1st QPatch Compact paper from Prof Bruce Bean’s lab at Harvard Medical School shows VX-150 and VX-548 target Nav1.8 ion channels for potential pain relief
The world’s first paper using the QPatch Compact focuses on studying the inhibition of Nav1.8 ion channels by two new pain-relief compounds, VX-150 and VX-548. Nav1.8 channels are key targets in pain-sensing neurons, making them critical for pain-related treatments. The research, conducted by Prof. Bruce Bean’s lab at Harvard Medical School, used the QPatch Compact semi-automated patch clamp system to carry out voltage-clamp recordings, analyzing the effects of these compounds on Nav1.8 sodium currents.
VX-150 and VX-548 are highly selective inhibitors of Nav1.8 channels, with VX-548 showing more potency (IC50 0.27 nM) than VX-150. The study revealed a unique property the authors dubbed “reverse use-dependence”, where inhibition is relieved during repeated depolarizations. This behavior demonstrates the potential effectiveness of these drugs in treating pain while maintaining selectivity and minimizing side effects.
The research highlights the increasingly important role of using automated systems like QPatch Compact for higher-throughput and precision experiments. This enabled lead author Dr. Patric Vaelli and colleagues to efficiently test and characterize drug pharmacology, and the study is another significant step toward developing novel, non-opioid pain therapies targeting Nav1.8 channels.