Bilactorfin instead of morphine

A safe alternative to opioids has been created

Sergey Kolenov, Hi-tech+

16 years ago, Australian scientists discovered a new species of mold fungus from the genus Penicillium on the island of Tasmania. During the biochemical analysis, it turned out that it produces three previously unknown tetrapeptide molecules with an unusual molecular structure that affects human opioid receptors.

Taking these molecules as a basis, researchers from the University of Sydney, whose work is described in the press release Estuarine waters hold promise in global pain-relief hunt, synthesized the drug bilorphin. It belongs to the family of opioid receptor agonists associated with G-proteins.

Compounds from this group are considered particularly promising as a safe replacement for traditional opioids. It is assumed that they have the same analgesic effect as morphine, but do not depress breathing and do not lead to constipation.

Scientists have selected several variations of bilorphin and confirmed that one of them, the so-called bilactorfin, has significant analgesic activity. It can be administered both orally and intravenously.

In experiments with mice, the new analgesic was almost as good as morphine. At the same time, unlike opioids, the new drug does not penetrate the blood-brain barrier, which significantly reduces the risk of overdose.

The authors hope that they will soon be able to move on to clinical trials in humans and release bilactorfin to the market within ten years. This will be an important step in the fight against the epidemic of opioid painkiller overdose deaths unfolding in the United States. According to some estimates, an overdose has claimed the lives of 700,000 Americans since the 1990s.

Article by Dekan et al. A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor is published in the journal PNAS – VM.

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