Ro 61-8048

Biological Activity

Ro 61-8048 is a potent and competitive kynurenine 3-monooxygenase (kynurenine 3-hydroxylase; KMO) inhibitor (K_i = 4.8 nM, IC₅₀ = 37 nM). Increases kynurenic acid levels to concentrations that antagonize the glycine site of NMDA receptors. Brain penetrant and exhibits antidystonic, anticonvulsant and neuroprotective activities. Ro 61-8048 decreases nicotine self-administration in vivo. Ro 61-8048 prevents post-operative brain edema and consequent neuronal apoptosis in a rat model of surgically induced brain injury.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Apicomplexan parasite, Eimeria falciformis, co-opts host tryptophan catabolism for life cycle progression in mouse.
   Schmid M, Lehmann MJ, Lucius R, Gupta N
   J. Biol. Chem., 2012;287(24):20197-207.
2. Kynurenine 3-monooxygenase mediates inhibition of Th17 differentiation via catabolism of endogenous aryl hydrocarbon receptor ligands.
   Stephens G, Wang Q, Swerdlow B, Bhat G, Kolbeck R, Fung M
   Eur J Immunol, 2013;43(7):1727-34.
3. Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid.
   Justinova et al.
   Nat.Neurosci., 2013;16:1652
4. Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high affinity inhibitors of kynurenine 3-hydroxylase.
   Rover et al.
   J.Med.Chem., 1997;40:4378
5. Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischaemic neuronal death in organotypic hippocampal slice cultures.
   Carpenedo et al.
   J.Neurochem., 2002;82:1465
6. Effects of kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt^sz mutant.
   Hamann et al.
   Eur.J.Pharmacol., 2008;586:156

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