Bupropion (Amfebutamone) 是一种口服有效，选择性的 5-羟色胺再摄取抑制剂 (SSRI)。Bupropion 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 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) 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 is an atypical antidepressant of the aminoketone group. Bupropion can be used for the research of smoking cessation aid[1][2][3]. |
体外研究
(In Vitro) | Bupropion (Amfebutamone) inhibits CYP2D6 with the IC50of 58 μM[1].
Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells[3].
Bupropion 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) reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms[3].
Bupropion (100 μg/mL) 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) 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) 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.) 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 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com