Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT

Product Name : Nalfurafine hydrochloride Catalog Number : T2388 CAS Number : 152658-17-8 Molecular Formula : C28H33ClN2O5 Molecular Weight : 513.03 Apprearence : Solid

Description: Nalfurafine(TRK-820) is an opioid κ-selective agonist; has been approved in Japan for treatment of itch in patients with chronic kidney disease.

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

DMSO 10 mM Solubility ( < 1 mg/ml refers to the product slightly soluble or insoluble )

Receptor (IC50) κ-opioid receptor

In vivo Activity 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]. Animal Experiment Animal Model: Mice

Reference 1. Acta Derm Venereol. 2015 Feb;95(2):147-50. doi: 10.2340/00015555-1879. 2. Ikeda K, et al. TRK-820, a selective kappa opioid receptor agonist, could effectively ameliorate L-DOPA-induced dyskinesia symptoms in a rat model of Parkinson's disease. Eur J Pharmacol. 2009 Oct 12;620(1-3):42-8. 3. Yoshikawa S, et al. Effects of TRK-820, a selective kappa opioid receptor agonist, on rat schizophrenia models. Eur J Pharmacol. 2009 Mar 15;606(1-3):102-8.

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