The Inhibitory Effect of Synthetic Steroids on Proestrous Gonadotropin Release in theRat
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Synthetic steroids norethisterone, d-norgestrel, 3-keto-desogestrel, and gestrinone completely blocked proestrous gonadotropin surges in rats, demonstrating antigonadotropic activity.
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Abstract
This study was performed to evaluate the inhibitory effect of synthetic steroids on the hypothalamo-pituitary axis. Six synthetic steroids, used for contraception or other gynecologic indications, were injected to female rats on diestrus 2 (2 mg/kg, sc), and the animals were sacrificed in the afternoon of proestrus. Serum levels of LH, FSH and progesterone, the pituitary contents of LH and FSH, and LH-RH in the median eminence were measured by radioimmunoassays. Among the synthetic steroids tested in this study, norethisterone, d-norgestrel, 3-keto-desogestrel and gestrinone completely blocked the gonadotropin surge on proestrus, showing stronger antigonadotropic activity than progesterone. Desogestrel did not affect proestrous gonadotropin release at this dose. The suppressive effect of danazol could be seen only in a larger dose (20 mg/kg). These findings reconfirmed previously reported results, which demonstrated that the hypothalamo-pituitary complex was a major site of action of these steroids.
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