IndraLab

Statements

BL-1249 activates KCNK2. 7 / 7
| 7
reach
"Finally, Tertyshnikova et al. used a similar approach to demonstrate that BL-1249 enhanced TREK-1 currents in human bladder cells [XREF_BIBR]."
29928032
reach
"BL-1249 activates K 2.1(TREK-1) and K 10.1(TREK-2), but its effects on other K channels have not been characterized."
30089357
reach
"Finally, both BL-1249 and ML67-33 are known to activate TREK channels and they induce a current very similar to that induced by riluzole in nodose neurons [XREF_BIBR, XREF_BIBR]."
29928032
reach
"Similar to many K activators, BL-1249 enhances TREK subfamily currents by stimulating the selectivity filter C-type gate."
30089357
reach
"Furthermore, spadin was unable to prevent activation of TREK-1 by BL-1249, CDC, or the related bioactive lipid, DHA."
32317978
reach
"Thus, the data show that extracellular application of BL-1249 activates all members of the mechano- and thermosensitive TREK subfamily while sparing the other subfamilies and shows selectivity for K 2.1(TREK-1) and K 10.1(TREK-2) over K 4.1(TRAAK)."
30089357
reach
"Together with previous single point concentration studies showing the insensitivity of K 2.1(TREK-1) W275S in mammalian cells, our data provide definitive evidence that BL-1249 activates K 2.1(TREK-1) by stimulating the C-type gate."
30089357