Modulation of ERG channels by XE991.

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Modulation of ERG channels by XE991. / Elmedyb, Pernille; Calloe, Kirstine; Schmitt, Nicole; Hansen, Rie Schultz; Grunnet, Morten; Olesen, Søren-Peter.

In: Basic & Clinical Pharmacology & Toxicology, Vol. 100, No. 5, 2007, p. 316-22.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Elmedyb, P, Calloe, K, Schmitt, N, Hansen, RS, Grunnet, M & Olesen, S-P 2007, 'Modulation of ERG channels by XE991.', Basic & Clinical Pharmacology & Toxicology, vol. 100, no. 5, pp. 316-22. https://doi.org/10.1111/j.1742-7843.2007.00048.x

APA

Elmedyb, P., Calloe, K., Schmitt, N., Hansen, R. S., Grunnet, M., & Olesen, S-P. (2007). Modulation of ERG channels by XE991. Basic & Clinical Pharmacology & Toxicology, 100(5), 316-22. https://doi.org/10.1111/j.1742-7843.2007.00048.x

Vancouver

Elmedyb P, Calloe K, Schmitt N, Hansen RS, Grunnet M, Olesen S-P. Modulation of ERG channels by XE991. Basic & Clinical Pharmacology & Toxicology. 2007;100(5):316-22. https://doi.org/10.1111/j.1742-7843.2007.00048.x

Author

Elmedyb, Pernille ; Calloe, Kirstine ; Schmitt, Nicole ; Hansen, Rie Schultz ; Grunnet, Morten ; Olesen, Søren-Peter. / Modulation of ERG channels by XE991. In: Basic & Clinical Pharmacology & Toxicology. 2007 ; Vol. 100, No. 5. pp. 316-22.

Bibtex

@article{f5b862c0ab5311ddb5e9000ea68e967b,
title = "Modulation of ERG channels by XE991.",
abstract = "In neuronal tissue, KCNQ2-5 channels conduct the physiologically important M-current. In some neurones, the M-current may in addition be conducted partly by ERG potassium channels, which have widely overlapping expression with the KCNQ channel subunits. XE991 and linopiridine are known to be standard KCNQ potassium channel blockers. These compounds have been used in many different tissues as specific pharmacological tools to discern native currents conducted by KCNQ channels from other potassium currents. In this article, we demonstrate that ERG1-2 channels are also reversibly inhibited by XE991 in the micromolar range (EC(50) 107 microM for ERG1). The effect has been characterized in Xenopus laevis oocytes expressing ERG1-2 and in the mammalian HEK293 cell line stably expressing ERG1 channels. The IC(50) values for block of KCNQ channels by XE991 range 1-65 microM. In conclusion, great care should be taken when choosing the concentration of XE991 to use for experiments on native potassium channels or animal studies in order to be able to conclude on selective KCNQ channel-mediated effects.",
author = "Pernille Elmedyb and Kirstine Calloe and Nicole Schmitt and Hansen, {Rie Schultz} and Morten Grunnet and S{\o}ren-Peter Olesen",
note = "Keywords: Acetylcholine; Animals; Anthracenes; Carbamates; Cell Line; Chromans; Dose-Response Relationship, Drug; Electrophysiology; Ether-A-Go-Go Potassium Channels; Gene Expression; Indoles; Oocytes; Patch-Clamp Techniques; Phenylenediamines; Potassium Channel Blockers; Potassium Channels, Voltage-Gated; Pyridines; Xenopus laevis",
year = "2007",
doi = "10.1111/j.1742-7843.2007.00048.x",
language = "English",
volume = "100",
pages = "316--22",
journal = "Basic & Clinical Pharmacology & Toxicology",
issn = "1742-7835",
publisher = "Wiley-Blackwell",
number = "5",

}

RIS

TY - JOUR

T1 - Modulation of ERG channels by XE991.

AU - Elmedyb, Pernille

AU - Calloe, Kirstine

AU - Schmitt, Nicole

AU - Hansen, Rie Schultz

AU - Grunnet, Morten

AU - Olesen, Søren-Peter

N1 - Keywords: Acetylcholine; Animals; Anthracenes; Carbamates; Cell Line; Chromans; Dose-Response Relationship, Drug; Electrophysiology; Ether-A-Go-Go Potassium Channels; Gene Expression; Indoles; Oocytes; Patch-Clamp Techniques; Phenylenediamines; Potassium Channel Blockers; Potassium Channels, Voltage-Gated; Pyridines; Xenopus laevis

PY - 2007

Y1 - 2007

N2 - In neuronal tissue, KCNQ2-5 channels conduct the physiologically important M-current. In some neurones, the M-current may in addition be conducted partly by ERG potassium channels, which have widely overlapping expression with the KCNQ channel subunits. XE991 and linopiridine are known to be standard KCNQ potassium channel blockers. These compounds have been used in many different tissues as specific pharmacological tools to discern native currents conducted by KCNQ channels from other potassium currents. In this article, we demonstrate that ERG1-2 channels are also reversibly inhibited by XE991 in the micromolar range (EC(50) 107 microM for ERG1). The effect has been characterized in Xenopus laevis oocytes expressing ERG1-2 and in the mammalian HEK293 cell line stably expressing ERG1 channels. The IC(50) values for block of KCNQ channels by XE991 range 1-65 microM. In conclusion, great care should be taken when choosing the concentration of XE991 to use for experiments on native potassium channels or animal studies in order to be able to conclude on selective KCNQ channel-mediated effects.

AB - In neuronal tissue, KCNQ2-5 channels conduct the physiologically important M-current. In some neurones, the M-current may in addition be conducted partly by ERG potassium channels, which have widely overlapping expression with the KCNQ channel subunits. XE991 and linopiridine are known to be standard KCNQ potassium channel blockers. These compounds have been used in many different tissues as specific pharmacological tools to discern native currents conducted by KCNQ channels from other potassium currents. In this article, we demonstrate that ERG1-2 channels are also reversibly inhibited by XE991 in the micromolar range (EC(50) 107 microM for ERG1). The effect has been characterized in Xenopus laevis oocytes expressing ERG1-2 and in the mammalian HEK293 cell line stably expressing ERG1 channels. The IC(50) values for block of KCNQ channels by XE991 range 1-65 microM. In conclusion, great care should be taken when choosing the concentration of XE991 to use for experiments on native potassium channels or animal studies in order to be able to conclude on selective KCNQ channel-mediated effects.

U2 - 10.1111/j.1742-7843.2007.00048.x

DO - 10.1111/j.1742-7843.2007.00048.x

M3 - Journal article

C2 - 17448117

VL - 100

SP - 316

EP - 322

JO - Basic & Clinical Pharmacology & Toxicology

JF - Basic & Clinical Pharmacology & Toxicology

SN - 1742-7835

IS - 5

ER -

ID: 8418570