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Venlafaxine HCl

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Chemical Structure| 99300-78-4 同义名 : 盐酸万拉法新 ;Wy 45030 hydrochloride;Venlafaxine (hydrochloride) (CRM);Wy 45030;Wy 453 HCl;Venlafaxine hydrochloride
CAS号 : 99300-78-4
货号 : A847890
分子式 : C17H28ClNO2
纯度 : 99%
分子量 : 313.863
MDL号 : MFCD03658865
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(159.31 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

H2O: 100 mg/mL(318.61 mM)
动物实验配方：
生物活性
描述 Venlafaxine hydrochloride is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. 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]. 40 mg/kg of VLX (Venlafaxine) treatment has a potent relieving effect against oxaliplatin-induced neuropathic pain, and α₂-adrenergic receptor, and both α₂-adrenergic and 5-HT₃ receptors are involved in this effect of VLX on cold and mechanical allodynia, respectively[4]. Co-administration of venlafaxine (40 mg/kg) with morphine not only inhibited the naloxone-precipitated withdrawal signs including jumping and weight loss, but also reduced the up-regulation of TNF-α, IL-1β, IL-6, NO and MDA contents in mice brain tissue[5]. Venlafaxine treatment (10 mg) may improve the depression-like behaviors and decrease over-expression of S100B protein and mRNA in the hippocampus in a rat model of depression[6].
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
NCT00084669 Breast Cancer ... 展开 >> Hot Flashes Sleep Disorders 收起 << Not Applicable Completed - United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Dana-Farber/Harvard Cancer Center at Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115-6084 收起 <<
NCT00316160 Depressive Disorder, Major ... 展开 >> Major Depressive Disorder (MDD) 收起 << Phase 4 Completed - -
NCT00043550 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.93mL

3.19mL

1.59mL

31.86mL

6.37mL

3.19mL
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]Li D, Lee JH, Choi CW, Kim J, Kim SK, Kim W. The Analgesic Effect of Venlafaxine and Its Mechanism on Oxaliplatin-Induced Neuropathic Pain in Mice. Int J Mol Sci. 2019 Apr 3;20(7):1652

[5]Mansouri MT, Naghizadeh B, Ghorbanzadeh B, Amirgholami N, Houshmand G, Alboghobeish S. Venlafaxine inhibits naloxone-precipitated morphine withdrawal symptoms: Role of inflammatory cytokines and nitric oxide. Metab Brain Dis. 2020 Feb;35(2):305-313

[6]Wang CH, Gu JY, Zhang XL, Dong J, Yang J, Zhang YL, Ning QF, Shan XW, Li Y. Venlafaxine ameliorates the depression-like behaviors and hippocampal S100B expression in a rat depression model. Behav Brain Funct. 2016 Dec 8;12(1):34