
Duloxetine
CAS No. 116539-59-4
Duloxetine ( —— )
产品货号. M21972 CAS No. 116539-59-4
度洛西汀是一种血清素-去甲肾上腺素再摄取抑制剂(Ki 为 4.6 nM),用于治疗重度抑郁症和广泛性焦虑症。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
25MG | ¥761 | 有现货 |
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50MG | ¥1126 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Duloxetine
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述度洛西汀是一种血清素-去甲肾上腺素再摄取抑制剂(Ki 为 4.6 nM),用于治疗重度抑郁症和广泛性焦虑症。
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产品描述Duloxetine is an inhibitor of serotonin-norepinephrine reuptake(Ki of 4.6 nM),with treatment of major depressive disorder and generalized anxiety disorder.IC50 of duloxetine for the resting and inactivated wild-type hNav1.7 Na+ channel were 22.1+/-0.4 and 1.79+/-0.10 microM, respectively (mean+/-SE, n=5).?The IC50 for the open Na+ channel was 0.25+/-0.02 microM (n=5), as determined by the block of persistent late Nav1.7 Na+ currents.?Similar open-channel block by duloxetine was found in the muscle Nav1.4 isoform (IC50=0.51+/-0.05 microM;?n=5).?Block by duloxetine appeared via the conserved local anesthetic receptor as determined by site-directed mutagenesis.?Finally, duloxetine elicited strong use-dependent block of neuronal transient Nav1.7 Na+ currents during repetitive stimulations.
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体外实验Duloxetine ((S)-Duloxetine) inhibits the reuptake of serotonin and norepinephrine in the central nervous system. Duloxetine is also considered a less potent inhibitor of dopamine reuptake. However, duloxetine has no significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and GABA receptors and can therefore be considered to be a selective reuptake inhibitor at the 5-HT and NA transporters. Duloxetine undergoes extensive metabolism, but the major circulating metabolites do not contribute significantly to the pharmacologic activity. Major depressive disorder is believed to be due in part to an increase in pro-inflammatory cytokines within the central nervous system. Antidepressants including ones with a similar mechanism of action as duloxetine, i.e. serotonin metabolism inhibition, cause a decrease in proinflammatory cytokine activity and an increase in anti-inflammatory cytokines; this mechanism may apply to duloxetine in its effect on depression but research on cytokines specific to duloxetine therapy is lacking. The analgesic properties of duloxetine in the treatment of diabetic neuropathy and central pain syndromes such as fibromyalgia are believed to be due to sodium ion channel blockade.
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体内实验——
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同义词——
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通路Others
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靶点Other Targets
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受体serotonin-norepinephrine reuptake
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研究领域——
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适应症——
化学信息
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CAS Number116539-59-4
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分子量297.42
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分子式C18H19NOS
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纯度>98% (HPLC)
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溶解度——
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SMILESCNCC[C@H](Oc1cccc2ccccc12)c1cccs1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Wang, S.Y., J. Calderon, and G. Kuo Wang, Block of neuronal Na+ channels by antidepressant duloxetine in a state-dependent manner. Anesthesiology, 2010. 113(3): p. 655-65.2. Ekram, A, R,et al. Duloxetine in Painful Diabetic Neuropathy: A Systematic Review[J]. Clinical Journal of Pain, 2016.
产品手册




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