Bupropion  (Synonyms: 安非他酮; Amfebutamone)

Bupropion (Amfebutamone) is an orally active, selective serotonin reuptake inhibitor (SSRI).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].

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].

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^[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].

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

239.74

C₁₃H₁₈ClNO

34911-55-2

安非他酮；安非布他酮；丁氨苯丙酮

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 depe  [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]. 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]

  [5]. Moreira, R., The efficacy and tolerability of bupropion in the treatment of major depressive disorder. Clin Drug Investig, 2011. 31 Suppl 1: p. 5-17.  [Content Brief]