GI-530159

GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC₅₀ of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect^[1]. IC50 & Target: Target: TREK1/2^[1] In Vitro: TREK (TWIK-related K) two pore domain potassium (K2P) channels regulate the excitability of somatosensory nociceptive neurons and mediate pain perception^[1].
GI-530159 (1 µM or 10 µM) shows selectivity and activates TREK1 and TREK2 channels but shows no significant effects on TRAAK channels or K channels tested^[1].
GI-530159 (0.1-30 µM) activates recombinant human TREK1 channels with EC₅₀s of 0.8 µM and 0.9 µM from Rb efflux and electrophysiological experiments, respectively^[1].
GI-530159 (1 µM) reduces rat dorsal root ganglion (DRG) neuron excitability, results in firing frequency reduction and a small hyperpolarisation of resting membrane potential (RMP)^[1].