Inhibition of Human TREK-1 Channels by Bupivacaine

Punke, Mark A.; Licher, Thomas; Pongs, Olaf; Friederich, Patrick

doi:10.1213/01.ane.0000062524.90936.1f

Cited by 39 publications

(25 citation statements)

References 21 publications

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“…We also found that 10 μmol/L AA increased TREK-1 current by 60.0%±3.6% (n=6) ( Figure 1Cc). These results are consistent with previous reports regarding the properties of TREK-1 channels [22] .…”

Section: Electrophysiological Properties Of Trek-1 Channelssupporting

confidence: 94%

Novel neuroprotectant chiral 3-n-butylphthalide inhibits tandem-pore-domain potassium channel TREK-1

Zhao

Cao

et al. 2011

Acta Pharmacol Sin

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Aim:To study the effects of 3-n-butylphthalide (NBP) on the TREK-1 channel expressed in Chinese hamster ovary (CHO) cells. Methods: Whole-cell patch-clamp recording was used to record TREK-1 channel currents. The effects of varying doses of l-NBP on TREK-1 currents were also observed. Current-clamp recordings were performed to measure the resting membrane potential in TREK-1-transfected CHO (TREK-1/CHO) and wild-type CHO (Wt/CHO) cells. Results: l-NBP (0.01-10 μmol/L) showed concentration-dependent inhibition on TREK-1 currents (IC 50 =0.06±0.03 μmol/L), with a maximum current reduction of 70% at a concentration of 10 μmol/L. l-NBP showed a more potent inhibition on TREK-1 current than d-NBP or dl-NBP. This effect was partially reversed upon washout and was not voltage-dependent. l-NBP 10 μmol/L elevated the membrane potential in TREK-1/CHO cells from -55.3 mV to -42.9 mV. However, it had no effect on the membrane potential of Wt/CHO cells. Conclusion: l-NBP potently inhibited TREK-1 current and elevated the membrane potential, which may contribute to its neuroprotective activity.

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Section: Electrophysiological Properties Of Trek-1 Channelssupporting

confidence: 94%

Novel neuroprotectant chiral 3-n-butylphthalide inhibits tandem-pore-domain potassium channel TREK-1

Zhao

Cao

et al. 2011

Acta Pharmacol Sin

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“…Application of a number of anaesthetic agents have been demonstrated to either activate or inhibit K 2P channels. The local anaesthetic bupivicaine has been reported to inhibit a number of tandem pore channels [20] including TASK-2 [19] and TREK-1 [34]. Application of 1 mM bupivicaine to the apical aspect of Calu-3 monolayers inhibited the basal I sc by 11.4±1.7 lA cm À2 or 39.6±9.0% (n = 13; Fig.…”

Section: Evidence For Functional K 2 P Channels In Calu-3 Cellsmentioning

confidence: 92%

Two-pore-domain potassium channels support anion secretion from human airway Calu-3 epithelial cells

Davis

Cowley

2005

Pflugers Arch - Eur J Physiol

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Potassium channels are required for the absorption and secretion of fluids and electrolytes in epithelia. Calu-3 cells possess a secretory phenotype, and are a model human airway submucosal gland serous cell. Short-circuit current (I(sc)) recordings from Calu-3 cells indicated that basal anion secretion was reduced by apical application of the K+ channel inhibitors bupivicaine, lidocaine, clofilium, and quinidine. Application of riluzole resulted in a large increase in I(sc), inhibited by apical application of either bupivicane or the cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channel blocker DPC. These results suggested that one or more members of the two-pore-domain K+ (K(2P)) channel family could influence anion secretion. Using RT-PCR, we found that Calu-3 cells express mRNA transcripts for TASK-2 (KCNK5), TWIK-1 (KCNK1), TWIK-2 (KCNK6) and TREK-1 (KCNK2). TASK-2, TWIK-2 and TREK-1 protein were detected by Western blotting, while immunolocalization of polarized cells confirmed protein expression of TREK-1 and TWIK-2 at the plasma cell membrane. TASK-2 protein staining was localized to intracellular vesicles, located beneath the apical membrane. While the pro-secretory role of basolateral K+ channels is well established, we suggest that apically located K2P channels, not previously described in airway epithelial cells, also play an important role in controlling the rate of transepithelial anion secretion.

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“…We firstly demonstrated whether three K 2 p channels (TREK-1, TREK-2, and TRAAK) were expressed in neural stem cells (NSCs) derived from the hippocampus of fetal Sprague-Dawley rats. The proliferation, differentiation, and apoptosis of embryonic NSCs were then evaluated under two opposing regime where TREK-1 had been overexpressed by transfection with an hTREK-1 gene or suppressed by bupivacaine and curcumin, two strong TREK-1 channel inhibitors (Enyeart et al 2008;Punke et al 2003), respectively. Secondly, we investigated the influence of dexamethasone (DEX), a glucocorticoid hormone receptor agonist, on the proliferation and TREK-1 expression of embryonic NSCs.…”

Section: Introductionmentioning

confidence: 99%

Fluoxetine attenuates the inhibitory effect of glucocorticoid hormones on neurogenesis in vitro via a two-pore domain potassium channel, TREK-1

Zhang

et al. 2010

Psychopharmacology

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Inhibition of Human TREK-1 Channels by Bupivacaine

Cited by 39 publications

References 21 publications

Novel neuroprotectant chiral 3-n-butylphthalide inhibits tandem-pore-domain potassium channel TREK-1

Novel neuroprotectant chiral 3-n-butylphthalide inhibits tandem-pore-domain potassium channel TREK-1

Two-pore-domain potassium channels support anion secretion from human airway Calu-3 epithelial cells

Fluoxetine attenuates the inhibitory effect of glucocorticoid hormones on neurogenesis in vitro via a two-pore domain potassium channel, TREK-1

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