Novel Compound Halts Cocaine Addiction, Researchers Say

Novel Compound Halts Cocaine Addiction, Researchers Say

Novel Compound Halts Cocaine Addiction, Researchers Say

Novel Compound Halts Cocaine Addiction, Researchers SayCocaine is a stimulant drug with a well-established potential to produce the long-term changes in brain function associated with physical dependence and addiction. Currently, the scientific/medical community has no proven or reliable medication-based option for treating people addicted to this powerful drug. In a study published in April 2014 in the journal Neuropsychopharmacology, a team of U.S. and Chinese researchers explored the potential usefulness of a newly developed compound, known only as RO5263397, in helping address the effects of cocaine addiction. The researchers concluded that, in preliminary animal testing, this compound produced clearly beneficial results.

Potential Treatments

Medications are available for the treatment of a number of forms of substance addiction, including opioid addiction, alcoholism and nicotine addiction. The National Institute on Drug Abuse reports that several treatments used to address the effects of these addictions (including the alcoholism medication disulfiram) are under consideration as potential options to help people addicted to cocaine. Other options under consideration include the sleep apnea medication modafinil, the anti-seizure medications topiramate and tiagabine, and a cocaine vaccine that preemptively inoculates people from the mind-altering effects of cocaine use. Some of the approaches under development show genuine promise as options for easing at least some of the effects of cocaine addiction (including such things as ongoing cravings and a craving-related risk for a relapse back into drug use during recovery). However, no medication has provided enough of a consistent benefit to qualify as an approved cocaine addiction treatment.


In order to produce their drug effects, cocaine and other substances of abuse must first find a way to enter the brain. As a rule, this access is provided by sites (called receptors) located on nerve cells in the central nervous system (brain and spinal cord). Researchers have known for some time that it’s possible to deny some drugs access to the brain by preventing them from reaching the necessary receptor sites. In fact, certain medications already in use for the treatment of other forms of addiction rely on this blocking effect to produce their benefits. According to researchers from the State University of New York at Buffalo, the compound RO5263397 may play a useful role in the treatment of cocaine addiction because it specifically targets and blocks a receptor in the brain that helps cocaine users experience intake of the drug as a rewarding or pleasurable activity.

Does It Work?

In the study published in Neuropsychopharmacology, researchers from SUNY Buffalo, the College of Charleston, Research Triangle International and China’s Tianjin Medical University used laboratory experiments on rats to explore the potential effectiveness of RO5263397 in cocaine addiction treatment. Specifically, the researchers looked at whether use of the compound could interfere with the tendency of cocaine-exposed rats to return repeatedly to the environments in which they have received doses of the drug in the past. Broadly speaking, this repetitive behavior mimics the human tendency to establish drug cravings after recurring exposure to a substance that produces rewarding or pleasurable effects inside the brain.

When the researchers gave RO5263397 to a group of cocaine-accustomed rats, these rats largely stopped exhibiting the repetitive behavior associated with cocaine use. The researchers interpreted this change in behavior as a sign that RO5263397 blocks the rewarding effects of cocaine inside the brain. When given to rats that had previously had their access to cocaine terminated, the compound substantially reduced the tendency of these animals to relapse back into cocaine use when the drug again became available. In addition, the researchers gauged the impact of RO5263397 on how much effort rats were willing to expend to restore their access to cocaine; they concluded that rats treated with the compound significantly reduce their efforts to acquire the drug.

First-Ever Research

The authors of the study published in Neuropsychopharmacology believe they are the first researchers to thoroughly demonstrate the potential usefulness of RO5263397 as a treatment option for cocaine addiction. The authors of the study do not address the issue of human trials, and no one can really say when RO5263397 or a similar treatment might become available to humans.

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