Opioids are incredibly effective in relieving even the most severe pain, but their addictiveness and death toll call for a safer way to treat pain. In 2016 alone, more than 60,000 Americans died from overdoses, more than the number of Americans who died in the Vietnam War.
New research from the University of North Carolina School of Medicine has brought scientists one step closer to developing non-addictive opioids. The study led by Bryan Roth, a pharmacologist, examined the kappa opioid receptor (KOR), a receptor protein that interacts with opioids in the brain.
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Most opioids bind to the opioid receptors on the surface of the cells, one of the primary reasons why they’re so effective in alleviating pain but cause a range of side effects from nausea to constipation to death by respiratory depression.
“To create better opioids, we need to know the structure of their receptors,” Roth said. “Until recently, this was impossible. But now we know the structure of the activated kappa opioid receptor.”
Researchers in Roth’s lab were able to use the KOR structure to synthesize a drug-like compound that only binds to the KORs.
“Tens of thousands of people who take opioids die every year, and so we need safer and more effective drugs for treating pain and related conditions,” Roth said. “One of the big ideas is to target KORs because the few drugs that bind to it don’t lead to addiction or cause death due to overdose.”
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However, the drugs that do bind to KORs still produce unpleasant side effects such as hallucinations and dysphoria. Further research needs to examine how the receptor is activated so that a compound can attach to it and only relieve pain.
Although Roth’s findings present a wealth of possibility for new drug development, the drug-like compound has only been tested in cell cultures thus far, and it will likely take years for non-addictive opioid alternatives to become available.
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