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Biological Activity for Ro 61-8048
Ro 61-8048 is a potent and competitive kynurenine 3-monooxygenase (kynurenine 3-hydroxylase; KMO) inhibitor (Ki = 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.
Compound Libraries for Ro 61-8048
Technical Data for Ro 61-8048
|Storage||Store at +4°C|
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.
Solubility Data for Ro 61-8048
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Ro 61-8048
The following data is based on the product molecular weight 421.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.37 mL||11.86 mL||23.73 mL|
|5 mM||0.47 mL||2.37 mL||4.75 mL|
|10 mM||0.24 mL||1.19 mL||2.37 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References for Ro 61-8048
References are publications that support the biological activity of the product.
Rover et al (1997) Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high affinity inhibitors of kynurenine 3-hydroxylase. J.Med.Chem. 40 4378 PMID: 9435907
Carpenedo et al (2002) Kynurenine 3-mono-oxygenase inhibitors attenuate post-ischaemic neuronal death in organotypic hippocampal slice cultures. J.Neurochem. 82 1465 PMID: 12354294
Hamann et al (2008) Effects of kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dtsz mutant. Eur.J.Pharmacol. 586 156 PMID: 18353306
Justinova et al (2013) Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid. Nat.Neurosci. 16 1652 PMID: 24121737
Secci et al (2017) Attenuating nicotine reinforcement and relapse by enhancing endogenous brain levels of kynurenic acid in rats and squirrel monkeys. Neuropsychopharmacology 42 1619 PMID: 28139681
Zakhary et al (2020) Modification of kynurenine pathway via inhibition of kynurenine hydroxylase attenuates surgical brain injury complications in a male rat model. J Neurosci Res 98 155 PMID: 31257634
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Keywords: Ro 61-8048, Ro 61-8048 supplier, Potent, kynurenine, 3-hydroxylase, inhibitors, inhibits, NMDA, antagonists, increases, kynurenic, acid, levels, Tryptophan, Hydroxylase, 11-β, 11-beta, LTB-omega-Hydroxylase, Kynurenine, 3-Hydroxylase, Hydroxylases, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotr, 3-monooxygenase, 3254, Tocris Bioscience
2 Citations for Ro 61-8048
Citations are publications that use Tocris products. Selected citations for Ro 61-8048 include:
Gimenez-Gomez et al (2018) Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens. Neuropharmacology. 135 581 PMID: 29705534
Mailankot (2010) Induction of indoleamine 2,3-dioxygenase by IF.-gamma in human lens epithelial cells: apoptosis through the formation of 3-hydroxykynurenine. Int J Biochem Cell Biol 42 1446 PMID: 20435158
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
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Parkinson's Disease Poster
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