ArticlePharmaceutica analytica acta2012
"All in the mind"? Brain-targeting chemical delivery system of 17β-estradiol (Estredox) produces significant uterotrophic side effect.
Article in Pharmaceutica analytica acta, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
10 citing papers in PubMed, 14 citations in OpenAlex.
- Redox Heterocyclic Platforms Engineered for Brain Drug Delivery and Beyond.Chemical record (New York, N.Y.) · 2026Review
- The impact of 17β-estradiol on the estrogen-deficient female brain: from mechanisms to therapy with hot flushes as target symptoms.Frontiers in endocrinology · 2023Review
- A Novel Prodrug Approach for Central Nervous System-Selective Estrogen Therapy.Molecules (Basel, Switzerland) · 2019Review
- Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach.Pharmaceutics · 2019Article
- 10β,17α-Dihydroxyestra-1,4-dien-3-one: A Bioprecursor Prodrug Preferentially Producing 17α-Estradiol in the Brain for Targeted Neurotherapy.ACS chemical neuroscience · 2018Article
- Current Challenges and Opportunities in Treating Glioblastoma.Pharmacological reviews · 2018Article
- Non-Feminizing Estrogens Do Not Exhibit Antidepressant-like Activity.Journal of pharmaceutics and drug research · 2016Article
- The prodrug DHED selectively delivers 17β-estradiol to the brain for treating estrogen-responsive disorders.Science translational medicine · 2015Article
- 17β-estradiol eye drops protect the retinal ganglion cell layer and preserve visual function in an in vivo model of glaucoma.Molecular pharmaceutics · 2013Article
- Design and exploratory neuropharmacological evaluation of novel thyrotropin-releasing hormone analogs and their brain-targeting bioprecursor prodrugs.Pharmaceutics · 2013Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
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
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.