Bupropion is an inhibitor of the reuptake of dopamine and norepinephrine (IC50 = 6.5 and 3.4 μM, respectively). It is also an antagonist of neuronal acetylcholine nicotinic receptors (nAChR), blocking α3β2 better than α4β2 and α7 (IC50 = 1.3, 8, and 60 μM, respectively). As a dual inhibitor of dopamine and norepinephrine reuptake, bupropion is efficacious as an antidepressant. Because of its effects on nicotinic receptors, it is also used to promote smoking cessation.
