Desvenlafaxine succinate hydrate 是 Venlafaxine 主要代谢物的丁二酸盐形式，在人多巴胺转运体上显示弱的结合亲和力。它是具有口服活性的、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 hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).

Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] Desvenlafaxine Succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with Desvenlafaxine Succinate, which could impact the metabolism of drugs metabolized via this enzyme. [2]

Desvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. [1] Desvenlafaxine Succinate exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.[2]

386750-22-7

C20H33NO7

399.48

Desvenlafaxine Succinate;WY 45233 Succinate;O-Desmethylvenlafaxine succinate hydrate;琥珀酸去甲文拉法辛

DMSO:33 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years