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Arachidonic acid activates KCNK2. 52 / 53
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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."
29416642
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"Application of arachidonic acid (10 mumol/L), chloroform (1 mmol/L) or etomidate (10 mumol/L) substantially increased TREK-1 channel currents in CHO and hTREK -1 cells."
27397543
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"Consistent with these previous studies, fluoxetine inhibited TREK1 in basal conditions (I /I = 0.45 ± 0.04, Figure 5A, left panel and Figure 5E), but not TREK1 stimulated by AA (I /I = 1.21 ± 0.06, Figure 5A, right panel and Figure 5E)."
30233308
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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."
28937579
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"TREK1, TREK2, and TRAAK are activated by arachidonic acid (AA) and other polyunsaturated fatty acids, such as docosahexaenoic acid and linoleic acid [ xref xref xref xref xref ]."
27790056
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"Taken together these data demonstrated that spadin displays direct, selective antagonism of AA-activation of TREK-1 channels."
32317978
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"Arachidonic acid (an activator of TREK channels) had no effect on this conductance."
16265669
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"The activation of TREK-1 by AA and inhibition by forskolin were closely linked to membrane hyperpolarization and depolarization, respectively."
23858003
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"Mechanistically, TREK-1 channel may be activated by intracellular acidification and AA accumulation known to occur during ischemia [32,34,9]."
31511966
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"Application of 10 muM arachidonic acid (AA) (free fatty acid) to cells expressing TREK-1 robustly activates TREK-1."
28793254
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"Spadin Specifically Antagonizes AA-Activation of TREK-1 Channels."
32317978
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"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."
32317978
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"To sum up, we reproduced TREK-1 activation by AA upon electrical stimulation."
32499717
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"TRAAK, TREK-1, and TREK-2 channels are activated by arachidonic acid (AA)."
26919430
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"Therefore, we suppose that the mechanical stretch due to the mastication activates phospholipase A (2) to release arachidonic acid (AA) from membrane, then, the released AA activates TREK-1."
17786632
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"Spadin Selectively Antagonizes Arachidonic Acid Activation of TREK-1 Channels."
32317978
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"Although known as an inhibitor of many K + channels [13], AA also has been demonstrated to stimulate hEAG1 [16], Kir2.3 [17], and the TREK subfamily of K2P channels, including TREK-1, TREK-2, and TRAAK [18]."
30661462
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"The effect of cochlin was opposite to the well-known effects of shear stress stimulation by fluid flow or arachidonic acid (20microM), which significantly increased TREK-1 current by 72.1 +/-21.9% and 148.7 +/-50.1%, respectively (n = 5 each; Fig."
28352076
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"Our data suggest that the opening of background K (+) channels, like TREK-1 and TRAAK, which are activated by arachidonic acid and other polyunsaturated fatty acids such as docosahexaenoic acid and linolenic acid, is a significant factor in this neuroprotective effect."
10775263
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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]."
35216214
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"Since the known membrane curvature inducer AA had been shown previously to reversibly activate TREK-1, we also tested its effect."
32499717
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"Therefore, we suppose that the mechanical stretch due to the mastication activates phospholipase A (2) to release arachidonic acid (AA) from membrane, then, the released AA activates TREK-1."
17786632
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"TREK1, TREK2, and TRAAK are activated by arachidonic acid (AA) and other polyunsaturated fatty acids, such as docosahexaenoic acid and linoleic acid [XREF_BIBR XREF_BIBR XREF_BIBR XREF_BIBR XREF_BIBR]."
27790056
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"Single channel recording via patch clamping showed that the TREK-1 outward currents in astrocytes could be activated by arachidonic acid (AA) or chloroform with the conductance of 113 +/-14 and 120 +/-13pS, respectively."
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"AA activates TREK-1 with a dose-dependent manner and requires C-terminal part of the channel which is crucial for the activation and the inhibition following phosphorylation by the protein kinase A (PKA)."
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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."
29416642
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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."
32317978
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"Fluoxetine had no effect on AA-activated TRAAKpCt TREK1 (I fluoxetine /I control = 0.92 ± 0.03) (Figure xref , right panel andFigure xref )."
