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Pregabalin

普瑞巴林

Mechanism of action:

Pregabalin 是一種 γ-胺基丁酸（GABA）類似物。Pregabalin 高親和力結合中樞神經系統中的電壓門控鈣離子通道（voltage-gated Ca²⁺ channels）的 α₂δ-1 與 α₂δ-2 亞基。當神經元去極化（depolarization）時，pregabalin 會降低鈣離子進入突觸前神經末梢的量，進而抑制神經傳導物質的釋放。

​Reference(s):

1. Authors unspecified et al. (2005). Schedules of controlled substances: placement of pregabalin into schedule V. Fed Regist. 


2. Su TZ et al. (2005). Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther. 


3. Li Z et al. (2011). Pregabalin is a potent and selective ligand for alpha(2)delta-1 and alpha(2)delta-2 calcium channel subunits. Eur J Pharmacol.

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