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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Hormone-like behavioral effects of levonorgestrel and its metabolites in the male rat.
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Hormone-like behavioral effects of levonorgestrel and its metabolites in the male rat.

机译：左炔诺孕酮及其代谢物在雄性大鼠中的激素样行为作用。

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Levonorgestrel (LNG), a contraceptive progestin, exhibits, besides its progestational activity, other hormone-like effects at the peripheral level. To assess whether LNG and its metabolites exert androgenic and/or estrogenic actions at the central nervous system (CNS), their effects on male sexual behavior in castrated rats were examined. LNG, 5alpha-dihydro LNG (5alphaLNG), and the 3alpha,5alpha- and 3beta,5alpha-tetrahydro derivatives of LNG (3alphaLNG and 3betaLNG, respectively) were administered for 3 weeks either alone (1000 microg/day) or in combination (300 microg/day) with 5alpha-dihydrotestosterone (DHT, 300 microg/day) or with estradiol-17beta (E(2), 5 microg/day). Copulatory behavior was assessed twice per week and sex accessory organs weights recorded at the end of treatments. LNG restored full copulatory behavior comparable to that of testosterone treated animals, although with a slight delay, whereas 5alphaLNG induced male sexual behavior in a significantly lower number of subjects. 3betaLNG and 3alphaLNG induced mounting but failed to restore intromission and ejaculation. Combined LNG+E(2) treatment fully activated mounting and intromission, but ejaculation was only partially restored. Combined 5alphaLNG+E(2) treatment and the combinations of 3alphaLNG or 3betaLNG with E(2) were significantly less effective, activating fewer intromissions and ejaculations. 3alphaLNG and 5alphaLNG, in combination with DHT, restored male sexual behavior. LNG, but not its metabolites, induced a significant increase on the weight of sex accessory organs. The overall results demonstrated that high doses of LNG induce a potent androgen agonistic behavioral effect and that its A-ring reduction diminishes this potency and enables a shift towards a weak estrogen-like effect.
机译：左炔诺孕酮（LNG）是一种避孕性孕激素，除具有孕激素作用外，在外周水平还具有其他激素样作用。为了评估LNG及其代谢产物是否对中枢神经系统（CNS）产生了雄激素和/或雌激素作用，研究了它们对cast割大鼠雄性行为的影响。 LNG，5alpha-dihydro LNG（5alphaLNG）以及LNG的3alpha，5alpha-和3beta，5alpha-四氢衍生物（分别为3alphaLNG和3betaLNG）单独给药（1000微克/天）或联合给药3周（300微克/天）与5α-二氢睾丸激素（DHT，300微克/天）或与雌二醇17beta（E（2），5微克/天）。每周两次评估交配行为，并在治疗结束时记录性附属器官的重量。 LNG恢复了与睾丸激素治疗的动物相当的完全交配行为，尽管稍有延迟，而5alphaLNG则在明显更少的受试者中诱导了男性性行为。 3betaLNG和3alphaLNG诱导了坐骑，但未能恢复内吸和射精。液化天然气+ E（2）联合治疗完全激活安装和介绍，但射精只是部分恢复。组合的5alphaLNG + E（2）处理以及3alphaLNG或3betaLNG与E（2）的组合效果显着降低，激活了较少的内分泌和射精。 3alphaLNG和5alphaLNG与DHT结合可恢复男性的性行为。 LNG（但不是其代谢物）引起性附属器官的重量显着增加。总体结果表明，高剂量的LNG会诱导强效的雄激素激动作用，而降低A环的作用会减弱这种作用力，并使之转变为类似雌激素的弱效作用。

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