盐酸纳呋拉啡
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 |
盐酸纳呋拉啡 用途与合成方法
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.
