Bupropion (Amfebutamone) hydrobromide is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion hydrobromide block dopamine (DA) uptake or Methamphetamine-induced DA release with IC 50 s of 1.76 μM and 14.2 μM, respectively. Bupropion hydrobromide is an atypical antidepressant that can be used for the research of smoking cessation aid.

Bupropion (Amfebutamone) inhibits CYP2D6 with the IC 50 of 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 IC 50 values 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.

Bupropion (Amfebutamone) shows convulsant and anticonvulsant effects in mice. Bupropion dose-dependently causes clonic convulsions in mice, with the CD 50 (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 CD 50 and CD 97 being 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.

905818-69-1

C13H19BrClNO

320.65

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;Amfebutamone hydrobromide;Bupropion hydrobromide

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years