152658-17-8
中文名称
盐酸纳呋拉啡
英文名称
Nalfurafine
CAS
152658-17-8
分子式
C28H33ClN2O5
分子量
513.025
MOL 文件
152658-17-8.mol
更新日期
2026/08/01 09:25:12
结构式
基本信息
中文别名
盐酸呐呋拉菲
盐酸纳呋拉啡
纳呋拉啡盐酸
纳呋拉啡盐酸盐
盐酸纳呋拉啡
纳呋拉啡盐酸
纳呋拉啡盐酸盐
英文别名
TRK-820 HYDROCHLORIDE
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride
2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,hydrochloride (1:1), (2E)-
(E)-N-((4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-(furan-3-yl)-N-methylacrylamide
17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride
2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,hydrochloride (1:1), (2E)-
(E)-N-((4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl)-3-(furan-3-yl)-N-methylacrylamide
所属类别
有机原料：羧酸类化合物及衍生物
物理化学性质
| 熔点 | 207-217 °C |
| 储存条件 | -20°C储存 |
| 溶解度 | DMF: 16 mg/mL; DMSO: 33 mg/mL; Ethanol: 0.33 mg/mL; PBS (pH 7.2): 5 mg/mL |
| 形态 | 固体 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H336-H302 |
| 防范说明 | P261-P271-P304+P340-P312-P403+P233-P405-P501-P264-P270-P301+P312-P330-P501 |
应用领域
用途1
Nalfurafine hydrochloride was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by hemodialysis. It showed significant opioid 魏-agonist acti
vity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test.
A new therapeutic agent for the treatment of uremic pruritus in hemodialysis patients.
常见问题列表
生物活性
Nalfurafine hydrochloride (TRK-820 hydrochloride) 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，具有很高的翻译潜力。Nalfurafine hydrochloride (TRK-820 hydrochloride) 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的相关研究。
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 pre-injection 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. |