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.
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Yan Zhou, et al. Handb Exp Pharmacol. Preclinical Studies on Nalfurafine (TRK-820), a Clinically Used KOR Agonist
 Shane W Kaski, et al. J Pharmacol Exp Ther . Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine
 Hugh C Rayner, et al. Clin J Am Soc Nephrol. International Comparisons of Prevalence, Awareness, and Treatment of Pruritus in People on Hemodialysis
 Thomas Mettang, et al. Kidney Int. Uremic pruritus
 T Endoh, et al. Jpn J Pharmacol. TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys
 T Endoh, et al. Eur J Pharmacol. Characterization of the antinociceptive effects of TRK-820 in the rat
 T Endoh, et al. Life Sci . Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist
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