Bupropion (Amfebutamone) hydrobromide 是一种口服有效，选择性的 5-羟色胺再摄取抑制剂 (SSRI)。Bupropion hydrobromide 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 hydrobromide 是一种非典型抗抑郁剂，可用于辅助戒烟的研究。
| 生物活性 | Bupropion (Amfebutamone) hydrobromide is an orally active, selectiveserotonin reuptakeinhibitor (SSRI)[1].Bupropion hydrobromide block dopamine (DA) uptake or Methamphetamine-induced DA release withIC50s of 1.76 μM and 14.2 μM, respectively[2]. Bupropion hydrobromide is an atypical antidepressant that can be used for the research of smoking cessation aid[3]. |
| IC50& Target[1][2] | DA uptake 1.76 μM (IC50) | DA release 14.2 μM (IC50) | CYP2D6 58 μM (IC50) |
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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].
Bupropion is a weak, competitive inhibitor of norepinephrine (NE) uptake into rat hypothalamic synaptosomes and of dopamine (DM) uptake into rat striatal synaptosomes, having IC50values of 6.5 μM and 3.4 μM, respectively[4].
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. |
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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[5].
| Animal Model: | Male Swiss mice weighing 20-25 g[5] | | Dosage: | 100-160 mg/kg | | Administration: | I.p. | | 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. |
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| 中文名称 | 氢溴酸安非他酮；氢溴酸安非拉酮；氢溴酸安非布他酮；氢溴酸丁氨苯丙酮； 布普品 |
| 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. |
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