Anti-addiction medication

Drug addiction continues to plague vast numbers of people across the world, destroying and ending lives, while attempts to develop more effective pharmaceutical addiction treatments continue.
Vigabatrin is an anti-epilepsy medication approved by the Food and Drug Administration that has also been shown to be effective against addiction to cocaine, nicotine, methamphetamine, heroin and alcohol in animal models.

In humans, vigabatrin eliminates cocaine addiction in 28 percent of patients. It works by blocking an enzyme-aminobutyric acid (GABA) aminotransferase, which breaks down GABA. The result is higher levels of this neurotransmitter in the brain and diminished narcotic-activated release of dopamine. Long-term vigabatrin therapy can have serious side effects however, causing eye damage in up to 40 percent of those treated.

In previous work, the researchers designed a compound, CPP-115, that is 186 times more efficient in inactivating GABA aminotransferase than vigabatrin. In this study, they used computational molecular dynamics simulations of CPP-115 in complex with the enzyme to develop a new and improved agent with 10 times greater efficiency.

The drug should also be less likely to cause side effects, as it has fewer off-target activities in in vitro tests. In initial rat experiments, the new compound was far better at blocking dopamine release after a cocaine or nicotine stimulus than CPP-115.
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Activating brain region creates desire for cocaine

Researchers have identified a part of the brain that intensifies desire for rewards like addiction to cocaine. Activating part of the amygdala, an almond-shaped brain region, intensifies motivation to consume cocaine far beyond ordinary drug levels, similar to its ability to intensify motivation for sweet foods like sugar.

Amygdala plays a key role in drug addiction. For addicts, drugs become so attractive as to cause intense motivation focused entirely on obtaining drugs at the expense of other normal life enjoyment. Researchers implanted rats with a catheter that allowed them to earn doses of cocaine, activating brain region creates intense desire to use cocaine.

Researchers implanted rats with a catheter that allowed them to earn doses of cocaine by poking their noses into small holes in the wall. Whenever rats would poke their nose into one particular hole to earn intravenous cocaine, a laser light would also activate the neurons in the central amygdala at the same time

Poking their nose into a different hole earned identical cocaine, but never activated the amygdala. Rats focused only on the port that earned cocaine together with amygdala-activating laser, consumed much more cocaine than rats without amygdala activation, and avidly nibbled around the laser-cocaine hole for more.

The amygdala activation intensified motivation when cocaine was also present. By contrast, when the researchers temporarily inactivated the amygdala using a painless drug infusion, rats completely stopped responding for cocaine.
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