Many analgesics act via proteins on the surface of cell surfaces that activate adapter molecules, G proteins. G protein-coupled receptors (GPCRs) are hampered by the propensity of GPCRs to couple with multiple intracellular signaling pathways. This in turn leads to several downstream cellular effects, which are not always desirable. This is especially true for conventional drugs that target adenosine A1 receptors (A1Rs), which can cause sedation and heart issues.

To solve this problem, scientists at the University of Warwick, University of Cambridge, University of Bern, Monash University, Coventry University, and industrial partners tested BnOCPA, which doesn't cause sedation, bradycardia, hypotension, or respiratory depression (Nature Communications, July 18, 2022). Instead, BnOCPA selectively activates the A1Rs so that potential side effects are reduced.

The selectivity and potency of BnOCPA make it unique and with further research it could be used to generate potent painkillers and has demonstrated a new method for targeting other GPCRs in drug discovery, according to the researchers.