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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
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pubmed:dateCreated |
1992-9-17
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pubmed:abstractText |
The concentration of AZT in mice plasma and brain was measured using HPLC after an ingestion of 20 mg/kg of AZT or the molar equivalent of hexadecyl 2-(alpha-D-mannopyranosidyl)ethyl 3'-azido-3'-deoxy-5'-thymidinyl phosphate 3. The results demonstrated the promising qualities of the prodrug 3 which gave AZT-5'-phosphate as the main metabolite: the total concentration of AZT derivatives detected in brain presented a peak of 156 nmol/g (5 nmol/g for AZT) at 1 h; the half-life was about 24 h (1 h for AZT) with an AUC of 4366 nmol h/g as compared to 4 nmol h/g for AZT. The lipophilic properties of 3 were confirmed by its in vitro transport of inside synaptosomes. The derivative 2-(alpha-D-mannopyranosidyl)ethyl 3'-azido-3'-deoxy-5'-thymidinyl phosphate (2) provided also a good delivery of AZT to the central nervous system, with values intermediate between those of AZT and 3.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
7
|
pubmed:volume |
35
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
3039-44
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1501232-Animals,
pubmed-meshheading:1501232-Brain,
pubmed-meshheading:1501232-Chromatography, High Pressure Liquid,
pubmed-meshheading:1501232-Esters,
pubmed-meshheading:1501232-Half-Life,
pubmed-meshheading:1501232-Male,
pubmed-meshheading:1501232-Mice,
pubmed-meshheading:1501232-Prodrugs,
pubmed-meshheading:1501232-Synaptosomes,
pubmed-meshheading:1501232-Zidovudine
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pubmed:year |
1992
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pubmed:articleTitle |
Improved brain delivery of AZT using a glycosyl phosphotriester prodrug.
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pubmed:affiliation |
Unité de Chimie Organique, URA CNRS 487, Institut Pasteur, Paris, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|