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5α-雄甾烷-3β,17β-二醇可与雄激素和雌激素受体结合,但不会引发雌性大鼠的交配行为。

5 alpha-androstane-3 beta, 17 beta-diol binds to androgen and estrogen receptors without activating copulatory behavior in female rats.

作者信息

Doering C H, Gladue B A

出版信息

Pharmacol Biochem Behav. 1982 May;16(5):837-40. doi: 10.1016/0091-3057(82)90244-1.

Abstract

The ability of the androgen metabolite 5 alpha-androstane-3 beta, 17 beta-diol (3 beta-A-diol) to facilitate copulatory behavior was assessed directly in adult ovariectomized rats. Neither the highest dosage of 5 mg/day for three days, nor 2 mg/day for 15 days could induce lordosis behavior in females that displayed typically high lordosis quotients with low dosages of estradiol (E). Furthermore, prolonged administration of 5 alpha-dihydrotestosterone (DHT) induced a low but significant level of male-typical mounting behavior in females, whereas 3 beta-a-diol administered for 20 days (2 mg/day) had no effect on mounting behavior. However, this reduced androgen metabolite did compete moderately well for DHT and E binding sites on androgen and estrogen receptors respectively in hypothalamic cytosol preparations. We conclude that in spite of its ability to bind to these receptors in the brain 3 beta-A-diol, a major metabolite of DHT, is totally inert with respect to sexual behavior.

摘要

直接在成年去卵巢大鼠中评估雄激素代谢物5α-雄烷-3β,17β-二醇(3β-A-二醇)促进交配行为的能力。无论是连续三天每天5毫克的最高剂量,还是连续15天每天2毫克的剂量,都无法在给予低剂量雌二醇(E)时通常表现出高脊柱前凸商数的雌性大鼠中诱导出脊柱前凸行为。此外,长期给予5α-双氢睾酮(DHT)可诱导雌性大鼠出现低水平但显著的雄性典型爬跨行为,而连续20天(每天2毫克)给予3β-A-二醇对爬跨行为没有影响。然而,这种减少的雄激素代谢物分别在下丘脑胞质溶胶制剂中与雄激素和雌激素受体上的DHT和E结合位点竞争的能力适中。我们得出结论,尽管DHT的主要代谢物3β-A-二醇能够与大脑中的这些受体结合,但在性行为方面它完全没有活性。

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