Venlafaxine hydrochloride是一种具有口服活性的5-羟色胺和去甲肾上腺素再摄取抑制剂 （SNRIs; Serotonin-norepinephrine reuptake inhibitors），对配体与人NE和5-HT转运蛋白结合的Ki值分别为2480nM和82nM。
Cas No.:99300-78-4
Sample solution is provided at 25 µL, 10mM.
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Venlafaxine hydrochloride is an orally active serotonin-norepinephrine reuptake inhibitor (SNRIs) with Ki values of 2480nM and 82nM for ligand binding to human NE and 5-HT transporters, respectively[1]. Venlafaxine hydrochloride has been used clinically as an antidepressant[2-3].
In vitro, treatment of BV-2 cells with Venlafaxine hydrochloride (0.01-1mM) for 24 hours showed mild survival impairment only at high non-physiological concentrations (1mM), with no cytotoxicity at other concentrations, and only slightly inhibited nitric oxide (NO) production in BV-2 cells stimulated by LPS (1μg/ml) [4]. Treatment of human colon cancer cells (HCT116 and SW480) with Venlafaxine hydrochloride (10μM) for 24-72 hours antagonized the effect of NE by inhibiting NET expression, thereby inhibiting the progression of colon cancer[5].
In vivo, Venlafaxine hydrochloride (1mg/100g; 2mg/ml; 28 days; i.p.) in a SD rat depression model increased the expression level of BDNF in the rat hippocampus by affecting the PI3k/PKB/eNOS pathway, repaired the damaged pyramidal cell layer of the hippocampus, and effectively improved the behavioral ability of depressed rats[6]. Venlafaxine hydrochloride (40-60mg/kg; 1-3h; i.p.) effectively relieved neuropathic pain induced by Oxaliplatin injection in mice by activating spinal cord α2-adrenergic receptors[7].
References:
[1]. Bymaster F P, Dreshfield-Ahmad L J, Threlkeld P G, 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[J]. Neuropsychopharmacology, 2001, 25(6): 871-880.
[2]. Schweizer E, Thielen R J, Frazer A. Venlafaxine: a novel antidepressant compound[J]. Expert opinion on investigational drugs, 1997, 6(1): 65-78.
[3]. Daiss J O, Burschka C, Mills J S, et al. Sila-venlafaxine, a sila-analogue of the serotonin/noradrenaline reuptake inhibitor venlafaxine: synthesis, crystal structure analysis, and pharmacological characterization[J]. Organometallics, 2006, 25(5): 1188-1198.
[4]. Dubovický M, Császár E, Melicherčíková K, et al. Modulation of microglial function by the antidepressant drug venlafaxine[J]. Interdisciplinary toxicology, 2014, 7(4): 201-207.
[5]. Zhang H, Han J, Zhang J, et al. Venlafaxine antagonizes the noradrenaline-promoted colon cancer progression by inhibiting the norepinephrine transporter[J]. Cell death discovery, 2023, 9(1): 152.
[6]. Huang X, Mao Y S, Li C, et al. Venlafaxine inhibits apoptosis of hippocampal neurons by up-regulating brain-derived neurotrophic factor in a rat depression model[J]. Die Pharmazie-An International Journal of Pharmaceutical Sciences, 2014, 69(12): 909-916.
[7]. Li D, Lee J H, Choi C W, et al. The analgesic effect of venlafaxine and its mechanism on oxaliplatin-induced neuropathic pain in mice[J]. International Journal of Molecular Sciences, 2019, 20(7): 1652.
