Vanoxerine

Vanoxerine (GBR12909) is a potent and selective DRI (Dopamine reuptake inhibitor).IC50 value:Target: Dopamine reuptake inhibitorAt 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.

Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter

Research Areas >> Neurological Disease

[1]. Mahmud F, et al. Reentrant excitation in an analog-digital hybrid circuit model of cardiac tissue. Chaos. 2011 Jun;21(2):023121.

[2]. Lacerda AE, et al. Vanoxerine: cellular mechanism of a new antiarrhythmic. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.

Vanoxerine dihydrochloride | Fipexide | Dasotraline (hydrochloride) | Diclofensine (hydrochloride) | GBR 12935 dihydrochloride | Levophacetoperane (hydrochloride) | SPD-473 citrate | Centanafadine Hydrochloride