GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K_2P ) channel opener, reduces rat dorsal root ganglion neuron excitability.

ABSTRACT:

Background and purpose

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.

Experimental approach

The effect of GI-530159 on TREK channels was demonstrated using ⁸⁶ Rb efflux assays, whole-cell and single-channel patch-clamp recordings from recombinant TREK channels. The expression of K_2P 2.1 (TREK1), K_2P 10.1 (TREK2

SUBMITTER: Loucif AJC 

PROVIDER: S-EPMC5980259 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature