Scientists claim creation of a non-addictive opioid compound

In what has been called a potential“holy grail” of opioid research,scientists at Wake Forest BaptistMedical Center have created whatthey are calling a non-addictive opioidcompound, a result which could havewidespread repercussions for paintreatment and the ongoing opiateaddiction crisis.

Reported in the journal Proceedings ofthe National Academy of Sciences, thestudy profiles the synthetic opioidBU08028 which was tested on 12 non-human primates and found to not onlybe an effective pain killer but also to be free of adverse side effects such as decreased respiratory functionand, importantly, addiction.

“Based on our research, this compound has almost zero abuse potential and provides safe and effective painrelief,” says Mei-Chuan Ko, professor of physiology and pharmacology at Wake Forest Baptist and leadauthor of the study. “This is a breakthrough for opioid medicinal chemistry that we hope in the future willtranslate into new and safer, non-addictive pain medications.”

Ever since heroin was first synthesized in the late 1800s -and initially proclaimed to be free from the hazardsof abuse- research efforts have been ongoing in the quest to create an opioid analgesic which does notpromote addictive behaviour. And while advances in pharmacology over the past few decades haveproduced dozens of synthetic opioids currently in use for pain management, from effective pain killers likeoxycodone and the extremely potent fentanyl to opioid antagonists such as naloxone that block the body’sreceptor sites from taking in other opioids, the prospect of the addiction-free opioid has remained out ofreach.

But scientists see real potential in BU08028, which binds to two opioid receptors in the body named MOPand NOP like the known compound buprenorphine but is said to have improved activity over buprenorphineat NOP receptors. Researchers studied the behavioral, physiological and pharmacological effects ofBU08028 on non-human primates and found the drug to be highly potent and long-lasting in its analgesiceffect while not inhibiting respiratory or cardiovascular functioning or causing acute physical dependence.

“To our knowledge, the present study provides the first functional evidence in nonhuman primates thatBU08028 with mixed MOP/NOP agonist activities is an effective and safe analgesic without apparent abuseliability or other opioid-associated side effects,” say the study’s authors.

In a commentary on the new study, Dr. Jun-Xu Li of the Jacobs School of Medicine and Biomedical Sciencesat the University of Buffalo has written of the opioid’s “double-edged sword.” “Despite their effectiveness,opioids produce many clinically significant side effects.” says Li. “For decades, research pursued the ‘HolyGrail’ of opioid analgesic research: the development of opioids that retain the analgesic efficacy withreduced side effects. [The new study] reports a systematic evaluation of a novel opioid, BU08028, may leadus one step closer to this ultimate goal.”

The use and abuse of opioids for pain treatment has reached crisis levels in Canada and the United States.Last year in Canada alone, 21.7 million opioid prescriptions were dispensed, a 20 per cent increase over theprevious half-decade.