Scientists are developing a new non-opioid pain reliever with fewer side effects
- A promising compound benzyloxy-cyclopentyladenosine (BnOCPA) found to be a potent and selective analgesic in test model systems
- BnOCPA is also selective in its action and non-addictive, opening the potential for the development of potent analgesics without side effects
- Results revealed in a paper published by scientists from the University of Warwick, University of Cambridge, University of Bern, Monash University, Coventry University and industry partners
A promising new non-opioid pain reliever (analgesic) with potentially fewer side effects compared to other powerful pain relievers has been discovered.
A team of scientists, co-led by researchers from the School of Life Sciences, University of Warwick, investigated a compound called BnOCPA (benzyloxy-cyclopentyladenosine), which was found to be a potent and selective non-addictive analgesic in test models systems. BnOCPA also has a unique mode of action and potentially opens a new pipeline for the development of novel analgesic drugs.
The research by the Warwick team, along with colleagues from the University of Cambridge, the University of Bern, Monash University, Coventry University and industry collaborators, is published in Nature Communications in a document entitled “Selective activation of G?ob by an adenosine A1 receptor agonist produces analgesia without cardiorespiratory depression”.
In the UK, between a third and a half of the population report moderate to severe disabling chronic pain. Such pain has a negative impact on quality of life and many of the commonly used pain relievers cause side effects. Opioid drugs, such as morphine and oxycodone, can be addictive and dangerous in overdose. Consequently, there is an unmet need for new and potent pain-relieving drugs.
Many drugs work through proteins on the surface of cell surfaces that activate adapter molecules called G proteins. Activation of G proteins can lead to many cellular effects. BnOCPA is unique in that it activates only one type of G protein, resulting in very selective effects and thus reducing potential side effects.
Dr Mark Wall, from the School of Life Sciences at the University of Warwick, who led the research, said: “The selectivity and effectiveness of BnOCPA make it truly unique, and we hope that with further research it will be possible to generate powerful pain relievers to help patients manage chronic pain.”
Professor Bruno Frengueli, Principal Investigator of the project, from the School of Life Sciences at the University of Warwick, said: “This is a fantastic example of serendipity in science. We had no expectation that BnOCPA would behave differently from other molecules in its class, but the more we looked at BnOCPA, we discovered properties that had never been seen before and that could open up new areas of medicinal chemistry.
Professor Graham Ladds, the project’s co-principal investigator from the University of Cambridge, said: “This is an amazing story looking at agonist bias for GPCRs. BnOCPA not only has the potential to be a new type of pain reliever, but it has shown us a new method to target other GPCRs in drug discovery.
Original article: Scientists are developing a new non-opioid pain reliever with fewer side effects
Since: University of Warwick | Cambridge University | University of Bern | Monash University | Coventry University
A surprising new non-opioid pain killer with fewer side effects