A2764 dihydrochloride is a potent and selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), exhibiting moderate inhibitory effects on TREK-1 and TALK-1 channels. This compound demonstrates increased sensitivity to activated mTRESK channels, with an IC50 value of 6.8 μM. A2764 dihydrochloride effectively induces cell depolarization and enhances excitability in native cells, making it a valuable tool for investigating the role of TRESK channels in migraine pathophysiology and nociceptive signaling.
A2764 dihydrochloride is a potent and selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), exhibiting moderate inhibitory effects on TREK-1 and TALK-1 channels. This compound demonstrates increased sensitivity to activated mTRESK channels, with an IC50 value of 6.8 μM. A2764 dihydrochloride effectively induces cell depolarization and enhances excitability in native cells, making it a valuable tool for investigating the role of TRESK channels in migraine pathophysiology and nociceptive signaling.
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