How CPP-109 Works

The release of dopamine in the brain causes the "high" or exaggerated sense of pleasure associated with drug abuse. CPP-109 works by indirectly lowering the level of dopamine in the brain. Specifically, GABA — gamma-aminobutyric acid — is a neurotransmitter in the brain that inhibits the release of dopamine. GABA, however, is broken down by GABA transaminase (GABA-T). CPP-109 works by inhibiting GABA-T and consequently increasing the level of GABA, which then lowers the level of dopamine and turns off the "high."

CPP-109 works without the apparent side effects typically associated with GABA agonists. Thus targeting brain GABAergic systems with drugs such as CPP-109 is a potentially effective treatment for cocaine, methamphetamine and other substance dependencies.

 
Composite brain scans of six baboons
showing effect of CPP-109 on cocaine use
courtesy Brookhaven National Laboratory
normal dopaminehigh dopamine level after cocainenear normal dopamine level after cocaine and CPP-109
Baseline:
dopamine levels
normal		After cocaine:
dopamine levels
very high		After CPP-109
and cocaine: dopamine
levels near normal
 

Read a pilot study on vigabatrin and ocular safety.

See an animation of how CPP-109 works. (11.4 MB file, courtesy Brookhaven National Laboratory)