By Eric Sauter
Scientists from the Florida campus of The Scripps Research Institute (TSRI) have been awarded $2.4 million from the National Institute on Drug Abuse of The National Institutes of Health to expand development of new pain medications with fewer side effects than those currently available.
TSRI Professor Laura Bohn, who has been a leader in the development of pain therapies, will be the principal investigator of the new five-year grant.
“We are developing substitutes for narcotic pain killers with less risk for overdose and fewer side effects,” Bohn said. “The new grant enables us to study how these potential drugs, which utilize the same biological target as morphine, fundamentally differ from the current pain medications in how they engage neuronal signaling.”
Adverse side effects of current opioid drugs such as morphine and oxycodone can be serious and include respiratory suppression, constipation and addiction. According to the U.S. Centers for Disease Control, nearly two million Americans abused prescription painkillers in 2013; almost 7,000 people are treated each day in hospital emergency rooms for abuse of these drugs.
While the new compounds under development activate the same receptor as morphine—the mu opioid receptor or MOR—they do so in a way that avoids recruiting the protein beta-arrestin 2. Genetic studies have shown that animal models lacking beta-arrestin 2 experience robust pain relief with diminished side effects.
“The difference in the way that these new compounds work results in greater pain relief without as much respiratory suppression (overdose risk) and persistent constipation in preclinical studies,” said Bohn. “We are hoping to dial out dependence liabilities as we pursue bringing these drugs to clinical trials.”
The number of the new grant is 1R01DA038964.
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