纳呋拉啡
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- CAS号:
- 152657-84-6
- 英文名:
- NALFURAFINE
- 英文别名:
- NALFURAFINE;Nalfuranfine;Nalfuranfine impurity;Nalfuranfine Impurity 1;pruritis,uremic,inhibit,TRK 820,Inhibitor,agonist,Nalfurafine,Opioid Receptor,analgesic,TRK820;2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,(2E)-;2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-;(E)-N-[(5alpha,6beta)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide
- 中文名:
- 纳呋拉啡
- 中文别名:
- 纳呋芬;纳呋拉啡;纳呋拉啡杂质;纳呋拉啡杂质1;NALFURAFINE纳呋拉啡
- CBNumber:
- CB02451260
- 分子式:
- C28H32N2O5
- 分子量:
- 476.56
- MOL File:
- 152657-84-6.mol
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纳呋拉啡化学性质
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沸点:
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700.7±60.0 °C(Predicted)
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密度:
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1.41±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 10mM
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形态:
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A crystalline solid
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酸度系数(pKa):
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9.37±0.60(Predicted)
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纳呋拉啡性质、用途与生产工艺
Nalfurafine (TRK-820) 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，具有很高的转化潜力。Nalfurafine (TRK-820) 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研究的相关研究。
IC50: kappa opioid receptor (KOR)
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 preinjection level 4 hr after.
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Animal Model:
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Male and Female C57BL/6J mice
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Dosage:
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0.015 mg/kg
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Administration:
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Subcutaneous injection
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Result:
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Had the potential for enhancing the therapeutic potential of MOR-targeting analgesics, such as morphine.
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纳呋拉啡
上下游产品信息
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下游产品
152657-84-6, 纳呋拉啡 相关搜索:
- 杂质对照品
- 对照品-杂质对照品
- 医用原料
- 植物提取
- NALFURAFINE纳呋拉啡
- 纳呋芬
- 纳呋拉啡杂质
- 纳呋拉啡杂质1
- 纳呋拉啡
- 152657-84-6
- pruritis,uremic,inhibit,TRK 820,Inhibitor,agonist,Nalfurafine,Opioid Receptor,analgesic,TRK820
- Nalfuranfine Impurity 1
- 2-Propenamide, N-[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-,(2E)-
- 2-Propenamide, N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-, (2E)-
- NALFURAFINE
- Nalfuranfine impurity
- (E)-N-[(5alpha,6beta)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide
- Nalfuranfine