Bupropion

Bupropion (Amfebutamone) is an orally active, norepinephrine-dopamine reuptake inhibitor (NDRI). 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]. In Vitro:Bupropion (Amfebutamone) inhibits CYP2D6 with the IC₅₀ 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]. 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. 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.) dose-dependently increases the concentration of free dopamine and its metabolite homovanillic acid in the mouse brain^[5].