Nalfurafine hydrochloride

Modify Date: 2024-01-02 18:34:07

Nalfurafine hydrochloride Structure
Nalfurafine hydrochloride structure
Common Name Nalfurafine hydrochloride
CAS Number 152658-17-8 Molecular Weight 513.025
Density N/A Boiling Point N/A
Molecular Formula C28H33ClN2O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Nalfurafine hydrochloride


Nalfurafine hydrochloride is a κ-opioid agonist and an anti-itch drug approved in Japan.

 Names

Name Nalfurafine Hydrochloride
Synonym More Synonyms

 Nalfurafine hydrochloride Biological Activity

Description Nalfurafine hydrochloride is a κ-opioid agonist and an anti-itch drug approved in Japan.
Related Catalog
In Vivo Nalfurafine (subcutaneous injection; 0.015 mg/kg) combines with EOM-salvinorin-B  produces spinal antinociception equivalent to 5 mg/kg, it also enhances the supraspinal analgesic effect of 5 mg/kg morphine[1]. Nalfurafine (subcutaneous injection; 4 μg/kg) causes a dose-dependent increase of the inhibition of the acetic acid-induced abdominal constriction,and the inhibition of the abdominal constriction reaches its peak 30 min after injection, gradually declined and returned to the pre-injection level 4 hr after[2]. Animal Model: Male and Female C57BL/6J mice[1] Dosage: 0.015 mg/kg Administration: Subcutaneous injection Result: Had the potential for enhancing the therapeutic potential of MOR-targeting analgesics, such as morphine.
References

[1]. Kaski SW, et al. Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine.J Pharmacol Exp Ther. 2019 Nov;371(2):487-499.

[2]. Endoh T, et al. Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.Life Sci. 1999;65(16):1685-94.

 Chemical & Physical Properties

Molecular Formula C28H33ClN2O5
Molecular Weight 513.025
Exact Mass 512.207825
PSA 86.38000
LogP 3.82960
Storage condition -20℃

 Synonyms

Nalfurafine hydrochloride
(2E)-N-[(5α,6β)-17-(Cyclopropylmethyl)-3,14-dihydroxy-4,5-epoxymorphinan-6-yl]-3-(3-furyl)-N-methylacrylamide hydrochloride (1:1)
2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-, hydrochloride (1:1)
(E)-N-[(4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl]-3-(furan-3-yl)-N-methylprop-2-enamide,hydrochloride
Nalfurafine (hydrochloride)