Researchers at Indiana University say a modified version of cannabidiol, a chemical found in cannabis, could help reverse the effects of overdoses from drugs such as fentanyl.
In the study published in the Journal of Medicinal Chemistry on July 12, researchers hoped that the new discovery could lead to a new way to reverse overdoses either through a new product or by working synchronously with naloxone.
According to the Canadian government’s website, an average of 20 people die per day due to apparent opioid toxicity, with synthetic opioids like fentanyl being a major contributor. While naloxone is widely used as an antidote for opiate overdoses, it is found to be less effective against the synthetic opioids in the fentanyl category.
Researchers say in order to counteract the effects of an overdose, your body’s opioid receptors need something else to bind to.
“The synthetic opiates bind very tightly to the opioid receptors,” senior research scientist for the Gill Center for Biomolecular Science Alex Straiker said in a press release published on Tuesday.
“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.”
According to the University of Michigan, an allosteric modulator is a molecule that interacts with other molecules to the degree that it affects their behaviour.
Researchers conducted the experiment by testing 50 chemical compounds to determine which ones exhibited the most potential as a tool to cancel out the effects of fentanyl.
Researchers found cannabidiol, or CBD, “could behave as a negative allosteric modulator at the binding site,” however, high concentrations were needed during the first phase of testing.
After modifying the structure of the CBD to be more effective, researchers found that tests done on blood or tissue samples successfully reversed the effects of fentanyl.
“We’ve identified structural parts that are important for the desired antidote effect,” Straiker explained. “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.”
According to the study, the next important step is for researchers to test their findings on live subjects in order to determine whether they can reverse the effects of respiratory depression, which is what happens to your body during a drug overdose.
Source: Hayat Amanat – ctvnews.ca
