IndraLab

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ML67-33 activates KCNK2. 12 / 12
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"Thus, ML67-33 increases TREK current to reduce the TG excitability, leading to a decrease of the migraine phenotype observed in wild-type animals treated with NO-donors."
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"Although ML67-33 activation matches that of the most effective but unspecific activator, arachidonic acid, ML67-33 stimulation of K 2.1 (TREK-1) does not require Ct (Figure 6F), a channel element that is central to the action of chloroform, arachidonic acid, and other gating inputs."
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"Moreover, a dihydroacridine analog (ML67-33) has been described to selectively activate the TREK-1, TREK-2, and TRAAK channels, and has no effect on the TASK1, TASK2, and TASK3 or KCNQ2 channels [207]."
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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]."
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"The observation that ML67-33 activates K 2.1 (TREK-1) in excised membrane patches (Figure 5) demonstrates that the compound does not act by perturbing channel trafficking or via a mechanism that involves cytosolic proteins and suggests that ML67-33 acts directly on the channel.Diverse gating signals that include protons, temperature, mechanical force, and phosphorylation control K 2.1 (TREK-1) function."
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"Therefore, ML67-33 specifically activates TREK1 and/or TREK2 currents in TG sensory neurons."
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"Importantly, ML67-33 strongly activates the three members of the TREK subfamily but not TASK-1, TASK-2, TASK-3 or TRESK [XREF_BIBR]."
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"ML67-33 increases TREK1 and TREK2 currents in TG sensory neurons."
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"ML67-33 was developed from one of the activators and is reported to selectively activate members of the TREK subfamily."
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"TREK1 and TREK2 activation by ML67-33 reverses the migraine-like cutaneous allodynia in mice."
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"ML67-33 Activates the K 2P 2.1 (TREK-1) C-Type Gate."
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"ML67-33 application to excised membrane patched from HEK cells expressing K 2.1 (TREK-1) showed that ML67-33 activated K 2.1 (TREK-1) in both the outside-out (Figure 5A) and inside-out (Figure 5B) configurations."
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