Charybdotoxin, dendrotoxin and mast cell degranulating peptide block the voltage-activated K+ current of fibroblast cells stably transfected with NGK1 (Kvl.2) K+ channel complementary DNA

Werkman, T.R.; Kawamura, Tetsuro; Yokoyama, Shigeru; Higashida, Haruhiro; Rogawski, Michael A.

doi:10.1016/0306-4522(92)90216-o

Cited by 43 publications

(18 citation statements)

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“…9-11), and some of them have been expressed in cells normally lacking endogenous channels (12)(13)(14). We have taken advantage of such an expression system to study the interaction of fatty acids with Kv1.5, a voltage-dependent K+ channel present at a particularly high level in mammalian heart (including human) (15)(16)(17).…”

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confidence: 99%

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

Honoré

Barhanin

Attali

et al. 1994

Proc. Natl. Acad. Sci. U.S.A.

187

131

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The present work shows that arachidonic acid and some other long chain polyunsaturated fatty acids such as docosahexaenoic acid, which is abundant in fish oil, produce a direct open channel block of the major voltagedependent K+ channel (Kv1.5) cloned in cardiac cells. The inhibitory action of these selected fatty acids is seen when they are applied extracellularly but not when they are included in the patch pipette. Fatty acids then appear to bind to an external site on the Kv1.5 channel structure. Inhibition of Kv1.5 channel activity by polyunsaturated fatty acids (acceleration of the apparent inactivation and decrease of the peak current) is similar to that produced by the class m antiarrhythmic tedisamil. Docosahexaenoic acid and arachidonic acid also inhibit the delayed-rectifier K+ channel currents in cultured mouse and rat cardiomyocytes. These results are discussed in the light of the reported fatty acids effects on cardiac function in disasd states. Since Kv1.5 is also present in the brain, the results reported here could also have a significance in terms of processes such as long-term potentiation or depression.Fatty acids play an important role in the life and death of cardiac cells because (i) they are essential fuels for mechanical, electrical, and synthetic activities of the heart; (ii) their level is abnormally high in an ischemia followed by a reperfusion; and (iii) dietary fish oil is apparently beneficial for heart function (for a review, see ref. 1).In heart, voltage-gated K+ channels determine the resting potential, shape, and length of the action potential, thus controlling cardiac performance. Several different types of voltage-sensitive K+ channels are expressed in myocytes (for reviews, see refs. 2 and 3), and their intrinsic properties are regulated by guanine nucleotide-binding proteins (4) and by different types of kinases (5). Activation of one class of cardiac K+ channels by intracellular arachidonic acid (AA) has also been observed (6-8).

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mentioning

confidence: 99%

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

Honoré

Barhanin

Attali

et al. 1994

Proc. Natl. Acad. Sci. U.S.A.

187

131

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“…TEA at 5 mM also reversibly suppressed the K + current by 20.5 ± 6.5% (n = 3) at 100 mV (data not shown). α-Dendrotoxin, a blocker of Kv1.1 and Kv1.2 (16,17), at 100 nM did not suppress the outward K + current. A selective blocker of I Kr , E-4031, did not affect the I Kur current at 10 µM (data not shown) (18).…”

Section: Effects Of Other Kmentioning

confidence: 93%

“…Since α-dendrotoxin, which selectively blocks Kv1.1 and Kv1.2, did not inhibit the thiopentalsensitive current, the possibility that Kv1.1 or Kv1.2 channels carried this current was excluded (16,17).…”

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confidence: 99%

Inhibitory Effect of Thiopental on Ultra-rapid Delayed Rectifier K+ Current in H9c2 Cells

et al. 2005

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Abstract. Using the whole-cell voltage clamp technique, we investigated the effects of thiopental on membrane currents in H9c2 cells, a cell line derived from embryonic rat heart. Thiopental blocked a rapidly activating, very slowly-inactivating ultra-rapid type I Kur -like outward K + current in a concentration-dependent manner. The half-maximal concentration (IC 50 ) of thiopental was 97 µM with a Hill coefficient of 1.2. The thiopental-sensitive current was also blocked by high concentrations of nifedipine (IC 50 = 9

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“…Recrystallization from methanol afforded 123 mg (50%) of the compound RA-5 as a brownish solid. IR (KBr) (Cao and Houamed, 1999); hKv1.2-B82 cells (Werkman et al, 1992); mKv1.3-L929 cells (Grissmer et al, 1994); hKv7.4-HEK293 (a kind gift from Nicole Schmitt, University Copenhagen, Denmark); hERG-HEK293 (a kind gift from Craig January, University of Wisconsin, Madison, WI); hK Ca 2.1-HEK293 cells and rK Ca 2.2-HEK293 cells; hK Ca 2.3-COS7 cells (Sankaranarayanan et al, 2009); 3T3 fibroblasts (3T3-L1, ref# CL-173, American Type Culture Collection, Rockville, MD); U251 glioblastoma cells; and primary PCA endothelial cells (PCAECs) were cultured in Dulbecco's modified Eagle's medium supplemented with 10% fetal calf serum and penicillin/streptomycin (all from Biochrom KG, Berlin, Germany). The PCAECs were isolated from hearts as described previously (Oliván-Viguera et al, 2013).…”

Section: Methodsmentioning

confidence: 99%

A Novel Pan-Negative-Gating Modulator of K_Ca2/3 Channels, Fluoro-Di-Benzoate, RA-2, Inhibits Endothelium-Derived Hyperpolarization–Type Relaxation in Coronary Artery and Produces Bradycardia In Vivo

et al. 2014

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Charybdotoxin, dendrotoxin and mast cell degranulating peptide block the voltage-activated K+ current of fibroblast cells stably transfected with NGK1 (Kvl.2) K+ channel complementary DNA

Cited by 43 publications

References 44 publications

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

Inhibitory Effect of Thiopental on Ultra-rapid Delayed Rectifier K+ Current in H9c2 Cells

A Novel Pan-Negative-Gating Modulator of K_Ca2/3 Channels, Fluoro-Di-Benzoate, RA-2, Inhibits Endothelium-Derived Hyperpolarization–Type Relaxation in Coronary Artery and Produces Bradycardia In Vivo

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Charybdotoxin, dendrotoxin and mast cell degranulating peptide block the voltage-activated K+ current of fibroblast cells stably transfected with NGK1 (Kvl.2) K+ channel complementary DNA

Cited by 43 publications

References 44 publications

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

External blockade of the major cardiacdelayed-rectifier K+ channel (Kv1.5) by polyunsaturated fattyacids.

Inhibitory Effect of Thiopental on Ultra-rapid Delayed Rectifier K+ Current in H9c2 Cells

A Novel Pan-Negative-Gating Modulator of KCa2/3 Channels, Fluoro-Di-Benzoate, RA-2, Inhibits Endothelium-Derived Hyperpolarization–Type Relaxation in Coronary Artery and Produces Bradycardia In Vivo

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A Novel Pan-Negative-Gating Modulator of K_Ca2/3 Channels, Fluoro-Di-Benzoate, RA-2, Inhibits Endothelium-Derived Hyperpolarization–Type Relaxation in Coronary Artery and Produces Bradycardia In Vivo