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Venlafaxine

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Chemical Structure| 93413-69-5 同义名 : D，L-文拉法辛 ;Wy 45030
CAS号 : 93413-69-5
货号 : A901971
分子式 : C17H27NO2
纯度 : 98%
分子量 : 277.402
MDL号 : MFCD00864385
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(901.22 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：
生物活性
靶点

  • 5-HT
描述 Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant. Venlafaxine inhibited binding to the human NE and 5-HT transporters with K(i) values of 2480 and 82 nM, respectively, and with a K(i) ratio of 30. Venlafaxine inhibited ex vivo binding to rat 5-HT transporters and NE transporters with ED(50) values of 2 and 54 mg/kg, respectively. Venlafaxine had ED(50) values of 5.9 and 94 mg/kg for blocking p-chloramphetamine- and 6-hydroxydopamine-induced monoamine depletion, respectively[3]. Compared to acetic acid control, venlafaxine at dose of 40 mg/kg as well as dexamethasone significantly improved colitis parameters in both reserpinised and non-reserpinised animals. Venlafaxine reduced inflammatory injury in this animal model of induced ulcerative colitis[4]. Venlafaxine (16 mg/kg) reversed STZ-induced elevated thiobarbituric acid reactive substance (TBARS) levels and also restored the glutathione (GSH) levels in diabetic mice. Venlafaxine (8 and 16 mg/kg) per se does not produce any significant effect in normal animals. A dose-dependent antidepressant action of venlafaxine in diabetes-induced depressive mice[5].
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
NCT00788944 Depression Phase 4 Completed - -
NCT00205491 TBI (Traumatic Brain Injury) Phase 4 Completed - United States, Virginia ... 展开 >> Virginia Commonwealth University Richmond, Virginia, United States, 23298 收起 <<
NCT00316160 Depressive Disorder, Major ... 展开 >> Major Depressive Disorder (MDD) 收起 << Phase 4 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.60mL

0.72mL

0.36mL

18.02mL

3.60mL

1.80mL

36.05mL

7.21mL

3.60mL
参考文献

[1]Bymaster FP, Dreshfield-Ahmad LJ, et al. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80.

[2]Goeringer KE, McIntyre IM, et al. Postmortem tissue concentrations of venlafaxine. Forensic Sci Int. 2001 Sep 15;121(1-2):70-5.

[3]Bymaster FP, Dreshfield-Ahmad LJ, Threlkeld PG, Shaw JL, Thompson L, Nelson DL, Hemrick-Luecke SK, Wong DT. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80

[4]Minaiyan M, Hajhashemi V, Rabbani M, Fattahian E, Mahzouni P. Effect of venlafaxine on experimental colitis in normal and reserpinised depressed rats. Res Pharm Sci. 2015 Jul-Aug;10(4):295-306

[5]Khanam R, Najfi H, Akhtar M, Vohora D. Evaluation of venlafaxine on glucose homeostasis and oxidative stress in diabetic mice. Hum Exp Toxicol. 2012 Dec;31(12):1244-50