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编 号：F513856
分子式：C13H19BrClNO
分子量：320.65
分子式：C13H19BrClNO
分子量：320.65
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CAS No: 905818-69-1
产品详情
生物活性：
Bupropion (Amfebutamone) hydrobromide is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion hydrobromide block dopamine (DA) uptake or Methamphetamine-induced DA release with IC50s 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.
体内研究：
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.Animal Model:Male Swiss mice weighing 20-25 g
Dosage:100-160 mg/kg
Administration:I.p.
Result:Caused clonic convulsions, with the CD50 and CD97 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.
体外研究：
Bupropion (Amfebutamone) inhibits CYP2D6 with the IC50 of 58 μM.Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells.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.Bupropion (1-100 μg/mL) reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms.Bupropion (100 μg/mL) increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h.Bupropion is a weak, competitive inhibitor of norepinephrine (NE) uptake into rat hypothalamic synaptosomes and of dopamine (DM) uptake into rat striatal synaptosomes, having IC50 values of 6.5 μM and 3.4 μM, respectively.
Bupropion (Amfebutamone) hydrobromide is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion hydrobromide block dopamine (DA) uptake or Methamphetamine-induced DA release with IC50s 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.
体内研究：
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.Animal Model:Male Swiss mice weighing 20-25 g
Dosage:100-160 mg/kg
Administration:I.p.
Result:Caused clonic convulsions, with the CD50 and CD97 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.
体外研究：
Bupropion (Amfebutamone) inhibits CYP2D6 with the IC50 of 58 μM.Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells.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.Bupropion (1-100 μg/mL) reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms.Bupropion (100 μg/mL) increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h.Bupropion is a weak, competitive inhibitor of norepinephrine (NE) uptake into rat hypothalamic synaptosomes and of dopamine (DM) uptake into rat striatal synaptosomes, having IC50 values of 6.5 μM and 3.4 μM, respectively.
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