NalfuRafine 是一种有效且特异性的 G 蛋白偏倚 κ-阿片受体激动剂,具有高转化潜力。 NalfuRafine 增强了 MOR 靶向镇痛药的生物学作用,可用于尿毒症瘙痒症的相关研究。
产品描述
Nalfurafine is an effective and selective agonist of G protein-biased κ-opioid receptor with high translational potential. Nalfurafine enhances the therapeutic potential of MOR-targeting analgesics and can be used for uremic pruritis treatment studies.
体内活性
Nalfurafine (4 μg/kg; s.c.) increased the inhibition of the acetic acid-induced abdominal constriction in a dose-dependent manner, inhibited the abdominal constriction reaching its peak 30 min after injection, gradually declined, and returned to the preinjection level 4 hr after[1]. Nalfurafine (0.015 mg/kg; s.c.) combines with EOM-salvinorin-B produced spinal antinociception equivalent to 5 mg/kg. Nalfurafine also enhanced the supraspinal analgesic effect of 5 mg/kg morphine[2].
Cas No.
152657-84-6
分子式
C28H32N2O5
分子量
476.573
别名
纳呋拉啡;TRK-820
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years