Quoted by Epoch Health
Naloxone has long been used by first responders, such as police officers, firefighters, and paramedics, to save the lives of those who have overdosed on opioids.
The effectiveness of naloxone has been challenged by the rising incidence of fentanyl, a synthetic opioid that is far more strong than heroin.
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Compound 368 is a newly found substance by Stanford researchers that improves naloxone’s capacity to treat opioid overdoses, especially ones containing fentanyl.
It was discovered through an extensive search of billions of compounds. While Fentanyl is 50 – 100 times more potent than heroin. The extreme potency of fentanyl makes it harder for naloxone alone to reverse overdoses effectively.
“Naloxone binding to an opioid receptor turns it mostly off, but not all the way,” said Evan O’Brien, the lead author of the new study, in a press release. “Our data shows that compound 368 is able to increase the binding of naloxone and turn the receptor off more completely.”
“The compound itself doesn’t bind well without naloxone,” said Mr. O’Brien, a post-doctoral scholar at Stanford. “We think naloxone has to bind first, and then compound 368 is able to come in and cap it in place.”
“The compound in mice, at least from the assays we’ve run, does nothing on its own,” Mr. O’Brien said. “We don’t see anything happen to the mice even when we inject a massive amount of compound 368.”
“When we start to give them more and more of compound 368 with that low dose of naloxone, they take their tail out of the water pretty quickly,” Mr O’Brien said.
