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盐酸纳呋拉啡

盐酸纳呋拉啡,152658-17-8,结构式
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
盐酸纳呋拉啡化学性质
  • 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。
  • 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.

盐酸纳呋拉啡上下游产品信息
上游原料
下游产品
盐酸纳呋拉啡生产厂家
  • 公司名称:LGM Pharma
  • 联系电话:1-(800)-881-8210
  • 电子邮件:inquiries@lgmpharma.com
  • 国家:美国
  • 产品数:2127
  • 优势度:70
  • 公司名称:上海喀露蓝科技有限公司
  • 联系电话: 18149758185
  • 电子邮件:sales-cpd@caerulumpharma.com
  • 国家:中国
  • 产品数:3420
  • 优势度:58
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