Vanoxerine

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Vanoxerine
Systematic (IUPAC) name
1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine
Identifiers
CAS number 67469-78-7
ATC code  ?
PubChem 3455
Chemical data
Formula  ?
Mol. mass 450.563 g/mol (freebase); 523.494 g/mol (dihydrochloride)
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 6 hours approx
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?
Legal status

Investigational New Medicine
Routes  ?

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 decanoate ester of vanoxerine, DBL-583, has also been developed, which slowly breaks down in the body and lasts for up to a month after a single injection.

DBL-583
DBL-583

  • 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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