TRPA1 - "High Throughput Activation and Block of hTRPA1 on Nanion’s SyncroPatch 384PE"
SyncroPatch 384PE (a predecessor model of the SyncroPatch 384) application note (0.6 MB)
Cells were kindly provided by Millipore.
Transient receptor potential (TRP) channels have become important potential targets in drug discovery for the treatment of, for example, pain, respiratory diseases such as asthma, cancer and immune disorders, multiple kidney diseases and skeletal disorders1 . The transient receptor potential ankyrin 1 (TRPA1), a member of the TRP family of cation channels, plays a predominant role in the sensation of noxious cold² and inflammatory pain3 . The channel is activated by a range of environmental irritants causing pain, pungent compounds found in foods such as garlic, mustard and cinnamon, as well as metabolites produced during oxidative stress4 . Consistent with its proposed function in nociception, TRPA1 has been shown to be expressed in sensory neurons of the dorsal root ganglion (DRG) and trigeminal ganglion, both of which transmit painful responses². Thus, within drug development, much attention is paid to the TRPA1 channel. Preclinical data and data from a recent human genetic study5 highlight TRPA1 antagonists as a promising new approach for the treatment of acute and chronic pain. Indeed, a TRPA1 antagonist has shown positive results in a proof-ofconcept study for diabetic neuropathic pain6 . The most challenging aspects involved in the screening of the TRPA1 channel are the channel’s mechanosensitivity, fast desensitization and activity dependence on intracellular calcium. Here, we present high quality data with reliable pharmacology on hTRPA1 expressing HEK cells collected on the SyncroPatch 384PE. Data is presented showing activation of the TRPA1 channel by SCMA and inhibition by A-967079.