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  1. Neuronal Signaling
  2. Serotonin Transporter
  3. Desvenlafaxine succinate

Desvenlafaxine succinate  (Synonyms: O-Desmethylvenlafaxine succinate; Wy-45233 succinate)

目錄號: HY-16170
產(chǎn)品使用指南

Desvenlafaxine succinate 是 Venlafaxine (HY-B0196) 主要代謝物的丁二酸鹽形式,是具有口服活性的、能透過血腦屏障的 5-HT 和 去甲腎上腺素 (norepinephrine) 再攝取的抑制劑,對hSERT和hNET 的IC50值分別為47.3 nM和531.3 nM。Desvenlafaxine succinate (DVS) 在人多巴胺(DA)轉(zhuǎn)運體上顯示弱的結(jié)合親和力。

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Desvenlafaxine succinate Chemical Structure

Desvenlafaxine succinate Chemical Structure

CAS No. : 448904-47-0

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Desvenlafaxine succinate 的其他形式現(xiàn)貨產(chǎn)品:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Desvenlafaxine succinate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), 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[1][2].

IC50 & Target

IC50: 47.3 nM (hSERT), 531.3 nM (hNET)[1].

體外研究
(In Vitro)

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內(nèi)研究
(In Vivo)

Desvenlafaxine succinate (30 mg/kg, orally) significantly increases extracellular NE levels but had no effect on DA levels using microdialysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats[1].
Dosage: 30 mg/kg.
Administration: Orally.
Result: Significantly increased extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis.
分子量

381.46

Formula

C20H31NO6

CAS 號
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

純度 & 產(chǎn)品資料
參考文獻(xiàn)
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  • Do most proteins show cross-species activity?

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產(chǎn)品名稱:
Desvenlafaxine succinate
目錄號:
HY-16170
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