Scientists from the University of Warwick have developed a non-opioid pain killer with minimal side effects.
Opioids are a class of drugs that work to produce a variety of effects, including pain relief. These drugs attach to opioid receptors in the brain cells to release signals that block the perception of pain and boost feelings of pleasure. However, opioids can be dangerous as they are highly addictive, and the feelings of pleasure can contribute to psychological dependence on the drugs.
The addictive nature of opioids drives scientists and researchers to develop alternatives that can provide similar benefits. Scientists from the University of Warwick, with support from the University of Cambridge, University of Bern, Monash University, Coventry University and industrial partners, have now created a non-opioid pain killer with few side effects.
The team’s discovery is published in Nature Communications.
Developing a non-opioid pain killer
Scientists co-led by researchers from the School of Life Sciences, University of Warwick, investigated a compound called BnOCPA (benzyloxy-cyclopentyladenosine) and found it to be a potent and selective analgesic, which is non-addictive in test model systems. BnOCPA has the potential to open new opportunities for future analgesic drugs.
Dr Mark Wall, from the School of Life Sciences at the University of Warwick, who led the research, said: “The selectivity and potency of BnOCPA make it truly unique and we hope that with further research, it will be possible to generate potent painkillers to help patients cope with chronic pain.”
Meeting the medication needs of chronic pain patients
In the UK, one-third to one-half of the population report moderate to severe chronic pain. This disabling pain can affect the quality of life, and common opioids lead to sometimes deadly side effects. The dangers of opioids generate a need for new and potent non-opioid pain killers.
Many drugs act via proteins on the surface of cell surfaces that activate adapter molecules called G proteins. Activating G proteins leads to many cellular effects, and the unique quality of BnOCPA only activates a singular G protein. This leads to very selective effects, resulting in reduced possible side effects.
Professor Bruno Frenguelli, the principal investigator on the project from the University of Warwick’s School of Life Sciences, said: “This is a fantastic example of serendipity in science. We had no expectations that BnOCPA would behave any differently from other molecules in its class; the more we looked into BnOCPA, we discovered properties that had never been seen before and which may open up new areas of medicinal chemistry.”
Professor Graham Ladds, the co-principal investigator on the project from the University of Cambridge, concluded: “This is an amazing story looking at agonist bias for a GPCR. Not only does BnOCPA have the potential to be a new type of painkiller, but it has shown us a new method for targeting other GPCRs in drug discovery.”
