A2793 (100 μM) inhibits the unstimulated channel by 43.0±8.9% (n=5) while after ionomycin activation the reduction of the TRESK current is 85.5±2.9% (n=5).
It inhibits TASK-1 (100 μM, 53.4±13,5%, n=5), while A2764 is more selective for TRESK, it only moderately influences TREK-1 and TALK-1.
A2793 may be considered as a tool to discriminate between the resting and activated channels in heterologous expression systems, and to block TRESK activated by calcineurin in the native cells which do not express TASK-1.
