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Ro 61-8048

Cat. No. M3736

All AbMole products are for research use only, cannot be used for human consumption.

Ro 61-8048 Structure
Size Price Availability Quantity
5mg USD 58  USD58 In stock
10mg USD 78  USD78 In stock
50mg USD 210  USD210 In stock
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Quality Control & Documentation
Biological Activity

Ro 61-8048 is a potent and selective inhibitors of kynurenine hydroxylase with IC50 of 37 nM. In the present study, intrastriatal injections of Ro 61-8048 (60-80 microg/hemisphere) significantly reduced the severity of dystonia in dt(sz) hamsters, suggesting that kynurenine 3-hydroxylase inhibitors may be interesting candidates for managing dyskinesias which are related to striatal dysfunction. Ro 61-8048 increases brain KYNA levels and attenuates cannabinoid-induced increases in extracellular dopamine in reward-related brain areas. In the self-administration model of compound abuse, Ro 61-8048 reduced the rewarding effects of THC and the synthetic cannabinoid WIN 55,212-2 in squirrel monkeys and rats, respectively, and it also prevented relapse to drug-seeking induced by reexposure to cannabinoids or cannabinoid-associated cues. The effects of enhancing endogenous KYNA levels with Ro 61-8048 were prevented by positive allosteric modulators of α7nAChRs.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male albino rats and female gerbils
Formulation Suspended in 0.1% Tween-80 in water
Dosages 30 μmol/kg
Administration p.o.
Chemical Information
Molecular Weight 421.45
Formula C17H15N3O6S2
CAS Number 199666-03-0
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Justinova Z, et al. Nat Neurosci. Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid.

[2] Patricia A Zunszain, et al. Neuropsychopharmacology. Interleukin-1β: a new regulator of the kynurenine pathway affecting human hippocampal neurogenesis

[3] Caroline L Bellac, et al. J Neuropathol Exp Neurol. Inhibition of the kynurenine-NAD+ pathway leads to energy failure and exacerbates apoptosis in pneumococcal meningitis

[4] Hamann M, et al. Eur J Pharmacol. Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant.

[5] Richter A, et al. Eur J Pharmacol. The kynurenine 3-hydroxylase inhibitor Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia.

[6] S Rover, et al. J Med Chem. Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase

[7] QIN Xiuping, et al. Tianjin Journal of Traditional Chinese Medicine. Research progress of tryptophan-kynurenine metabolic pathways and neurodegenerative diseases with intervention of traditional Chinese medicine

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Keywords: Ro 61-8048 supplier, inhibitors, activators

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