NalfuRafine hydrochloride 是一种阿片类 κ 选择性激动剂,可增强 MOR 靶向缓解疼痛类药物的生物学作用,有潜力用于尿毒症瘙痒的相关研究。
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描述
Nalfurafine(TRK-820) is an opioid κ-selective agonist; has been approved in Japan for treatment of itch in patients with chronic kidney disease.
体内活性
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].
Cas No.
152658-17-8
分子式
C28H33ClN2O5
分子量
513.03
别名
TRK-820 hydrochloride;盐酸纳呋拉啡
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years