General description
一种有效的选择性的多巴胺再摄取(DRI)抑制剂。
Vanoxerine 2 Hcl(GBR12909) is a potent and selective DRI (Dopamine reuptake inhibitor). IC50 value: 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. 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.
Vanoxerine 2 Hcl(GBR12909)是一种有效的选择性DRI(多巴胺再摄取抑制剂)。 IC50值:目标:多巴胺再摄取抑制剂在细胞水平上,vanoxerine起到阻断心脏离子通道的作用。 Vanoxerine是一种多通道阻滞剂,作用于IKr(钾),L型钙和钠离子通道。 通过阻断这些特定的通道,延长了细胞的动作电位,从而防止了折返电路的重新激活。 阻断与频率密切相关:随着心脏起搏的增加,香草醛对离子通道的阻断频率也随之增加。 Vanoxerine是治疗心律不齐的潜在有效方法。 心脏心律不齐的一个重要原因是折返,这是一种电生理事件,其中的增殖信号拒绝终止,并在不应期后持续使心脏兴奋。
Properties
Iupac Name: | 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline dihydrochloride |
Inchi Code | 1S/C13H13N3.2ClH/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;;/h1-2,4-5,8-9,14H,3,6-7H2;2*1H |
Inchi Key | NZVVYNGXLGJKCW-UHFFFAOYSA-N |
安全信息