According to the Centers for Disease Control, overdoses claim the lives of 100,000 Americans annually, with a significant majority attributed to the consumption of synthetic opiates such as fentanyl. Although naloxone, currently the only antidote for opiate overdose, is more widely available now, i
Researchers have discovered a potential new method for reversing fentanyl overdoses by using modified cannabidiol as a negative allosteric modulator at the opioid receptor binding site. Initial in vitro tests showed that modified CBD successfully reversed fentanyl effects, and further in vivo testing is planned to assess its ability to counteract respiratory depression, a primary overdose effect.
“The synthetic opiates bind very tightly to the opioid receptors,” said Alex Straiker, senior research scientist for the Gill Center for Biomolecular Science. “Naloxone must compete with opioids for the same binding site in the central nervous system to cancel out an overdose. But during a fentanyl overdose, naloxone and fentanyl bind to different sites, meaning there is no competition. We wanted to see if a negative allosteric modulator could reverse the fentanyl effects.
“We’ve identified structural parts that are important for the desired antidote effect,” Straiker said. “Some of these compounds are much more potent than the lead. We’ve worked with a third lab to model the binding site that may help identify additional compounds moving forward.”
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