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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox.
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New evidence for the selective, long-lasting central effects of the brain-targeted estradiol, Estredox.

机译：针对大脑的雌二醇Estredox具有选择性，长效中枢作用的新证据。

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摘要

The present study examined the dose- and time-dependent central effects of an estradiol chemical delivery system cyclodextrin complex (E(2)-CDS-CD) on the reestablishment of copulatory behavior of castrated male and ovariectomized female rats with concomitant determination of the blood luteinizing hormone (LH) and E(2) levels. In orchidectomized males, Estredox, after single doses of 0.3 and 3.0 mg/kg iv, reestablished the mounting and intromission up to 4 weeks. The LH suppressive effect lasted to Day 7 and 28, respectively. After repeated administration for 10 days at a dose of 0.01mg/kg iv, significant effect was obtained by Day 14. Ovariectomized females were treated iv daily for 5 days either with E(2)-CDS-CD, estradiol benzoate (EB) or vehicle, and the lordosis quotient was determined. At a dose of 0.03 mg/kg the duration of EB's effect was 10 days shorter and only one-third of that of E(2)-CDS-CD. The LH suppression lasted to Day 18. On the other hand, after EB treatment there was no significantdecrease in LH levels. The low plasma E(2) levels indicated fast rate of peripheral elimination in both males and females. The brain-targeting E(2) indicates better efficacy and increased safety in replacement therapies because of the reduced peripheral side effects.
机译：本研究检查了雌二醇化学递送系统环糊精复合物（E（2）-CDS-CD）对cast割的雄性和去卵巢雌性大鼠的交配行为的重建，并伴随着血液的测定的剂量和时间依赖性中心作用黄体生成素（LH）和E（2）的水平。在经睾丸切除的雄性动物中，单次静脉注射0.3和3.0 mg / kg的Estredox可以在长达4周的时间里重新建立坐骑和入雌。 LH抑制作用分别持续至第7天和第28天。静脉内以0.01mg / kg的剂量重复给药10天后，在第14天获得了明显的效果。每天用E（2）-CDS-CD，雌二醇苯甲酸酯（EB）或静脉内对去卵巢的女性进行静脉内治疗5天。车辆，并确定脊柱前凸商。在0.03 mg / kg的剂量下，EB的作用持续时间缩短了10天，仅是E（2）-CDS-CD的三分之一。 LH抑制持续至第18天。另一方面，EB治疗后LH水平没有明显下降。低血浆E（2）水平表明男性和女性的外周血清除速度都很快。以大脑为目标的E（2）可以降低周边副作用，因此在替代疗法中具有更好的疗效和更高的安全性。

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