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Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active kappa opioid receptor (KOR) agonist. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics.
A single administration of subcutaneous TRK-820 significantly increased spontaneous ipsilateral rotational behavior of hemi-parkinsonian rats at 30 μg/kg though the efficacy is moderate and also significantly inhibited L-DOPA-induced dyskinesia at 10 and 30 μg/kg; this inhibition is reversed in the presence of nor-binaltorphimine, a kappa opioid receptor antagonist. TRK-820 dose-dependently inhibited phencyclidine-induced rat hyperlocomotion. TRK-820 dose-dependently attenuated the biochemical changes of both dopamine and serotonin in the prefrontal cortex of rats treated with phencyclidine without affecting their basal levels in normal rats.
| Molecular Weight | 513.03 |
| Formula | C28H33ClN2O5 |
| CAS Number | 152658-17-8 |
| Solubility (25°C) | DMSO 30 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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