Doxepin hydrochloride 是一种具有口服活性的三环抗抑郁剂。Doxepin hydrochloride 是一种有效的选择性组胺受体H1拮抗剂。Doxepin hydrochloride 也是一种有效的CYP450抑制剂,并显着抑制CYP450 2C19和CYP450 1A2。Doxepin是作为三环类抗抑郁药,可抑制血清素和去甲肾上腺素的再摄取。Doxepin对特应性皮炎、慢性荨麻疹有治疗作用,能改善认知过程,保护中枢神经系统。Doxepin也被认为是抗氧化应激的保护因子。
生物活性 | Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selectivehistamine receptorH1antagonist. Doxepin hydrochloride is also a potentCYP450inhibitor and significantly inhibitsCYP450 2C19and1A2[1][2].
Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclicantidepressant[3]..
Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system[4]..
Doxepin has also been proposed as a protective factor against oxidative stress[5].. |
体外研究 (In Vitro) | The protective effect of doxepin is associated with the enhancement of PSD-95 and synapsin 1 expression via PI3K/AKT/mTOR signaling pathway[6]..
Western Blot Analysis Cell Line: | SH-SY5Y human neuroblastoma cell line | Concentration: | 10 ng/ml | Incubation Time: | 2 h | Result: | Improved the protein expre-ssion levels of PSD-95, synapsin 1 and p-AKT in SH-SY5Y cells, and decreased the protein expression level of p-mTOR in SH-SY5Y cells. |
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体内研究 (In Vivo) | Doxepin (intraperitoneal injection of 1 mg/kg and 5 mg/kg doxepin once a day for 21 days) can protect against the Aβ1-42-induced memory impairment in rats[6]..
Animal Model: | SD male rats[6]. | Dosage: | 1, 5mg/kg | Administration: | Doxepin (intraperitoneal injection of 1 mg/kg and 5 mg/kg doxepin once a day for 21 days) | Result: | Improved the protein expression levels of PSD-95 and synapsin 1 in hippocampus and tem-poral lobe, and decreased the protein expression level of p-AKT in hippocampus and temporal lobe after treatment of 1 mg/kg of doxepin. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(316.62 mM) H2O : ≥ 50 mg/mL(158.31 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.1662 mL | 15.8308 mL | 31.6616 mL | 5 mM | 0.6332 mL | 3.1662 mL | 6.3323 mL | 10 mM | 0.3166 mL | 1.5831 mL | 3.1662 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 140 mg/mL (443.26 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.92 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.92 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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