New compound enhances the brain’s ability to generate natural painkillers.

Indiana University Researchers may have developed a new compound that could help in the fight against the opiod abuse epidemic in the United States.

Opiod dependency is a public health emergency in the US today. According to the U.S. Department of Health and Human Services, over 15,000 people died when they overdosed on prescription opiod drugs in 2015 alone.

While politicians and other policy makers are looking for ways to help those people already struggling with addiction, researchers within academia and the pharmaceutical industry are trying to develop alternatives to opiods that relieve pain but without the dependency issues.

Scientists at Indiana University recently reported encouraging results for a new positive allosteric modulator (PAM) developed at Northeastern University in mice. The compound, GAT211, was shown to enhance the ability of the brains in mice to produce natural painkillers. Compared to two other alternative pain relievers, GAT211 was found to be most likely to maintain its effectiveness over time and less likely to create addiction.

Instead of turning processes on and off, PAMs act by targeting specific receptors that amplify them. The compound developed by the IU researchers enhances the production of anandamide and 2-arachidonoylglycerol, chemicals that relieve pain by acting on the CB1 receptor in the brain. This receptor is the same receptor targeted by tetrahydrocanabinal (THC), the active ingredient in cannabis. The mice in the study, however, experienced pain relief without the other effects associated with using marijuana, including impaired motor function. Importantly, the compound also didn’t result in tolerance in the mice – which is what typically leads to dependency issues.

The IU scientists suggest that the compound is effective because it targets a limited number of receptors rather than a large number located throughout the body. “If these effects could be replicated in people, it would be a major step forward in the search for new, non-addictive forms of pain relief," said study coordinator Andrea G. Hohmann, a Neuroscience Professor at IU Bloomington.

Within the industry, companies such as Trevena, Mebias and Nektar Therapeutics are conducting clinical trials with different opiod alternatives designed to produce opioid-like pain relief without the risk of dependency and other adverse effects.