去卵巢大鼠
药理学
前药
副作用(计算机科学)
医学
子宫
抗抑郁药
激素
雌激素
催产素
药物输送
化学
内科学
海马体
计算机科学
有机化学
程序设计语言
作者
Katalin Prókai-Tátrai,Szabolcs Szarka,Vien Nguyen,Fatima Sahyouni,Cary Walker,Shastazia White,Tatjana Talamantes,László Prókai
出处
期刊:Pharmaceutica Analytica Acta
[OMICS Publishing Group]
日期:2011-01-01
被引量:11
标识
DOI:10.4172/2153-2435.s7-002
摘要
Here we revisit the peculiarly named redox chemical delivery system concept. This unique prodrug approach has long been claimed to be capable of targeting 17β-estradiol (E2), which has numerous beneficial central effects, into the brain without detrimental peripheral hormonal exposure. Using a well-established protocol to monitor E2's antidepressant-like effect, we show that the administration of this chemical delivery system incorporated into hydroxypropyl-β-cyclodextrin (i.e., Estredox), indeed, triggers a transient antidepressant-like behavior in ovariectomized mice. At the same time, even an acute dose of the carefully purified chemical delivery system produces significant circulating E2 levels and uterotrophic side effects for several days after drug administration. For the first time, we also unequivocally show by liquid chromatography coupled with tandem mass spectrometry that the uterus of the Estredox-treated animals contains a large quantity of E2 compared to that of the control group. These thus far unexposed yet consequential peripheral side effects brought about by Estredox call for a thorough and unbiased reassessment of the extent of brain-targeting of the hormone via the chemical delivery system approach.
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