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Bupropion hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bupropion hydrochloride图片
CAS NO:31677-93-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
盐酸氨非他酮
Amfebutamone hydrochloride
产品介绍
Bupropion (Amfebutamone) hydrochloride 是一种口服有效,选择性的 5-羟色胺再摄取抑制剂 (SSRI)。Bupropion hydrochloride 阻断多巴胺 (DA) 摄取或 Methamphetamine 诱导的 DA 释放,IC50分别为 1.76 μM 和 14.2 μM。Bupropion hydrochloride 是一种非典型氨基酮类抗抑郁剂,可用于辅助戒烟的研究。
生物活性

Bupropion (Amfebutamone) hydrochloride is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion block dopamine (DA) uptake or Methamphetamine-induced DA release with IC50s of 1.76 μM and 14.2 μM, respectively. Bupropion hydrochloride is an atypical antidepressant of the aminoketone group. Bupropion hydrochloride can be used for the research of smoking cessation aid[1][2][3].

体外研究
(In Vitro)

Bupropion (Amfebutamone) hydrochloride inhibits CYP2D6 with the IC50of 58 μM[1].
Bupropion hydrochloride, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells[3].
Bupropion hydrochloride activates caspase 3 through the induction of endoplasmic reticulum stress responses and activation of JNK, and consequently induces apoptotic cell death in SH-SY5Y cells[3].
Bupropion (1-100 μg/mL) hydrochloride reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms[3].
Bupropion (100 μg/mL) hydrochloride increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h[3].

Cell Viability Assay[3]

Cell Line:SH-SY5Y human catecholaminergic cells
Concentration:0, 1, 10, 50, and 100 μg/mL
Incubation Time:24 hours
Result:Cell viability decreased significantly in a concentration-dependent manner.

Western Blot Analysis[3]

Cell Line:SH-SY5Y human catecholaminergic cells
Concentration:100 μg/mL
Incubation Time:1, 3, 8, 24 hours
Result:The immunoreactivity for p-EIF-2α increased significantly within 1 h of Bupropion treatment and was sustained for 3 h, indicating that Bupropion rapidly stimulates PERK.
Slightly but significantly increased the expression of GRP78 and markedly activated JNK. This early activation of the ER stress pathways by Bupropion returned to basal levels 8 h after treatment.
体内研究
(In Vivo)

Bupropion (Amfebutamone) hydrochloride shows convulsant and anticonvulsant effects in mice. Bupropion dose-dependently causes clonic convulsions in mice, with the CD50(convulsive dose50, i.e., the dose producing convulsions in 50% of mice) at 119.7 mg/kg[4].
Bupropion (10, 15, 20 and 40 mg/kg., i.p.; Male albino mice weighing between 22–30 g) hydrochloride dose-dependently decreases immobility period (in seconds) with respect to vehicle control group. ED50values of bupropion in reducing the immobility period was found to be 18.5 and 18 mg/kg i.p., in forced swim test and tail suspension test, respectively. Bupropion (10, 20 and 40 mg/kg., i.p.) hydrochloride dose-dependently increases the concentration of free dopamine and its metabolite homovanillic acid in the mouse brain[5].

Animal Model:Male Swiss mice weighing 20-25 g[4]
Dosage:100-160 mg/kg
Administration:IP
Result:Caused clonic convulsions, with the CD50and CD97being 119.7 (104.1-137.6) and 156.7 mg/kg, respectively.
When given at a full convulsant dose of 160 mg/kg, the median latency was 6.00 min (3.50-8.15). Tonic convulsions were observed occasionally (1 per 8 mice) only in the groups receiving 140 or 160 mg/kg.
分子量

276.20

性状

Solid

Formula

C13H19Cl2NO

CAS 号

31677-93-7

中文名称

盐酸安非他酮;盐酸安非布他酮;盐酸丁氨苯丙酮

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 : 33.33 mg/mL(120.67 mM;ultrasonic and warming and heat to 80℃)

H2O : 5.56 mg/mL(20.13 mM;ultrasonic and warming and heat to 80℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.6206 mL18.1028 mL36.2056 mL
5 mM0.7241 mL3.6206 mL7.2411 mL
10 mM0.3621 mL1.8103 mL3.6206 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 (9.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.05 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (9.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.05 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (9.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.05 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。