Quetiapine hemifumarate 是一种5-HT受体激动剂，对人5-HT1A的pEC50值为 4.77。Quetiapine hemifumarate 是多巴胺受体 (dopamine receptor) 拮抗剂，对人D2的pIC50值为 6.33。Quetiapine hemifumarate 对人D2，HT1A，5-HT2A，5-HT2C受体具有中高等亲和力，pKi值为 7.25，5.74，7.54，5.55。具有抗抑郁和抗焦虑作用。
| 生物活性 | Quetiapine hemifumarate is a5-HT receptorsagonist with apEC50of 4.77 for human5-HT1A receptor. Quetiapine hemifumarate is adopamine receptorantagonist with apIC50of 6.33 for humanD2 receptor. Quetiapine hemifumarate has moderate to high affinity for the humanD2,HT1A,5-HT2A,5-HT2C receptorwithpKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1]. |
| IC50& Target[1] | 5-HT1AReceptor 5.74 (pKi) | 5-HT2AReceptor 7.54 (pKi) | 5-HT2CReceptor 5.55 (pKi) | 5-HT1AReceptor 4.77 (pEC50) | D2 Receptor 7.25 (pKi) | D2 Receptor 6.33 (pIC50) |
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体外研究
(In Vitro) | Quetiapine (<100 μM; 24 hours) has no significant effect on cell viabilities[2].
Quetiapine (10 μM) inhibits NO release, which increased by LPS (0.1-100 ng/mL) in concentration-dependent manner[2].
Quetiapine (10 μM) also inhibits TNF-α synthesis[2].
Cell Viability Assay[2] | Cell Line: | N9 microglial cells | | Concentration: | 0, 0.1, 1, 10, 50, and 100 μM | | Incubation Time: | 24 hours | | Result: | Had no significant effect on cell viabilities at various concentrations under 100 μM, in which significant toxicity could be observed. |
RT-PCR[2] | Cell Line: | N9 microglial cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Dramatically inhibited TNF-α synthesis. |
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体内研究
(In Vivo) | Quetiapine (10 mg/kg/day; ingested) can alleviate the recruitment and activation of microglia and promote myelin repair in Cuprizone (CPZ)-induced chronic mouse model of demyelination[1].
| Animal Model: | C57BL/6 mice[2] | | Dosage: | 10 mg/kg/day | | Administration: | Ingested | | Result: | Significantly increased in optical density of myelin basic protein (MBP) staining compared to Veh group. |
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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 : 50 mg/mL(113.24 mM;Need ultrasonic) H2O : 1.25 mg/mL(2.83 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2648 mL | 11.3240 mL | 22.6480 mL | | 5 mM | 0.4530 mL | 2.2648 mL | 4.5296 mL | | 10 mM | 0.2265 mL | 1.1324 mL | 2.2648 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.66 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.66 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.66 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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