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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.
Int Immunopharmacol. 2023 Dec;125(Pt B):111196.
Tryptophan metabolism regulates inflammatory macrophage polarization as a predictive factor for breast cancer immunotherapy
Ro 61-8048 purchased from AbMole
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Animal models | Male albino rats and female gerbils |
Formulation | Suspended in 0.1% Tween-80 in water |
Dosages | 30 μmol/kg |
Administration | p.o. |
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 |
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