Venlafaxine hydrochloride是一种具有口服活性的5-羟色胺和去甲肾上腺素再摄取抑制剂 （SNRIs; Serotonin-norepinephrine reuptake inhibitors），对配体与人NE和5-HT转运蛋白结合的Ki值分别为2480nM和82nM[1]。Venlafaxine hydrochloride已作为临床抗抑郁药物进行使用[2-3]。
在体外，Venlafaxine hydrochloride（0.01-1mM）处理BV-2细胞24小时，仅在高非生理浓度（1mM）下观察到轻度存活损伤，其余浓度没有细胞毒性，且仅对LPS（1μg/ml）刺激BV-2细胞产生的一氧化氮（NO）产生轻微抑制作用[4]。Venlafaxine hydrochloride（10μM）处理人结肠癌细胞（HCT116和SW480）24-72小时，通过抑制NET表达拮抗NE的作用，抑制结肠癌的进展[5]。
在体内，Venlafaxine hydrochloride（1mg/100g; 2mg/ml; 28 days; i.p.）处理SD大鼠抑郁模型，通过影响PI3k/PKB/eNOS通路提高了大鼠海马中BDNF的表达水平，修复了受损的海马体锥体细胞层，有效改善了抑郁大鼠的行为能力[6]。Venlafaxine hydrochloride（40-60mg/kg; 1-3h; i.p.）通过激活脊髓α2-肾上腺素能受体有效缓解了小鼠因注射Oxaliplatin引起的神经性疼痛[7]。
| Cell experiment [1]: | |
Cell lines | BV-2 |
Preparation Method | The immortalized mouse microglial cell line BV-2 was cultured in DMEM, supplemented with 10% FBS, and 1% P/S (100U/ml penicillin, 100µg/ml streptomycin) and maintained in 5% CO2 at 37℃. Cells were used for 10 passages at maximum. The stock solution of Venlafaxine hydrochloride was prepared in distilled water. The inflammogen was added to the cells in the presence of the compound tested or of a vehicle. |
Reaction Conditions | 0.01-1mM; 24h |
Applications | Venlafaxine hydrochloride caused mild survival impairment at high concentrations (1mM), while other concentrations showed no cytotoxicity and only slightly inhibited nitric oxide (NO) production in BV-2 cells stimulated by LPS (1μg/ml). |
| Animal experiment [2]: | |
Animal models | SD rats |
Preparation Method | The animals were equally assigned to a normal control(NC)group, a depression modeled group and a venlafaxine-treatment group. Animals in NC group did not receive any stimulation, and the remaining animals received any one of the following stimulations randomly daily for 28 days: swimming in ice cold water (4℃) for 5min, swimming in hot water (48℃) for 5min, starvation for 48h, restraint from food and water for 24h, day-night reversal for 24h, clamping the tail and shaking for 2min, and electric shock of the sole at 1mA for 10s at a 1-min interval x 30. The same stimulation would not be used consecutively. Behaviors of the animals were evaluated at the end of stimulation everyday. Venlafaxine hydrochloride (2mg) was dissolved in 1ml normal saline (NS). After successful establishment of the depression model as described, Venlafaxine hydrochloride(1mg/100g; 2mg/ml) was injected intraperitoneally (i.p.) to animals in venlafaxine group 30min before initiation of the stimulation at 7:30. The same amount of NS was injected i.p. to animals in depression group, both for 28 days. |
Dosage form | 1mg/100g; 2mg/ml; 28 days; i.p. |
Applications | Venlafaxine hydrochloride treatment of an SD rat depression model increased BDNF expression in the hippocampus by affecting the PI3k/PKB/eNOS pathway, repaired damaged hippocampal pyramidal cell layers, and effectively improved the behavioral abilities of depressed rats. |
References: | |
| Cas No. | 99300-78-4 | SDF | |
| 别名 | 盐酸文拉法辛; Wy 45030 hydrochloride | ||
| 化学名 | 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol;hydrochloride | ||
| Canonical SMILES | CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl | ||
| 分子式 | C17H27NO2.HCl | 分子量 | 313.86 |
| 溶解度 | ≥ 15.693mg/mL in DMSO, ≥ 13.47 mg/mL in EtOH, ≥ 79 mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1861 mL | 15.9307 mL | 31.8613 mL |
| 5 mM | 637.2 μL | 3.1861 mL | 6.3723 mL |
| 10 mM | 318.6 μL | 1.5931 mL | 3.1861 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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- Purity: >99.50% Appearance: A solid
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