30233308
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"As shown in XREF_FIG, TREK-1 current was potentiated by 10muM arachidonic acid (AA) and application of SPA (10 -6 M) inhibited the AA activated TREK-1 current."
28105440
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"Since TREK and TRAAK channels are activated by arachidonic acid, it has been suggested that the mechanically sensitive phospholipase A 2 could mediate these effects XREF_BIBR although TRAAK mechanical activation is still possible in the presence of phospholipase A 2 inhibitors."
23691227
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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)."
26914156
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"Mutation of the same threonine residues also blunts activation of TREK-1 by arachidonic acid and PIP 2 xref ."
31455781
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"In a number of experiments, we examined the action of AA on membrane patches, keeping in mind that AA could stimulate TREK-1 directly [21]."
30661462
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"Application of 10 muM arachidonic acid (AA) (free fatty acid) to cells expressing TREK-1 robustly activates TREK-1."
28793254
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"Our data infers that spadin is able to antagonize AA-activation of TREK-1 channels via a mechanism that is distinct from the likely site of AA activity, the C-terminal domain, therefore suggesting an allosteric mechanism of antagonism."
32317978
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"Our data suggest that the opening of background K(+) channels, like TREK-1 and TRAAK, which are activated by arachidonic acid and other polyunsaturated fatty acids such as docosahexaenoic acid and linolenic acid, is a significant factor in this neuroprotective effect."
10775263
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"However, the addition of AA to cells can activate TREK-1 in seconds, and our lipidomics study incorporated AA over 15 min."
28793254
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"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 )."
32317978
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"In contrast, TREK-1 currents are increased by LecA and AA, both in response to mechanical and electrical stimulation."
32499717
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"Similarly, arachidonic acid is suggested to activate TREK1 through incorporation in the outer leaflet of the bilayer XREF_BIBR and yet arachidonic does not stimulate TRPC5 XREF_BIBR."
19324410
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"The activation of TREK-1 by AA and inhibition by forskolin were closely linked to membrane hyperpolarization and depolarization, respectively."
23858003
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"As expected, 10 muM of AA produced robust activation of TREK-1 in whole-cell recordings, which reversed slowly upon wash-out (XREF_SUPPLEMENTARY)."
32499717
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"As shown in XREF_FIG, TREK-1 current was potentiated by 10muM arachidonic acid (AA) and application of SPA (10 -6 M) inhibited the AA activated TREK-1 current."
28105440
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"Swelling activated and arachidonic acid induced currents are TREK-1 in rat bladder smooth muscle cells."
26911303
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"Furthermore, as predicted based on arachidonic acid activation of both TREK-1 and TREK-2, some of the small molecules from this TREK-2 HTS were found to activate both TREK-1 and TREK-2."
27805811
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"Finally, we show that Glu306, an amino acid that has previously been found to be important in the modulation of TREK-1 by arachidonic acid, membrane stretch and internal pH, is critical for the activating effects of the anesthetic gases."
14742687
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"The channel failed to open in the absence of PLD2 despite very high concentrations of anesthetics in a biological membrane.TWIK-related arachidonic acid-stimulated K+ channel (TRAAK) is an anesthetic-insensitive homolog of TREK-1 (SI Appendix, Fig. S3E)."
32467161
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"Arachidonic acid (AA) which is generated during CRH stimulation activates TREK-1 channels and causes hyperpolarization."
22225940
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"Treatment of 100 nM spadin inhibited about 60% of the TREK-1 current stimulated by arachidonic acid in TREK-1-transfected COS-7 cells."
33348878
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"Activation of TREK-1 by arachidonic acid (AA) is proposed to occur by a process linked to stretch activation (Brohawn, 2015)."
28242754
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"In inside-out patches, AA activated TRAAK, TREK-1, and TREK-2 channels with EC 50 values of 1.2 ± 0.1, 6.9 ± 1.2, and 3.8 ± 0.4 μM, respectively ( xref B and S6C)."
26919430
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"Mouse TREK-1 and TREK-2 channel currents were both significantly increased by AA, BL-1249, and CDC, similar to their human homologs."
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