Scientists Have Discovered Way To Make Fentanyl Safer

Modifying fentanyl's chemical structure reduces harmful side effects while maintaining its pain-relieving properties, new research suggests.

Fentanyl is a synthetic opioid that is up to 100 times more potent than morphine and about 50 times stronger than heroin. In 2021, more than 80,000 people in the U.S. died from an opioid overdose.

In the study published in the peer-reviewed journal Nature, researchers from the University of Florida, Washington University in St. Louis, the University of Southern California, and Stanford University gained new insights into how opioid receptors work. The knowledge allowed them to generate a new, safer medicine.

Fentanyl works by binding to the mu-opioid receptor on nerve cells. The interaction triggers pain relief but can also cause serious side effects, such as respiratory distress, sedation, addiction, and even death.

By applying new knowledge about the receptor structure, scientists altered fentanyl to make it bind to the established site of activity on the outside of the mu-opioid receptor. At the same time, it engages a binding site for sodium ions that exists deep within the receptor.

When the newly designed drug interacts with both sites on the mu-opioid receptor, it maintains its painkilling effects while reducing harmful side effects.

"The newly designed fentanyl medication is engineered to work as a partial agonist, which are drugs that bind to and activate a receptor but only have partial efficacy," study co-author Jay McLaughlin, Ph.D., a professor of pharmacodynamics at the University of Florida College of Pharmacy said in a press release.

Fentanyl is a prescription drug used to treat people in severe pain, such as cancer or terminally ill patients. When sold illegally, it is often mixed with other recreational drugs, increasing the risk of overdose.

Since 2000, there have been 400,000 opioid-involved deaths in the U.S. The opioid epidemic, driven by overprescription and the influx of illegal drugs, mostly from foreign cartels, costs the country tens of billions of dollars every year.

Last year, researchers from the University of Houston developed a vaccine that could eliminate fentanyl's "high" by blocking the drug's ability to enter the brain. The vaccine, which was only tested in rats, is hoped to prevent a relapse in fentanyl addiction recovery.

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