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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 2024/03/25 22:11:38
152658-17-8 结构式 152658-17-8 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
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
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

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.
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