Abstract
A novel potent and selective kynurenine-3-hydroxylase inhibitor is descibed along a preliminary evaluation in a in vivo gerbil model of its ability to increase the kynurenine and kynurenic acid concentration in both plasma and brain. These data support the notion that kynurenine-3-hydroxylase inhibitors may have a sustained therapeutic potential in those diseases characterized by unbalance in the QUIN/KYNA branches of the kynurenine pathway.
MeSH terms
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Animals
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Brain / drug effects
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Brain / metabolism
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Gerbillinae
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Humans
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In Vitro Techniques
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Kynurenine / metabolism*
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Kynurenine 3-Monooxygenase
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Mixed Function Oxygenases / antagonists & inhibitors*
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Mixed Function Oxygenases / chemistry
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Models, Molecular
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Neuroprotective Agents / chemistry
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Neuroprotective Agents / pharmacology*
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Protein Conformation
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Tryptophan / metabolism*
Substances
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Enzyme Inhibitors
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Neuroprotective Agents
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Kynurenine
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Tryptophan
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Mixed Function Oxygenases
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Kynurenine 3-Monooxygenase