| Bioactivity | Bupropion (Amfebutamone) hydrobromide is an orally active, selective serotonin reuptake inhibitor (SSRI)[1].Bupropion hydrobromide block dopamine (DA) uptake or Methamphetamine-induced DA release with IC50s of 1.76 μM and 14.2 μM, respectively[2]. Bupropion hydrobromide is an atypical antidepressant that can be used for the research of smoking cessation aid[3]. |
| Invitro | 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].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[4]. Cell Viability Assay[3] Cell Line: |
| 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[5]. Animal Model: |
| Name | Bupropion hydrobromide |
| CAS | 905818-69-1 |
| Formula | C13H19BrClNO |
| Molar Mass | 320.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. C Lindsay DeVane. Antidepressant-drug interactions are potentially but rarely clinically significant. Neuropsychopharmacology. 2006 Aug;31(8):1594-604; discussion 1614-5. [2]. Linda D Simmler, et al. Bupropion, methylphenidate, and 3,4-methylenedioxypyrovalerone antagonize methamphetamine-induced efflux of dopamine according to their potencies as dopamine uptake inhibitors: implications for the treatment of methamphetamine depe [3]. Eun-Hee Jang, et al. Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells. Toxicology. 2011 Jul 11;285(1-2):1-7. [4]. Dr. R. M. Ferris, et al. Some neurochemical properties of a new antidepressant, bupropion hydrochloride (Wellbutrin™). Drug Development Research. 1981,1(1): 21-35. [5]. Piotr Tutka, et al. Convulsant and anticonvulsant effects of bupropion in mice. Eur J Pharmacol. 2004 Sep 19;499(1-2):117-20. |