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so how neurotoxic is bupropion if it is?

T9358

Bluelighter
Joined
Dec 5, 2012
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92
a study I found ---Bupropion is an atypical antidepressant that is currently used as a smoking cessation aid. Bupropion interferes with monoamine reuptake and is potentially neurotoxic, although this is yet to be confirmed. In this study, we evaluated the cytotoxicity of bupropion using SH-SY5Y human catecholaminergic cells as the in vitro model. Exposure of the cells to bupropion for 24h reduced their viability in a concentration-dependent manner. Treatment of the cells with a toxic concentration of bupropion (100μg/mL) induced the phosphorylation of eukaryotic initiation factor alpha (EIF-2α), c-JUN N-terminal kinase (JNK), and p38 mitogen-activated protein kinase (MAPK) within 1h, which later declined to baseline levels. However, bupropion failed to splice X-box binding protein 1 (XBP1) mRNA. Bupropion caused mitochondrial cytochrome c release and activated caspases 9, 8, and 3 in a time-dependent manner. The reduction in cell viability was significantly inhibited by a caspase 3 inhibitor. Bupropion also induced the mRNA expression of the death receptors DR4 (TRAILR1) and DR5 (TRAILR2). However, bupropion did not increase the level of cellular oxidative stress. Taken together, our data indicate that 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


I can understand a little of it but I know you guys can, I was suspicious as it is a halogenated substituted cathinone, I was thinking in comparison to chloro-amphetamine.
 
All it says is that high doses of buproprion kill neural cells? I don't know if it reaches 100 micrograms per mL in humans though.

This book says the therapeutic concentrations of buproprion are 0.05 to 0.1 mg/L or 0.05 to 0.1 micrograms per mL. Apparently there was a case where someone ate 23 grams of buproprion (!) and died. They had a blood level of 0.45 micrograms per mL. So the toxic levels used in the study are about a thousand times higher than seen in typical usage and are unlikely to ever occur in man.
 
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