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Desvenlafaxine

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Chemical Structure| 93413-62-8 同义名 : o-去甲文拉法辛 ;O-Desmethylvenlafaxine;DVS 233;MDD-XR;(±)-O-Desmethyl Venlafaxine;WY 45233 Succinate
CAS号 : 93413-62-8
货号 : A105155
分子式 : C16H25NO2
纯度 : 98%
分子量 : 263.375
MDL号 : MFCD00871934
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(189.84 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

0.5% methylcellulose+0.2% Tween 80+water 30 mg/mL suspension

生物活性
靶点

  • 5-HT

    5-HT, Ki:40.2 nM
描述 Biogenic amines such as serotonin (5-HT), norepinephrine (NE), and dopamine (DA) are neurotransmitters found in areas of the central nervous system (CNS) known to be important for regulation of cognitive function, mood, thermo-regulation, pain sensation, sexual function, and various aspects of endocrine function related to homeostasis. Desvenlafaxine exhibits inhibitory activity of serotonin (5-HT) and norepinephrine (NE) reuptake with Ki of 40.2 and 558.4 nM, respectively. Desvenlafaxine inhibited the uptake of [3H]5-HT at the hSERT with a mean IC50 value of 47.3 ± 19.4 nM. In addition, the IC50 value of desvenlafaxine for [3H]NE uptake was 531.3 ± 113.0 nM. Acute oral administration of desvenlafaxine (30 mg/kg) did not significantly alter concentrations of 5-HT in the hypothalamus. However, pretreatment with WAY-100635 (5-HT1A antagonist, 0.3 mg/kg s.c.), which did not alter 5-HT levels on its own, resulted in a significant 78% increase in extracellular 5-HT levels in the rat hypothalamus. In contrast, acute administration of desvenlafaxine, when given alone, produced a significant increase in NE concentrations[3]. The response and remission rates of depression at 8 weeks for the 50-mg dose of desvenlafaxine are 51-63% and 31-45%, respectively[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00797966 Major Depressive Disorder Phase 2 Completed - -
NCT00797966 - Completed - -
NCT01916824 Major Depressive Disorder ... 展开 >> Healthy Controls 收起 << Phase 4 Completed - United States, Georgia ... 展开 >> Emory Mood and Anxiety Disorders Program Atlanta, Georgia, United States, 30322 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.80mL

0.76mL

0.38mL

18.98mL

3.80mL

1.90mL

37.97mL

7.59mL

3.80mL
参考文献

[1]Sopko MA Jr, Ehret MJ, Grgas M. Desvenlafaxine: another "me too" drug? Ann Pharmacother. 2008 Oct;42(10):1439-46.

[2]Deecher DC, Beyer CE, et al.Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.

[3]Deecher DC, Beyer CE, Johnston G, et al. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006;318(2):657‐665

[4]Sopko MA Jr, Ehret MJ, Grgas M. Desvenlafaxine: another "me too" drug?. Ann Pharmacother. 2008;42(10):1439‐1446