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

Loucif, Alexandre J C, Saintot, Pierre-Philippe, Liu, Jia, Antonio, Brett M, Zellmer, Shannon G, Yoger, Katrina, Veale, Emma L., Wilbrey, Anna, Omoto, Kiyoyuki, Cao, Lishuang, and others. (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K ) channel opener, reduces rat dorsal root ganglion neuron excitability. British journal of pharmacology, 175 (12). pp. 2272-2283. ISSN 1476-5381. (doi:10.1111/bph.14098) (Access to this publication is currently restricted. You may be able to access a copy if URLs are provided) (KAR id:75878)

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Abstract

BACKGROUND AND PURPOSE

TREK two-pore-domain potassium (K ) 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

This article is part of a themed section on Recent Advances in Targeting Ion Channels to Treat Chronic Pain. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v175.12/issuetoc.

Item Type:	Article
DOI/Identification number:	10.1111/bph.14098
Subjects:	Q Science
Divisions:	Faculties > Sciences > Medway School of Pharmacy
Depositing User:	Emma Veale
Date Deposited:	19 Aug 2019 21:30 UTC
Last Modified:	23 Jan 2020 04:16 UTC
Resource URI:	https://kar.kent.ac.uk/id/eprint/75878 (The current URI for this page, for reference purposes)
Veale, Emma L.:	https://orcid.org/0000-0002-6778-9929
Mathie, Alistair:	https://orcid.org/0000-0001-6094-2890

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