Vanoxerine抑制剂、激动剂(CAS号67469-69-6)Vanoxerine (GBR12909)是多巴胺重吸收抑制剂(DRI)。 Vanoxerine (GBR12909) is a potent and selective DRI (Dopamine reuptake inhibitor).
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Target: Dopamine reuptake inhibitor
At a cellular level, vanoxerine acts to block cardiac ion channels. Vanoxerine is a multichannel blocker, acting on IKr (potassium), L-type calcium and sodium ion channels.[14] By blocking these specific channels, there is a prolongation of the action potential of the cell, preventing reactivation by a reentrant circuit. The block is strongly frequency dependant: as the pacing of the heart increases so does the frequency of ion channel blocking by vanoxerine. Vanoxerine is a potentially effective treatment for cardiac arrhythmias. A significant cause of cardiac arrhythmias is reentry, an electrophysiologic event in which the proliferating signal that refuses to terminate, and endures to reexcite the heart after the refractory period.