Nalfurafine is an effective and selective agonist of G protein-biased κ-opioid receptor with high translational potential. Nalfurafine enhances the therapeutic potential of MOR-targeting analgesics.
In vivo, Nalfurafine (4 μg/kg; s.c.) increased the inhibition of the acetic acid-induced abdominal constriction in a dose-dependent manner, inhibited the abdominal constriction reaching its peak 30 min after injection, gradually declined, and returned to the preinjection level 4 hr after. Nalfurafine (0.015 mg/kg; s.c.) combines with EOM-salvinorin-B produced spinal antinociception equivalent to 5 mg/kg.
| Molecular Weight | 476.56 |
| Formula | C28H32N2O5 |
| CAS Number | 152657-84-6 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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