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Arachidonic acid activates KCNK2. 73 / 74
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"To further analyze the effects of pyrethroids in the K channels expressed in native neurons, we searched for small/medium-sized neurons, where arachidonic acid (a known activator of TREK-1, TREK-2, and TRAAK ) or cloxyquin (a TRESK-activating compound ) increased the current measured at hyperpolarized voltages in high extracellular K solution."
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"It is interesting to note that ALA (non-specific activator of TREK-1) or arachidonic acid (activator of TREK-1) increased CVSMCs whole-cell currents, which were blocked by selective blockers of large-conductance Ca-activated K+ channels in both wild-type and TREK-1 (gene name KCNK2) knockout mice [64]."
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"However, application of 1 μM spadin alone failed to inhibit mTREK-1-Y284A basal currents; 11.3 ± 1.9 μA (control) versus 11.3 ± 2.0 μA (spadin) ( xref ), and reinforces our suggestion that spadin is not a channel blocker of activated channels, but selectively and specifically antagonizes AA-activation of TREK-1 channels via an allosteric mechanism."
sparser
"Here, using murine forms of TREK-1 and TREK-2, we provide evidence that spadin is not a direct blocker of TREK-1 when expressed in heterologous systems but an antagonist, displaying no intrinsic activity, able to selectively prevent AA-activation of TREK-1 channels through an allosteric mechanism."
sparser
"However that spadin antagonizes AA activation of TREK-1 channels, and not that of DHA, suggests that AA activation of TREK-1 may involve a mechanism distinct from the C-terminal domain, interacting with other regions in TREK-1 or inducing its effects through interactions with the lipid bilayer ( xref )."
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"Deletion of the N-terminus (Chemin et al., 2005a) or the C-terminus (up to Thr322) of TREK1 channels does not affect either basal or AA activated TREK1 currents, but additional truncation of the C-terminal to Arg311 reduced the activation of the current by AA, and truncation at Val298 completely abolished AA stimulation (Patel et al., 1998; Maingret et al., 2000a)."
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"In fact, LPA strongly and reversibly reduced TREK1 currents expressed in oocytes and inhibited the TREK1 currents induced by AA and LPC, with all these effects involving the activation of the Phospholipase C pathway and requiring the C-terminus of the channel protein (Cohen et al., 2009)."
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"It is unlikely that block of phospholipase A underlies the substantive effects on TREK and TRESK channels seen here, because arachidonic acid enhances TREK (and TRAAK) channels (Fink et al., 1996; Enyedi and Czirják, 2010) and blocks TRESK channels (Sano et al., 2003; Kang et al., 2004)."
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"Two pore potassium channels (K ) are also called the background K conductance channels and are constituted by six sub-families: the TWIK, the TWIK-related K channel/TWIK-related arachidonic acid-stimulated K channels (TREK/TRAAK), the TASK, the TWIK-related alkaline pH-activated K channels (TALK), the tandem pore domain halothane-inhibited K channels (THIK) and the TWIK-related spinal cord K channels (TRESK) [157]."
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"Importantly, in uterine strips treated simultaneously with progesterone and L-methionine, no significant reduction in uterine contraction was observed, and the uterine contraction was at levels similar to those in control tissues without progesterone or L-methionine treatment, suggesting opposing effects of L-methionine and progesterone on TREK-1 channel mediated uterine relaxation TREK-1 activator arachidonic acid causes no further effect on progesterone induced uterine relaxation."
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"The present study showed that treatment of uterine strips with TREK-1 channel inhibitor L-methionine insignificantly increased uterine contraction, while treatment with TREK-1 activator arachidonic acid caused a dramatic reduction in uterine contraction, suggesting that the TREK-1 is active and functional during pregnancy in rats."