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
Publictions citing BOC Sciences Products
  • >> More
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Opioid Receptor Products


Alvimopan monohydrate
(CAS: 1383577-62-5)

The monohydrate salt form of Alvimopan could be commonly used in postoperative recovery of gastrointestinal for acting as a mu-opioid receptor (PAM-OR) antagoni...

CAS 89352-67-0 ICI 174,864

ICI 174,864
(CAS: 89352-67-0)

ICI 174,864 is a potent and highly selective δ opioid antagonist. It shows partial agonist in vitro activity at δ receptors at high concentrations.

CAS 83335-41-5 Dynorphin B

Dynorphin B
(CAS: 83335-41-5)

Dynorphin B is a 13-residue opioid peptide, which is derived from the cleavage of prodynorphin and found widely distributed in the central nervous system. It ac...

CAS 63631-40-3 DADLE

DADLE
(CAS: 63631-40-3)

DADLE is a prototypical δ-opioid receptor agonist with antinociceptive activity. It also exhibits activity at the μ-opioid receptor.

CAS 67197-96-0 (±)-U-50488 hydrochloride

(±)-U-50488 hydrochloride
(CAS: 67197-96-0)

(±)-U-50488 hydrochloride is a selective κ-opioid agonist with no μ-opioid antagonist effects. (±)-U-50488 hydrochloride blocks Na+ channels at high concentrati...

CAS 236098-40-1 [Arg14,Lys15]Nociceptin

[Arg14,Lys15]Nociceptin
(CAS: 236098-40-1)

[Arg14,Lys15]Nociceptin behaves as a highly potent agonist of the OP(4) receptor (EC50 = 1 nM) and is able to produce long-lasting effects in vivo, compared wit...

CAS 212609-11-5 Nocistatin (human)

Nocistatin (human)
(CAS: 212609-11-5)

Nocistatin (human) is a human putative counterpart of nocistatin (bovine). Nocistatin is widely present in the spinal cord and brain, and is a novel bioactive p...

CAS 189388-22-5 Endomorphin 1

Endomorphin 1
(CAS: 189388-22-5)

Endomorphin 1 is a high affinity (Ki = 360 pM) and highly selective agonist of theμ-opioid receptor with 4000- and 15000-fold preference over δ and κ respective...

CHIR 4531
(CAS: 158198-48-2)

CHIR 4531, an oligopeptides compound, has been found to be an opioid mu receptor agonist and was once studied in pain therapy.

CAS 1355244-02-8 ML 190

ML 190
(CAS: 1355244-02-8)

ML 190 is a κ opioid receptor antagonist with IC50 value of 120 nM.

CAS 207452-97-9 N-MPPP Hydrochloride

N-MPPP Hydrochloride
(CAS: 207452-97-9)

N-MPPP Hydrochloride is a high affinity and selective agonist of the κ opioid receptor (KOR-1) with no measured binding at μ or δ sites.

CAS 200959-47-3 Ac-RYYRWK-NH

Ac-RYYRWK-NH
(CAS: 200959-47-3)

Ac-RYYRWK-NH, a hexapeptide, is a partial agonist of the nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptorr (Ki = 0.71 nM), which exhibits selectivity over ...

CAS 850173-95-4 ADL5859 HCl

ADL5859 HCl
(CAS: 850173-95-4)

ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel.

CAS 64963-01-5 [D-Ala2]-Leucine enkephalin

[D-Ala2]-Leucine enkephalin
(CAS: 64963-01-5)

[D-Ala2]-Leucine enkephalin is a delta opioid agonist used to study the signaling pathway of delta opioid receptors.

CAS 684238-37-7 BMS 986187

BMS 986187
(CAS: 684238-37-7)

BMS 986187 is a potent and selective δ-opioid receptor positive allosteric modulator (EC50 = 30 nM) exhibiting 100-fold selectivity for δ over μ-opioid receptor...

CAS 141801-26-5 Endomorphin 2

Endomorphin 2
(CAS: 141801-26-5)

Endomorphin 2, an andogenous peptide, has high affinity and specificity for the μ-opioid receptor and displays reasonable affinities for kappa3 binding sites, w...

CAS 361444-66-8 JDTic

JDTic
(CAS: 361444-66-8)

A 4-phenylpiperidine derivative, for the κ-opioid receptor.

Cebranopadol
(CAS: 863513-91-1)

Cebranopadol is a novel first in class compounds with potent agonist activity on opioid receptor like -1(ORL-1) and the well established mu opioid receptor. lt ...

CAS 78123-71-4 DAMGO

DAMGO
(CAS: 78123-71-4)

DAMGO is a highly selective peptide agonist of the μ opioid receptor.

CAS 113158-35-3 Nor-Binaltorphimine dihydrochloride

Nor-Binaltorphimine dihydrochloride
(CAS: 113158-35-3)

Nor-Binaltorphimine dihydrochloride is a potent and selective kappa opioid receptor antagonist.

Chemical Structure

CAS 152657-84-6 Nalfurafine

Quick Inquiry

Verification code

Featured Items