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Prototype painkiller may be as effective as opioids, without side effects

A study has uncovered a new mechanism in opioid receptors that could lead to the development of new pain medications.

By Amy Wallace

Researchers in Germany have developed a new way of making painkillers that could lead to better medications without dangerous side effects.

The team from Charite Universitätsmedizin Berlin used computational simulation to analyze interactions of opioid receptors to create a morphine-like molecule.

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In tests using laboratory mice, the molecule substantially relieved pain in inflamed tissue without affecting surrounding healthy tissue. The findings suggest the prototype could be used to reduce or eliminate pain without severe side effects like those linked to opioid medications.

Opioids are a class of pain relieving medications used to treat pain from tissue damage and inflammation caused by surgery, nerve damage, arthritis or cancer. Side effects from opioid medications can include drowsiness, nausea, constipation and, in some cases, dependency.

Opioid addiction has grown to epidemic proportions in the United States in recent years, as well as in many other countries.

"By analyzing drug-opioid receptor interactions in damaged tissues, as opposed to healthy tissues, we were hoping to provide useful information for the design of new painkillers without harmful side effects," Dr. Christoph Stein, head of the Department of Anesthesiology and Surgical Critical Care Medicine at Charite Universitätsmedizin Berlin, said in a press release.

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The researchers identified a new pathway to produce pain relief without negative side effects by targeting medication at only the affected tissue, not healthy tissue.

"In contrast to conventional opioids, our NFEPP--prototype appears to only bind to, and activate, opioid receptors in an acidic environment," Dr. Viola Spahn and Dr. Giovanna Del Vecchio, first authors on the study, said in a press release. "This means it produces pain relief only in injured tissues, and without causing respiratory depression, drowsiness, the risk of dependency or constipation."

The study was published in Science.

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