Protein and Chemical Determinants of BL-1249 Action and Selectivity for K_2P Channels.

ABSTRACT: K_2P potassium channels generate leak currents that stabilize the resting membrane potential of excitable cells. Various K_2P channels are implicated in pain, ischemia, depression, migraine, and anesthetic responses, making this family an attractive target for small molecule modulator development efforts. BL-1249, a compound from the fenamate class of nonsteroidal anti-inflammatory drugs is known to activate K_2P2.1(TREK-1), the founding member of the thermo- and mechanosensitive TREK subfamily; however, its mechanism of action and effects on other K_2P channels are not well-defined. Here, we demonstrate that BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K_2P subfamilies. Patch clamp exper

SUBMITTER: Pope L 

PROVIDER: S-EPMC6302903 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature