere separation and single unpaired chromatids, and all tested doses reduce ovulated oocyte counts^[1].
Clomiphene (citrate) (1 mg/kg; p.o.; daily; 15 days) improves spatial and non-spatial memory impairment, restores reproductive hormone levels, increases serum antioxidant enzyme concentrations, and downregulates prefrontal cortex AchE gene expression in Letrozole (HY-14248)-induced PCOS rats, but does not reduce anxiety-like behavior^[2].
Clomiphene decreases serum gonadotropin levels and reduces testosterone secretion in rats^[4].