This analysis demonstrates pharmacological effects on TRP channels in HEK cells, suggesting implications for drug discovery.
Transient receptor potential (TRP) channels are non-selective cation channels activated by diverse stimuli, such as temperature, pharmacological agents, pH, osmolarity, and mechanical stress. In this study, we characterized the pharmacological and temperature-dependent modulation of TRPV3 and TRPM8 channels using Sophion’s automated patch clamp (APC) platforms, QPatch Compact, QPatch II, and Qube 384. Human embryonic kidney (HEK) cells expressing TRPV3 or TRPM8 were used. TRPV3 was probed with 2-aminoethoxydiphenyl borate (2-APB) and ruthenium red (RR), while TRPM8 was modulated with racemic menthol (RM), icilin, and capsazepine at distinct holding potentials and temperatures. TRPV3 currents were activated by 2-APB in a concentration-dependent manner, with IC50 values slightly increased at 34°C compared to 25°C. RR effectively blocked TRPV3 activity, with stronger inhibition at elevated temperature. Notably, the inhibitory effect of RR was more pronounced when higher concentrations were applied initially. TRPM8 activation by RM was consistently observed across all APC platforms, with enhanced efficacy at lower temperature (18°C). The logEC50 values indicated stronger activation at cooler conditions for both RM and icilin. Furthermore, capsazepine blocked RM-induced TRPM8 currents in a concentration-dependent manner, with inhibitory potency largely unaffected by temperature differences. Overall, both TRPV3 and TRPM8 channels displayed expected pharmacological and thermosensitive profiles in line with literature values. These findings demonstrate that Sophion’s APC platforms enable reliable and reproducible assessment of TRP channel pharmacology and biophysical properties, providing robust tools for ion channel research and drug discovery.
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Scaduto et al. (2026) studied this question.
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