How CPP-109 and CPP-115 Work

The release of dopamine in the brain causes the "high" or exaggerated sense of pleasure associated with drug abuse. CPP-109 and CPP-115 work 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 aminotransferase (GABA–AT, also known as GABA transaminase or GABA–T). CPP-109 and CPP-115 work by inhibiting GABA-AT and consequently increasing the level of GABA, which then lowers the level of dopamine and turns off the "high."

CPP-109 works for short-term treatment without the visual field defects typically associated with chronic administration of vigabatrin. Moreover, CPP-115 may not cause visual field defects at all. Thus tar­get­ing brain GABAergic systems with drugs such as CPP-109 and CPP-115 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
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 showing how CPP-109 and CPP-115 work.
(11.4 MB file, courtesy Brookhaven National Laboratory)

CPP-115 and CPP-109

Place cursor next to bottom molecule to see animation.

Molecular model of CPP-109 courtesy Dr. Joseph W. Lauher,
SUNY Stony Brook