Treating postoperative and chronic inflammatory pain should now be possible without causing side effects. Doing so would substantially improve patient quality of life. (Stock image) Credit: © imacoconut / Fotolia
Researchers discover new mechanism of action. Researchers from Charité – Universitätsmedizin Berlin have discovered a new way of developing painkillers. The team of researchers used computational simulation to analyze interactions at opioid receptors. When used in an animal model, their prototype of a morphine-like molecule was able to produce substantial pain relief in inflamed tissues. However, healthy tissues remained unaffected, suggesting the severe side effects might be avoided.
“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,” explains Prof. Dr. Christoph Stein, Head of the Department of Anesthesiology and Surgical Critical Care Medicine, Campus Benjamin Franklin. In cooperation with PD Dr. Marcus Weber from Zuse Institute Berlin, and with the help of innovative computational simulations, they were able to analyze morphine-like molecules and their interactions with opioid receptors. They were able to successfully identify a new mechanism of action, which is capable of producing pain relief only in the desired target tissues – those affected by inflammation.
Treating postoperative and chronic inflammatory pain should now be possible without causing side effects. Doing so would substantially improve patient quality of life. Dr. Viola Spahn and Dr. Giovanna Del Vecchio, explain: “In contrast to conventional opioids, our NFEPP-prototype appears to only bind to, and activate, opioid receptors in an acidic environment. This means it produces pain relief only in injured tissues, and without causing respiratory depression, drowsiness, the risk of dependency, or constipation.” After designing and synthesizing the drug prototype, the researchers subjected it to experimental testing. Using computer modeling, they simulated an increased concentration of protons, thereby mimicking the acidic conditions found in inflamed tissues. “We were able to show that the protonation of drugs is a key requirement for the activation of opioid receptors,” conclude the authors. Their findings, which may also apply to other types of pain, may even find application in other areas of receptor research. Thereby, the benefits of improved drug efficacy and tolerability are not limited to painkillers, but may include other drugs as well.
https://www.charite.de/en/service/press_reports/artikel/detail/painkillers_without_dangerous_side_effects/
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