Bupropion (Amfebutamone) hydrochloride is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion block dopamine (DA) uptake or Methamphetamine-induced DA release with IC 50 s of 1.76 μM and 14.2 μM, respectively. Bupropion hydrochloride is an atypical antidepressant of the aminoketone group. Bupropion hydrochloride can be used for the research of smoking cessation aid.
性状
Solid
体外研究(In Vitro)
Bupropion (Amfebutamone) hydrochloride inhibits CYP2D6 with the IC50 of 58 μM.Bupropion hydrochloride, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells.Bupropion hydrochloride 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.Bupropion (1-100 μg/mL) hydrochloride reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms.Bupropion (100 μg/mL) hydrochloride increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h. has not independently confirmed the accuracy of these methods.
体内研究(In Vivo)
Bupropion (Amfebutamone) hydrochloride shows convulsant and anticonvulsant effects in mice. Bupropion dose-dependently causes clonic convulsions in mice, with the CD 50 (convulsive dose50, i.e., the dose producing convulsions in 50% of mice) at 119.7 mg/kg.
Bupropion (10, 15, 20 and 40 mg/kg., i.p.; Male albino mice weighing between 22–30 g) hydrochloride dose-dependently decreases immobility period (in seconds) with respect to vehicle control group. ED 50 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.) hydrochloride dose-dependently increases the concentration of free dopamine and its metabolite homovanillic acid in the mouse brain.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (120.67 mM; ultrasonic and warming and heat to 80°C)H2O : 5.56 mg/mL (20.13 mM; ultrasonic and warming and heat to 80°C)