盐酸纳呋拉啡
| 中文名称 | 盐酸纳呋拉啡 |
|---|---|
| 中文同义词 | 盐酸纳呋拉啡;纳呋拉啡盐酸;盐酸呐呋拉菲;纳呋拉啡盐酸盐;盐酸纳呋拉啡,盐酸纳法拉芬;盐酸纳呋拉啡杂质 |
| 英文名称 | Nalfurafine |
| 英文同义词 | 17-Cyclopropylmethyl-3,14beta-dihydroxy-4,5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride;TRK-820 HYDROCHLORIDE;(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;2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,hydrochloride (1:1), (2E)-;Nafurarphine Hydrochloride;Nalfurafina;AC 820;AC820 |
| CAS号 | 152658-17-8 |
| 分子式 | C28H33ClN2O5 |
| 分子量 | 513.02502 |
| EINECS号 | 200-258-5 |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;医药原料药;医药原料;原料药及中间体;Agonists;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;Inhibitors;化药杂质-盐酸纳呋拉啡 |
| Mol文件 | 152658-17-8.mol |
| 结构式 |  |
盐酸纳呋拉啡 性质
| 熔点 | 207-217 °C |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：16mg/mL；二甲基亚砜：33mg/mL；乙醇：0.33mg/mL； PBS（pH 7.2）：5 mg/mL |
| 形态 | 固体 |
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. |
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 κ-agonist activity 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.