Desvenlafaxine succinate 是 Venlafaxine 主要代谢物的丁二酸盐形式，是具有口服活性的、能透过血脑屏障的 5-HT 和 去甲肾上腺素 (norepinephrine) 再摄取的抑制剂，对hSERT和hNET 的IC50值分别为47.3 nM和531.3 nM。Desvenlafaxine succinate (DVS) 在人多巴胺(DA)转运体上显示弱的结合亲和力。
| 生物活性 |
Desvenlafaxine succinate, the succinate salt form of the isolated major active metabolite of Venlafaxine , is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. |
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| 体外研究 |
Desvenlafaxine succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Desvenlafaxine succinate also induces CYP3A4, which could impact the metabolism of drugs metabolized via this enzyme. |
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| 体内研究 |
Desvenlafaxine succinate (30 mg/kg, orally) significantly increases extracellular NE levels but had no effect on DA levels using microdialysis.
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| 分子式 |
C16H25NO2.C4H6O4
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| 分子量 |
381.46
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| CAS号 |
448904-47-0
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
纯度： 98%
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Data Sheet
