Nalfurafine - CAS 152657-84-6
Catalog number:
152657-84-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H32N2O5
Molecular Weight:
476.56
COA:
Inquire
Targets:
Opioid Receptor
Description:
Nalfurafine is a selective and centrally-penetrant κ-opioid receptor (KOR) agonist without significant activity on μ- and δ-opioid receptors. With antipruritic activity, nalfurafine hydrochloride can significantly decrease the worst itching, itching inten
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Appearance:
Solid powder
Synonyms:
(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 17-cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-(N-methyl-trans-
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -54℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Quantity:
Grams-Kilos
Boiling Point:
700.7±60.0 °C | Condition: Press: 760 Torr
Density:
1.41±0.1 g/cm3
InChIKey:
XGZZHZMWIXFATA-UEZBDDGYSA-N
InChI:
1S/C28H32N2O5/c1-29(23(32)7-4-18-9-13-34-16-18)20-8-10-28(33)22-14-19-5-6-21(31)25-24(19)27(28,26(20)35-25)11-12-30(22)15-17-2-3-17/h4-7,9,13,16-17,20,22,26,31,33H,2-3,8,10-12,14-15H2,1H3/b7-4+/t20-,22-,26+,27+,28-/m1/s1
Canonical SMILES:
CN(C1CCC2(C3CC4=C5C2(C1OC5=C(C=C4)O)CCN3CC6CC6)O)C(=O)C=CC7=COC=C7
1.Phoenixin: A candidate pruritogen in the mouse.
Cowan A1, Lyu RM2, Chen YH3, Dun SL4, Chang JK2, Dun NJ5. Neuroscience. 2015 Dec 3;310:541-8. doi: 10.1016/j.neuroscience.2015.09.055. Epub 2015 Sep 28.
Phoenixin (PNX) is a 14-amino acid amidated peptide (PNX-14) or an N-terminal extended 20-residue amidated peptide (PNX-20) recently identified in neural and non-neural tissue. Mass spectrometry analysis identified a major peak corresponding to PNX-14, with negligible PNX-20, in mouse spinal cord extracts. Using a previously characterized antiserum that recognized both PNX-14 and PNX-20, PNX-immunoreactivity (irPNX) was detected in a population of dorsal root ganglion (DRG) cells and in cell processes densely distributed to the superficial layers of the dorsal horn; irPNX cell processes were also detected in the skin. The retrograde tracer, Fluorogold, injected subcutaneously (s.c.) to the back of the cervical and thoracic spinal cord of mice, labeled a population of DRG, some of which were also irPNX. PNX-14 (2, 4 and 8 mg/kg) injected s.c.to the nape of the neck provoked dose-dependent repetitive scratching bouts directed to the back of the neck with the hindpaws.
2.Characteristics of scratching behavior in ADJM mice (atopic dermatitis from Japanese mice).
Nakasone T1, Sato T, Matsushima Y, Inoue T, Kamei C. Immunopharmacol Immunotoxicol. 2015 Apr;37(2):202-6. doi: 10.3109/08923973.2014.1001903. Epub 2015 Jan 12.
In order to elucidate the characteristics of scratching behavior in atopic dermatitis from Japanese mice (ADJM) mice, the effects of some antagonists of pruritogens on this behavior were studied. Both male and female ADJM mice showed frequent scratching behavior around the face, abdomen and back. The number of scratching behavior around the face was greater than on the abdomen and back, and scratching behavior in female mice was significantly more frequent than in male mice. Histamine H1 antagonist, chlorpheniramine, p.o., inhibited this behavior potently and dose-dependently. Histamine H1 antagonist with serotonin 5-TH(5-hydroxytryptamine)2 antagonist, cyproheptadine, also inhibited this behavior. However, NK1 antagonist, aprepitant, p.o., had no significant inhibitory effect even at a dose of 100 mg/kg, p.o., Mu antagonist, naloxone, and kappa agonist, nalfurafine, significantly inhibited this behavior at doses of 0.3 mg/kg, s.c., and 0.
3.An evidence-based review of systemic treatments for itch.
Pongcharoen P1, Fleischer AB Jr2. Eur J Pain. 2016 Jan;20(1):24-31. doi: 10.1002/ejp.766. Epub 2015 Sep 28.
BACKGROUND AND OBJECTIVE: Many treatment modalities are used for itch treatment in daily medical practices without adequate evidence of their efficacy. The purpose of this study was to provide an evidence-based review of the literature as to the clinical benefits of systemic anti-itch treatments.
4.Drug-Drug Interactions of a Novel κ-Opioid Receptor Agonist, Nalfurafine Hydrochloride, Involving the P-Glycoprotein.
Ando A1, Sasago S, Ohzone Y, Miyamoto Y. Eur J Drug Metab Pharmacokinet. 2015 Jun 10. [Epub ahead of print]
BACKGROUND AND OBJECTIVE: Nalfurafine hydrochloride (TRK-820), which exhibits strong κ-opioid agonistic activity, has an antipruritic effect on uremic pruritus. The permeability of nalfurafine across human P-glycoprotein (P-gp)-expressing LLC-PK1 cells was investigated to evaluate drug-drug interactions (DDI) involving the P-gp efflux transporter of nalfurafine. Furthermore, we assessed the ratio of brain/plasma concentrations (K p) as an indicator to investigate the changes in the blood-brain barrier (BBB) transport through P-gp when digoxin or verapamil was concomitantly administered with nalfurafine in mice.
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CAS 152657-84-6 Nalfurafine

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