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CAS No. : 31677-93-7
MCE 国际站:Bupropion hydrochloride
产品活性: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。
研究领域:Neuronal Signaling
作用靶点:Serotonin Transporter | Dopamine Transporter
In Vitro: Bupropion (Amfebutamone) hydrochloride inhibits CYP2D6 with the IC50 of 58 μM.
Bupropion hydrochloride, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells.
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.
Bupropion (1-100 µg/mL) hydrochloride reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms.
Bupropion (100 μg/mL) hydrochloride increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h.
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.
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. ED50 values 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.
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