Enclomiphene citrate

Enclomiphene citrate ((E) -Clomifene, cis-Clomifene, RMI-16289, ICI-46476) is a nonsteroidal selective estrogen receptor modulator (SERM) that is under development for the treatment of male hypogonadism; inhibits the ER in the pituitary gland, reduces negative feedback by estrogen on the hypothalamic-pituitary-gonadal axis, increases gonadotropin secretion and hence gonadal production of testosterone.Sexual Dysfunction Phase 3 Clinical (In Vitro) :Enclomiphene citrate (0-100 μM, 6 h) dose-dependently inhibits basal and gonadotrophin-stimulated small and large ovine luteal cell progesterone secretion.Enclomiphene citrate (0-100 μg/mL, 24 h) dose-dependently inhibits fertilization rates, blastocyst formation rates, and degeneration rates in mouse oocytes.Enclomiphene citrate (1 nM-10 μM, 6 h) dose-dependently decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells. (In Vivo) :Enclomiphene citrate (subcutaneous injection, 0.25 and 0.5 mg/animal, daily) inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in intact or castrated rats.Enclomiphene citrate (oral adminstration, 0.03-3 mg/kg, daily for 90 days) reductes body weight to sham levels, and reduced serum cholesterol.