盐酸纳呋拉啡
- CAS号:152658-17-8
- 英文名:Nalfurafine
- 中文名:盐酸纳呋拉啡
- CBNumber:CB72502851
- 分子式:C28H33ClN2O5
- 分子量:513.02502
- MOL File:152658-17-8.mol
- 熔点 :207-217 °C
- 储存条件 :Store at -20°C
- 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 :A solid
盐酸纳呋拉啡性质、用途与生产工艺
- 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。
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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. -
用途
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.
- 公司名称:TORONTO
- 联系电话:--
- 电子邮件:info@trc-canada.com
- 国家:加拿大
- 产品数:6088
- 优势度:71