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UPF-648 is an inhibitor of kynurenine 3-monooxygenase (IC50 = 40 nM).1 It increases kynurenine and kynurenic acid and decreases 3-hydroxykynurenine brain levels in newborn rats for up to 12 hours when administered at a dose of 30 mg/kg.2 UPF-648 (30 µM) is protective against rhabdomere neurodegeneration in the eye in a Drosophila model of Huntington's disease.3 It also decreases hypersensitivity to mechanical and thermal stimuli in a rat model of neuropathic pain induced by chronic constriction injury to the sciatic nerve.4
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1. Modulation of the kynurine pathway of tryptophan metabolism in search for neuroprotective agents. Focus on kynurenine-
2. Perinatal kynurenine 3-
3. The kynurenine pathway modulates neurodegeneration in a Drosophila model of Huntington’s disease. Curr. Biol. 21(11), 9611-9966 (2011).
4. Pharmacological inhibition of indoleamine 2,3-