Cocaine Antidote Closer to Reality With Latest Research Breakthrough

By Victoria Kim 01/16/15

Though a potential aid in treating cocaine addiction is on the horizon, don't expect a miracle drug anytime soon.

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A recent discovery made by researchers from the University of Copenhagen could lead to a cocaine vaccine that would facilitate recovery from addiction to the stimulant and similar drugs.

The Danish study, published in the Journal of Biological Chemistry, revealed a better understanding of the biological mechanism behind cocaine’s euphoric effect, and could help in the development of future medical treatment against cocaine addiction.

There has yet been little detailed information about the ways in which dopamine or cocaine interact with the dopamine transporter protein.The researchers gained new insight into the mechanism behind the dopamine transporter.

“If we have a better understanding of the dopamine transporter function we will become more proficient in developing an antidote against addiction,” said Claus Juul Loland, associate professor in the Department of Neuroscience and Pharmacology at the University of Copenhagen.

The dopamine transporter facilitates regulation of the dopamine signal, controlling access of dopamine. It removes dopamine from the synaptic cleft and deposits it into surrounding cells, thus terminating the dopamine signal. When taken, cocaine blocks the normal role of the dopamine transporter in terminating dopamine signaling through molecular interactions that are only partially understood.

The researchers discovered an interaction, or “gate,” that controls access of dopamine, the hormone which signals pleasure in our brains, inside the dopamine transporter.

“We found two amino acids in the proteins that dynamically breaks and forms an interaction,” said Loland.

Besides controlling function, the sequence of the two amino acids is important for the overall structure of the dopamine transporter. “The breakage of the interaction could therefore be a signature for the binding of cocaine and cocaine-like drugs,” said Loland.

Cocaine acts as an inhibitor of the dopamine transporter, but the researchers found other inhibitors that, despite binding to the dopamine transporter with the same strength as cocaine, did not produce the same stimulatory response when administered to rats.

Understanding why the inhibitors are different could lead to the development of non-stimulatory inhibitors that could stop the binding of cocaine and produce an antidote, thus preventing the body from stimulating a response to the drug. The inhibitor would occupy the cocaine binding site without the stimulating action of cocaine.

The antidote, which would also work on similar drugs like amphetamine, would have to be taken regularly, having to be replenished, Loland explained.

“Our objective here is that cocaine will not then work anymore as the antidote will inhibit the stimulatory response of taking the drug,” said Loland.

The antidote is not a cure-all, however, and would be used to supplement drug treatment, similar to how methadone works for heroin addicts. “The drug is not a wonder drug,” Loland told Medical Daily. “It would aid in the treatment of cocaine addiction, but the patient would have to be willing to go into rehab and other actions have to be taken in addition to this.”

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