Table 2.

K_2P activators^{176,179,181,192,196–202}

Green indicates structurally validated activators Yellow indicates activators supported by mutagenesis or mutagenesis combined with simulation studies. Cells used to measure activity are indicated as follows

^aOocytes,

^bHEK cells,

^cCHO Cells,

^dThallium flux assay,

^eCOS cells,

^ftsA201 cells,

^gAZF cells,

^hfluorescent binding assay,

ⁱK_d values from native mass spectrometry with K_2P4.1a (TRAAK) isoform.

^*Only K_2Ps tested against the activator are listed (other K_2Ps may not have been tested).

^†Other closely related fenamates like mefenamic acid and niflumic acid possess similar activity and selectivity to flufenamic acid.

^‡I/I₀ values at 10 lM DCPIB. EC₅₀ values were not determined as E_max was not reached, even at very high DCPIB concentrations (100 lM).

^§While the EC₅₀s for Pranlukast against the TREK family are nearly identical, the fold-activation observed for K_2P10.1 (TREK-2) was much higher than for K_2P2.1 (TREK-1) or K_2P4.1 (TRAAK).