152658-17-8

152658-17-8 structure

Name: Nalfurafine hydrochloride
Chemical Name: Nalfurafine Hydrochloride
CAS Number: 152658-17-8
Molecular Formula: C₂₈H₃₃ClN₂O₅
Molecular Weight: 513.025
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2018-03-21 08:00:00
Modify Date: 2024-01-02 18:34:07
Nalfurafine hydrochloride is a κ-opioid agonist and an anti-itch drug approved in Japan.

Name	Nalfurafine Hydrochloride
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)

Description	Nalfurafine hydrochloride is a κ-opioid agonist and an anti-itch drug approved in Japan.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
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.