Molecule blocks opioid receptors in brain

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Researchers at the Department of Infection and Immunity of the Luxembourg Institute of Health (LIH) recently developed a molecule that binds to and blocks a previously unknown opioid receptor in the brain.

The molecule, LIH383, modulates the levels of opioid peptides produced in the central nervous system and enhancing their natural painkilling and antidepressant properties.

Opioid peptides help to mediate pain relief and emotions, such as euphoria, anxiety, stress, and depression.

LIH383 increases the availability of opioid peptides that bind to classical opioid receptors in the brain by targeting and blocking the atypical chemokine receptor ACKR3.

ACKR3 is a new opioid receptor with negative regulatory properties, especially with the enkephalin, nociceptin, and dynorphin families. The interaction does not generate the typical pain-relief or tranquilizing messages typically found with classical opioid receptors.

“This is a glaring example of the way fundamental research can be translated into concrete applications with tangible benefits for patients, leading to improved clinical outcomes,” said study co-author Markus Ollert, director of the LIH Department of Infection and Immunity.

Prescription opioids target and activate opioid receptors to produce painkilling effects. Researchers are seeking to find new methods of producing painkilling results without the harmful effects of opioid use, such as respiratory disorders, dependence, and tolerance.

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