Chemical Name: 4,4'-[[2,2,2-Trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis[benzenamine]
Biological ActivityGI 530159 is a TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro.
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GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability.
Loucif et al.
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