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Encyclopedia > Vanoxerine

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 stongly 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. Basic piperazine structure Piperazine is a six-sided organic ring compound containing two opposing nitrogen atoms (see image). ... Dopamine Reuptake Inhibitors or Dopamine Uptake Inhibitors are compounds that inhibit the reuptake of the neurotransmitter dopamine after it is released and used at the synapse. ... Dopamine is a chemical naturally produced in the body. ... Reuptake is the reabsorption of a neurotransmitter by the molecular transporter of a pre-synaptic neuron after it has performed its function of transmitting a neural impulse. ... This article is about the drug Cocaine. ...

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 succesfully 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. Addiction is a compulsion to repeat a behaviour regardless of its consequences. ... Agonists An agonist is a substance that binds to a receptor and triggers a response in the cell. ... Heroin or diacetylmorphine (INN) is a semi-synthetic opioid. ... Methadone is a synthetic opioid, used medically as an analgesic and in the treatment of narcotic addiction. ...

As of 2006, Vanoxerine is in Phase 2 trials in humans.



CAS# 67469-78-7

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.



  Results from FactBites:
Laboratory of Clinical Pharmacology - Publications (237 words)
In vitro human tissue models in risk assessment: report of a consensus-building workshop.
Metabolism of vanoxerine, 1-[2-[bis(4-flurophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine by human cytochrome P450 enzymes.
Bioavailablility of penclomedine and systemic exposure to 4-O-demethylpenclomedine in patients receiving oral and intravenous penclomedine.
  More results at FactBites »



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