IndraLab

Statements

BL-1249 activates KCNK2. 7 / 7
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"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
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"Similar to many K activators, BL-1249 enhances TREK subfamily currents by stimulating the selectivity filter C-type gate."
30089357
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"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
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"Finally, Tertyshnikova et al. used a similar approach to demonstrate that BL-1249 enhanced TREK-1 currents in human bladder cells [XREF_BIBR]."
29928032
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"Similarly, BL-1249 is described to directly activate TREK1 channels (Veale et al., 2014), however this compound not only activates the other two members of the TREK subfamily, but also other channels including TASK3 (K2P channel), calcium-activated BK channels, K 7.2, K 7.3 and also sodium channels (Na 1.7) (Loucif et al., 2018)."
30964046
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"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
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"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