| 中文名称 |
DOV-216,303 Free Base
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| 中文别名 |
1-(3,4-二氯苯基)-3-氮杂双环[3.1.0]己烷
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| 英文名称 |
DOV-216,303 Free Base
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| 英文别名 |
3-Azabicyclo[3.1.0]hexane, 1-(3,4-dichlorophenyl)-;1-(3,4-Dichloro-phenyl)-3-aza-bicyclo[3.1.0]hexane;1-(3,4-Dichlorophenyl)-3-azabicyclo[3.1.0]hexane;(-)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane;(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane;3,4-Dichlorophenyl-3-azabicyclo[3.1.0]hexane;ACMC-20mjef;AGN-PC-00054V;CTK0C8260;Dotriacontan-disaeure-dichlorid;dotriacontanedioic acid dichloride;dotricontanedioyl dichloride;DOV 216,303;racemic 1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane;DOV-216,303 Free Base;1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
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| Cas No. |
66504-40-3
|
| 分子式 |
C11H11NCl2
|
| 分子量 |
228.12
|
| 包装储存 |
Pure form -20°C 3 years;4°C 2 years
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| 详情描述 |
DOV-216,303 (Free Base) 是有效的 5-羟色胺、去甲肾上腺素、多巴胺再摄取的三重抑制剂,其对 hSERT、hNET 和 hDAT 的 IC50 值分别为 14 nM,20 nM和78 nM。在嗅球切除大鼠模型中,可增加前额皮质中单胺的释放及具有抗抑郁的作用。
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| 产品详情 |
DOV-216,303 (Free Base) 是有效的 5-羟色胺、去甲肾上腺素、多巴胺再摄取的三重抑制剂,其对 hSERT、hNET 和 hDAT 的 IC50 值分别为 14 nM,20 nM和78 nM。在嗅球切除大鼠模型中,可增加前额皮质中单胺的释放及具有抗抑郁的作用。
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| 生物活性 |
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC 50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
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| 性状 |
Oil
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| IC50 & Target[1][2] |
IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine).
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| 体内研究(In Vivo) |
Acute treatment of DOV-216,303 (20 mg/kg, i.p.) significantly increases dopamine, norepinephrine and serotonin levels in both OBX and Sham animals.
Chronic treatment with DOV 216,303 (20 mg/kg, i.p., for 17 days) increases extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increases extracellular baseline serotonin concentrations. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Pure form -20°C 3 years;4°C 2 years
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| 参考文献 |
[1]. Shao L, et al. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41.[2]. Prins J, et al. The putative antidepressant DOV 216,303, a triple reuptake inhibitor, increases monoamine release in the prefrontal cortex of olfactory bulbectomized rats. Eur J Pharmacol. 2010 May 10;633(1-3):55-61.
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| 溶解度数据 |
In Vitro: DMSO : ≥ 125 mg/mL (547.96 mM)Ethanol : 100 mg/mL (438.37 mM; Need ultrasonic)
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[1]. Shao L, et al. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41.[2]. Prins J, et al. The putative antidepressant DOV 216,303, a triple reuptake inhibitor, increases monoamine release in the prefrontal cortex of olfactory bulbectomized rats. Eur J Pharmacol. 2010 May 10;633(1-3):55-61.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。