Scientists at the University of Arizona Health Sciences are developing a safe and effective non-opioid pain reliever after the new compound was found to reduce the sensation of pain by regulating a physiological channel linked to pain, according to Science Daily.
In the United States, 21 to 29% of patients who are prescribed opioids for chronic pain relief misuse them, while around 12% of people develop an opioid use disorder, according to the National Institute on Drug Abuse. In 2019 alone, about 50,000 Americans died from opioid overdoses.
Dr. Rajesh Khanna, Professor of Pharmacology in the UArizona College of Medicine, said, “Drug discovery for chronic pain is at the forefront of this research, and it’s being amplified by the intersection of the COVID-19 pandemic and the opioid epidemic.”
“Drug discovery is a very arduous process,” he added. “Our lab looked at a fundamental mechanism of pain, came up with a way to differentiate it from those before us and found a compound that has the potential as a new non-opioid treatment for pain.”
The study was published in Science Translational Medicine.
The physiological mechanism here is a sodium ion channel (NaV1.7) that previously was associated with the sensation of pain through genetic studies of people with rare pain disorders.
NaV1.7 is a human-validated target for pain so several attempts have tried to stop pain using sodium ion channel inhibitors that block NaV1.7; none have been successful.
However, Dr. Khanna and his team used a different approach. Rather than blocking NaV1.7, they indirectly regulated it using a compound they designed and dubbed 194 in a lab setting using nerve cells from four different species, including humans.
In animal models, the compound was found effective in reversing pain in six different pain models in both sexes. The researchers said 194 might also promote pain relief by activating the body’s endogenous, or naturally occurring, opioid system. Plus, the compound did not cause addiction, motor performance issues, and depressive behaviors.
Compound 194 has shown great promise for pain relief, but Dr. Khanna and his team have been working with the National Institutes of Health’s National Center for Advancing Translational Sciences (NCATS) to optimize the compound.
An NCATS team is now focusing on improving the compound’s half-life and its drug-like properties.
The researchers are now trying to optimize the compound’s potential as a pain-relieving drug and advance to the next stage. They will soon file for approval from the Food and Drug Administration (FDA) to study the compound in humans.