1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor

Nalfurafine hydrochloride (Synonyms: TRK-820 hydrochloride)

Cat. No.: HY-12745A Purity: 99.93%
Handling Instructions

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

For research use only. We do not sell to patients.

Nalfurafine hydrochloride Chemical Structure

Nalfurafine hydrochloride Chemical Structure

CAS No. : 152658-17-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 488 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 432 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 2160 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Other Forms of Nalfurafine hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

In Vivo

In mice with experimental dry skin, nalfurafine abolished spontaneous scratching but had no effect on alloknesis[1]. A single administration of subcutaneous TRK-820 significantly increased spontaneous ipsilateral rotational behavior of hemi-parkinsonian rats at 30 μg/kg though the efficacy is moderate and also significantly inhibited L-DOPA-induced dyskinesia at 10 and 30 μg/kg; this inhibition is reversed in the presence of nor-binaltorphimine, a kappa opioid receptor antagonist[2]. TRK-820 dose-dependently inhibited phencyclidine-induced rat hyperlocomotion. TRK-820 dose-dependently attenuated the biochemical changes of both dopamine and serotonin in the prefrontal cortex of rats treated with phencyclidine without affecting their basal levels in normal rats[3].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 21 mg/mL (40.93 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9492 mL 9.7460 mL 19.4920 mL
5 mM 0.3898 mL 1.9492 mL 3.8984 mL
10 mM 0.1949 mL 0.9746 mL 1.9492 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1][2]

Rats: Nalfurafine is given to male Sprague-Dawley rats at volume of 1 mL/kg. After collecting control samples for 80 min, PCP (10 mg/kg, i.p.) is administered to the rats, and then the collection of dialysate is continued for 180 min. Pre-treatment with TRK-820 or vehicle is performed subcutaneously 5 min before the administration of PCP. Dopamine and serotonin levels in the dialysate are quantified by high-performance liquid chromatography[2].

Mice: Chronic dry skin on the nape of the neck is induced on the C57BL/6 mice. Nalfurafine (20 μg/kg) or saline is administered. Then alloknesis testing is conducted[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

513.03

Formula

C₂₈H₃₃ClN₂O₅

CAS No.

152658-17-8

SMILES

O[[email protected]@]1(CC[[email protected]@H](N(C)C(/C=C/C2=COC=C2)=O)[[email protected]]3([H])OC4=C5O)[[email protected]]63C4=C(C=C5)C[[email protected]@]1([H])N(CC7CC7)CC6.[H]Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Nalfurafine hydrochloride
Cat. No.:
HY-12745A
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Nalfurafine hydrochloride

Cat. No.: HY-12745A