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The Sound of Evolution
Procainamide
普魯卡因胺
Mechanism of action:
Procainamide 是一種 class IA 鈉離子通道阻斷劑（class IA sodium channel blocker）。Procainamide 會結合心肌細胞膜上的電壓門控鈉離子通道（voltage-gated Na⁺ channel），降低第 0 期（phase 0）去極化速率，使心肌傳導速度變慢，尤其影響心房、心室與浦金耶纖維（Purkinje fiber）。除了鈉離子通道阻斷外，procainamide 亦會抑制部分鉀離子外流（K⁺ currents），導致動作電位時間延長、有效不反應期延長。
Reference(s):
1. Chiu PJ et al. (2004). Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci.
2. Tobita M et al. (2005). A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. Bioorg Med Chem Lett.
3. Liu T et al. (2025). BindingDB in 2024: a FAIR knowledgebase of protein-small molecule binding data. Nucleic Acids Res.
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