Amfebutamone，也称为安非他酮，抑制 CYP2D6，IC50 为 58 μM[1]。安非他酮等非典型抗抑郁药会在 SH-SY5Y 细胞中引起内质网应激和依赖于 caspase 的细胞毒性 [3]。通过触发内质网应激反应和 JNK 激活，安非他酮激活 caspase 3，导致 SH-SY5Y 细胞凋亡 [3]。 1–100 µg/mL 的安非他酮会降低细胞活力。细胞凋亡途径可能是安非他酮诱导的细胞活力降低的原因[3]。一小时内，安非他酮 (100 μg/mL) 增强 JNK、p38 MAPK、EIF-2α 和 GRP78 磷酸化版本的表达 [3]。

在小鼠中，安非他酮表现出惊厥和抗惊厥特性。安非他酮引起小鼠剂量依赖性阵挛性惊厥，惊厥剂量 50（或 CD50）为 119.7 mg/kg，在该水平下 50% 的小鼠出现惊厥[4]。在体重为 22-30 g 的雄性白化小鼠中，与载体对照（以秒为单位）相比，安非他酮（10、15、20 和 40 mg/kg，腹膜内注射）剂量依赖性地减少了不动时间。在强迫游泳试验和悬尾试验中观察到安非他酮可减少不动期，ED50 值分别为 18.5 和 18 mg/kg ip。安非他酮（10、20 和 40 mg/kg，腹腔注射）以剂量依赖性方式提高小鼠大脑中高香草酸（游离多巴胺的代谢产物）的浓度 [5]。

细胞活力测定 [3]
细胞类型： SH-SY5Y 人儿茶酚胺能细胞
测试浓度： 0、1、10、50 和 100 µg/mL
孵育持续时间：24小时
实验结果：细胞活力以浓度依赖性方式急剧下降。

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蛋白质印迹分析 [3]
细胞类型： SH-SY5Y 人儿茶酚胺能细胞
测试浓度： 100 µg/mL
孵育持续时间：1、3、8、24 小时
实验结果：安非他酮 1 小时内对 p-EIF-2α 产生免疫力治疗反应性显着增加并持续3小时，表明安非他酮快速刺激PERK。 GRP78的表达轻微但显着增加并且JNK显着激活。安非他酮对 ER 应激通路的早期激活在治疗后 8 小时恢复到基础水平。

Animal/Disease Models: Male Swiss mouse, weight 20-25 grams [4]
Doses: 100-160 mg/kg
Route of Administration: IP
Experimental Results:Caused clonic convulsions, CD50 and CD97 were 119.7 (104.1-137.6) and 156.7 respectively mg/kg. When administered at the full convulsive dose of 160 mg/kg, the median latency was 6.00 minutes (3.50-8.15). Catalonic convulsions were only observed occasionally (1 in 8 mice) in groups receiving doses of 140 or 160 mg/kg.

[1]. C Lindsay DeVane. Antidepressant-drug interactions are potentially but rarely clinically significant. Neuropsychopharmacology. 2006 Aug;31(8):1594-604; discussion 1614-5.
[2]. Linda D Simmler, et al. Bupropion, methylphenidate, and 3,4-methylenedioxypyrovalerone antagonize methamphetamine-induced efflux of dopamine according to their potencies as dopamine uptake inhibitors: implications for the treatment of methamphetamine depe
[3]. Eun-Hee Jang, et al. Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells. Toxicology. 2011 Jul 11;285(1-2):1-7.
[4]. Piotr Tutka, et al. Convulsant and anticonvulsant effects of bupropion in mice. Eur J Pharmacol. 2004 Sep 19;499(1-2):117-20.
[5]. Moreira, R., The efficacy and tolerability of bupropion in the treatment of major depressive disorder. Clin Drug Investig, 2011. 31 Suppl 1: p. 5-17.

C13H18NOCL

239.74112

34911-55-2

Bupropion hydrochloride;31677-93-7;Bupropion hydrobromide;905818-69-1

CC(C(=O)C1=CC(=CC=C1)Cl)NC(C)(C)C

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。