152657-84-6
152657-84-6 结构式
基本信息
中文别名
纳呋拉啡纳呋拉啡杂质
纳呋拉啡杂质1
英文别名
NALFURAFINENalfuranfine
Nalfuranfine impurity
2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,(2E)-
2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-
(E)-N-[(5alpha,6beta)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点700.7±60.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 10mM
酸度系数(pKa)9.37±0.60(Predicted)
形态结晶固体
常见问题列表
生物活性
Nalfurafine (TRK-820) 是一种强效选择性，具有口服活性的 G 蛋白偏倚 kappa opioid receptor (KOR) 激动剂，具有很高的转化潜力。Nalfurafine (TRK-820) 增强了 MOR 靶向镇痛药的生物学作用，它还有潜力用于尿毒症瘙痒研究的相关研究。靶点
IC50: kappa opioid receptor (KOR)
体内研究
Nalfurafine (subcutaneous injection; 0.015 mg/kg) combines with EOM-salvinorin-B produces spinal antinociception equivalent to 5 mg/kg, it also enhances the supraspinal analgesic effect of 5 mg/kg morphine. Nalfurafine (subcutaneous injection; 4 μg/kg) causes a dose-dependent increase of the inhibition of the acetic acid-induced abdominal constriction,and the inhibition of the abdominal constriction reaches its peak 30 min after injection, gradually declined and returned to the preinjection level 4 hr after.
| Animal Model: | Male and Female C57BL/6J mice |
| Dosage: | 0.015 mg/kg |
| Administration: | Subcutaneous injection |
| Result: | Had the potential for enhancing the therapeutic potential of MOR-targeting analgesics, such as morphine. |