Chronic pain is a condition that affects approximately 20 percent of the adult population. Today, poor efficacy and tolerability limit the chronic use of currently existing analgesics. The transient receptor potential (TRP) C4/C5 are a promising target for non-opioid paint treatment. TRPC4/C5 channels are widely present in the pain pathway and with a ubiquitous expression in peripheral sensory neurons, spinal cord neurons and in the brain. Inhibition of TRPC4/C5 channels is therefore a possible pain-alleviation mechanism.
In a new article published in International Journal of Molecular Science, researchers at Orion Pharma study the effect of the TRPC4/C5 inhibitor HC-070. Using Dynaflow Resolve in a whole-cell patch clamp setup, the authors studied the inhibitory potency of HC-070 on human TRPC4, demonstrating inhibitory effect at low nanomolar level. In vivo experiments in rats showed dose-dependent attenuation of colonic hypersensitivity. Moreover, HC-070 did not affect the withdrawal threshold in the uninjured paw in paw pressure mechanical sensitivity tests. “The results strengthen the idea that TRPC4/C5 antagonism is a novel, safe non-opioid treatment for chronic pain.”, Jalava et al. states.
We congratulate Dr. Ari-Pekka Koivisto and coworkers on their achievements and are honored that they have chosen to use Dynaflow Resolve in their important research.