中文名称:

纳呋拉啡

中文同义词:

纳呋拉啡;纳呋拉啡杂质1;纳呋拉啡杂质

英文名称:

NALFURAFINE

英文同义词:

NALFURAFINE;Nalfuranfine;(E)-N-[(5alpha,6beta)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide;Nalfuranfine impurity;2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-;2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,(2E)-

CAS号:

152657-84-6

分子式:

C28H32N2O5

分子量:

476.56

EINECS号:

相关类别:

植物提取;医用原料

Mol文件:

152657-84-6.mol

沸点 

700.7±60.0 °C(Predicted)

密度 

1.41±0.1 g/cm3(Predicted)

酸度系数(pKa)

9.37±0.60(Predicted)

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.

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.