Treating postoperative and chronic inflammatory pain should now be possible without causing side effects. Doing so would substantially improve patient quality of life. The study's first authors, 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, the researchers 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.
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