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Varenicline

伐尼克蘭

Mechanism of action:

Varenicline 是一種部分促效型菸鹼型乙醯膽鹼受體促效劑（partial nicotinic acetylcholine receptor agonist）。Varenicline 能部分促效中樞神經系統中的 α4β2 菸鹼型乙醯膽鹼受體（nicotinic acetylcholine receptor），促使多巴胺（dopamine）少量釋放，減少尼古丁戒斷引起的焦躁、煩躁、注意力下降。

​Reference(s):

1. Jorenby DE et al. (2006). Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 


2. Mihalak KB et al. (2006). Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 


3. Obach RS et al. (2006). Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos.

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