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GI‐530159, a novel, selective, mechanosensitive two‐pore‐domain potassium (K 2P ) channel opener, reduces rat dorsal root ganglion neuron excitability
Author(s) -
Loucif Alexandre J C,
Saintot PierrePhilippe,
Liu Jia,
Antonio Brett M,
Zellmer Shan G,
Yoger Katrina,
Veale Emma L,
Wilbrey Anna,
Omoto Kiyoyuki,
Cao Lishuang,
Gutteridge Alex,
Castle Neil A,
Stevens Edward B,
Mathie Alistair
Publication year - 2018
Publication title -
british journal of pharmacology
Language(s) - Uncategorized
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.14098
Subject(s) - mechanosensitive channels , dorsal root ganglion , hyperpolarization (physics) , patch clamp , electrophysiology , neuroscience , potassium channel , current clamp , sodium channel , chemistry , membrane potential , biophysics , ion channel , biology , sensory system , biochemistry , sodium , receptor , organic chemistry , nuclear magnetic resonance spectroscopy
TREK two-pore-domain potassium (K 2P ) channels play a critical role in regulating the excitability of somatosensory nociceptive neurons and are important mediators of pain perception. An understanding of the roles of TREK channels in pain perception and, indeed, in other pathophysiological conditions, has been severely hampered by the lack of potent and/or selective activators and inhibitors. In this study, we describe a new, selective opener of TREK channels, GI-530159.