Police officers, firefighters, and paramedics have been trained to save the lives of many overdose victims by administering naloxone, a drug that reverses the deadly effects of opioids such as heroin. But the recent flood of fentanyl into America—a synthetic opioid designed for severe and chronic pain relief that packs a punch 50 to 100 times greater than heroin—has stymied many life-saving efforts of first responders. Naloxone is effective at rapidly reversing an opioid overdose when administered because it replaces the deadly opioids in the opioid receptors.
The researchers, who searched through billions of compounds to find this one, said it can bind next to naloxone in the receptors. Working with mice, the scientists found that when they exposed cells with opioid receptors to compound 368, there was little effect. But when they combined 368 with naloxone, opioids were more effectively blocked from binding.
The more of this newly discovered compound was added, the better naloxone blocked opioids, including fentanyl and morphine. Because opioids reduce the sensation of pain, researchers tested how quickly the mice removed their tails from hot water to see the effects of varying doses of opioid antidotes. When the mice on morphine were given compound 368 alone, there was no difference in the length of time it took the mice to remove their tails from the water.
In other words, the sensation of pain was the same with or without compound 368. This confirmed that the compoun.
