Glucosylated deferiprone and its brain uptake: implications for developing glucosylated hydroxypyridinone analogues intended to cross the blood-brain barrier.
This report presents that Deferiprone, the only clinically used 3-hydroxypyridin-4-one (HPO), is able to penetrate the blood-brain barrier (BBB) in guinea pigs, whereas its glucosylated analogue is unable to do so. This finding is contrary to published information suggesting that the glucosylation of HPOs is a viable means of enhancing the brain uptake of this group of compounds.
Roy
Sourav
S
Pharmaceutical Science Division, King's College London, London, UK.
Preston
Jane E
JE
Hider
Robert C
RC
Ma
Yong Min
YM
D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism*; D000077543:Deferiprone; D006031:Glycosylation; D006168:Guinea Pigs; D007502:Iron Chelating Agents / Q000493:pharmacokinetics*; D008297:Male; D011728:Pyridones / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution
D007502:Iron Chelating Agents; D011728:Pyridones; D000077543:Deferiprone