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Vanoxerine chemical structure
| CAS number |
| ATC code |
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| DrugBank |
|Molecular weight||450.563 g/mol (freebase); 523.494 g/mol (dihydrochloride)|
|Elimination half-life||6 hours approx|
|Legal status||Investigational New Medicine|
|Routes of administration|
Vanoxerine, also known as GBR-12909, is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. GBR-12909 binds to the target site on the dopamine reuptake transporter around 500 times more strongly than cocaine, but has only mild stimulant effects, because as well as inhibiting the reuptake of dopamine, GBR-12909 inhibits dopamine release, and so produces only a slight elevation of dopamine levels.
Vanoxerine has been researched for use in treating cocaine addiction both as a substitute for cocaine and to block the rewarding effects. This strategy of using a competing agonist with a longer half-life has been successfully used to treat addiction to opiates such as heroin by substituting with methadone. It is hoped that vanoxerine will be of similar use in treating cocaine addiction.
As of 2006, vanoxerine is in Phase 2 trials in humans.
- A tolerance study of single and multiple dosing of the selective dopamine uptake inhibitor GBR 12909 in healthy subjects, by Sogaard U, Michalow J, Butler B, Lund Laursen A, Ingersen SH, Skrumsager BK, Rafaelsen OJ. Department of Psychiatry, Copenhagen University Hospital, Rigshospitalet, Denmark. Int. Clin. Psychopharmacol. 1990 Oct; 5(4):237-51
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