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Vanoxerine is an investigational dopamine transporter antagonist suggested to be beneficial in the treatment of cocaine addiction. It was synthesized in the late 1970s and developed as a potential treatment for depression.
- Mechanism
- Curator reviewed · 8 references
Vanoxerine is a highly selective dopamine transporter antagonist. Due to its ability to inhibit dopamine reuptake, it has been suggested that vanoxerine may be beneficial in treating cocaine addiction. Cocaine increases the amount of dopamine in the synapse by attaching and blocking the dopamine transporter. Compared to cocaine, vanoxerine has a higher affinity for the dopamine transporter and a slower dissociation rate, without the stimulant profile of cocaine. The use of vanoxerine to treat conditions characterized by low levels of dopamine, such as Parkinson's disease and depression, has also been investigated.
Vanoxerine is also a potent blocker of the hKV11.1 (hERG) cardiac potassium channel. Even at low concentrations, vanoxerine is capable of blocking calcium and sodium currents without having a significant effect on QT interval, action potential waveforms and transmural dispersion of repolarization. Because of this, the anti-arrhythmic and anti-atrial fibrillatory properties of vanoxerine have been investigated.
- Primary indication
- Vanoxerine has not been approved for therapeutic use.Curator reviewed
- Formula / weight
- C28H32F2N2O · 450.574 g/mol (avg)
- Code names
- GBR-12909
Resolves to
NAUWTFJOPJWYOT-UHFFFAOYSA-NSMILESFC1=CC=C(C=C1)C(OCCN1CCN(CCCC2=CC=CC=C2)CC1)C1=CC=C(F)C=C1What you can answer from here — as of September 12, 2026
Which drugs share a target with Vanoxerine, and which of those have an active Phase 3 trial?