Asc-534 Bupropion hydrochloride/盐酸安非他酮

Biological Description

Non-selective dopamine and norepinephrine transporter (DAT/NET) inhibitor (K_i values are 1.4, 2.8 and 45 μM for NET, DAT and SERT transporters respectively). Nicotinic acetylcholine receptor (nAchrs) antagonist (IC₅₀ = are 1.8 at α₂β₂ receptor). Displays anti-depressant activity.

Useful References

Dwoskin et al (2006) Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent. CNS Drug Rev. 12:178-207. abstract



Budzynska et al (2011) Effects of bupropion on the reinstatement of nicotine-induced conditioned place preference by drug priming in rats. Pharmacol Rep. 63:362-71. abstract



Damaj et al (2004) Enantioselective effects of hydroxy metabolites of bupropion on behavior and on function of monoamine transporters and nicotinic receptors. Mol Pharmacol. 66:675-82. abstract



 

Chemical Information

(±)-1-(3-Chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride

• Desiccate at RT


• MW 276.2


• Soluble in water to 100 mM


• C₁₃H₁₈ClNO.HCl


• 31677-93-7