Bupropion hydrobromide  (Synonyms: Amfebutamone hydrobromide)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

320.65

C₁₃H₁₉BrClNO

905818-69-1

CC(NC(C)(C)C)C(C1=CC=CC(Cl)=C1)=O.[H]Br

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. C Lindsay DeVane. Antidepressant-drug interactions are potentially but rarely clinically significant. Neuropsychopharmacology. 2006 Aug;31(8):1594-604; discussion 1614-5.  [Content Brief]

  [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 dependence. BMC Res Notes. 2013 Jun 5;6:220.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]