Ro 61-8048 is an inhibitor of kynurenine 3-hydroxylase which can potently and competitively inhibit kynurenine 3-monooxygenase with Ki value and IC50 value of 4.8 nM and 37 nM, respectively.
Kynurenine 3-hydroxylase is a component of the kynurenine pathway involved in neuronal injury. Ro 61-8048 is an inhibitor of kynurenine 3-hydroxylase with an IC50 value of 37 ± 3nM. It acts as a competitive inhibitor of kynurenine 3-hydroxylase with a Ki value of 4.8 ± 2.1nM. The ED50 values (μmol/kg, p.o.) of Ro 61-8048 for the ex vivo inhibition of kynurenine 3-hydroxylase activity in rat kidney and liver are 1.2 (0.8 – 1.3) and 4.7 (3.6 – 5.6), respectively. Ro 61-8048 also inhibited kynurenine 3-hydroxylase activity in Gerbils brain, kidney, and liver with ED50 values (μmol/kg, p.o.) of 5.5 (3.3 – 9.2), 0.8 (0.5 – 1.2), and 0.4 (0.3 – 0.5). In rat hippocampus after implantation of a transversal microdialysis probe, Ro 61-8048 at a dose of 50μmol/kg (p.o.) led to a 4-fold increase in kynurenic acid levels.[3]
作用机制
Ro 61-8048 is a competitive inhibitor of kynurenine 3-hydroxylase.[3]
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