Blocking effect of NIP-142 on the KCNQ1/KCNE1 channel current expressed in HEK293 cells

Iyuki Namekata; Noriko Tsuruoka; Yayoi Tsuneoka; Tomoyuki Matsuda; Akira Takahara; Yoshio Tanaka; Takeshi Suzuki; Tetsuo Takahashi; Naoko Iida-Tanaka; Hikaru Tanaka

doi:10.1248/bpb.34.153

Blocking effect of NIP-142 on the KCNQ1/KCNE1 channel current expressed in HEK293 cells

Iyuki Namekata, Noriko Tsuruoka, Yayoi Tsuneoka, Tomoyuki Matsuda, Akira Takahara, Yoshio Tanaka, Takeshi Suzuki, Tetsuo Takahashi, Naoko Iida-Tanaka, Hikaru Tanaka

Research output: Contribution to journal › Article › peer-review

5 Citations (Scopus)

Abstract

We examined the effect of NIP-142, a benzopyran compound with terminating effect on experimental atrial arrhythmia, on the KCNQ1/KCNE1 channel, which underlies the slow component of the cardiac delayed rectifier potassium channel (I_Ks). NIP-142, as well as chromanol 293B, showed concentration-dependent blockade of the current expressed in HEK293 cells; the EC₅₀ value of NIP-142 and chromanol 293B for the inhibition of tail current was 13.2 μM and 4.9 μM, respectively. These results indicate that NIP-142 has blocking effect on the KCNQ1/KCNE1 channel current.

Original language	English
Pages (from-to)	153-155
Number of pages	3
Journal	Biological and Pharmaceutical Bulletin
Volume	34
Issue number	1
DOIs	https://doi.org/10.1248/bpb.34.153
Publication status	Published - 2011
Externally published	Yes

Keywords

Atrial fibrillation
KCNE1
KCNQ1
NIP-142

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

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10.1248/bpb.34.153

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title = "Blocking effect of NIP-142 on the KCNQ1/KCNE1 channel current expressed in HEK293 cells",

abstract = "We examined the effect of NIP-142, a benzopyran compound with terminating effect on experimental atrial arrhythmia, on the KCNQ1/KCNE1 channel, which underlies the slow component of the cardiac delayed rectifier potassium channel (IKs). NIP-142, as well as chromanol 293B, showed concentration-dependent blockade of the current expressed in HEK293 cells; the EC50 value of NIP-142 and chromanol 293B for the inhibition of tail current was 13.2 μM and 4.9 μM, respectively. These results indicate that NIP-142 has blocking effect on the KCNQ1/KCNE1 channel current.",

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author = "Iyuki Namekata and Noriko Tsuruoka and Yayoi Tsuneoka and Tomoyuki Matsuda and Akira Takahara and Yoshio Tanaka and Takeshi Suzuki and Tetsuo Takahashi and Naoko Iida-Tanaka and Hikaru Tanaka",

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T1 - Blocking effect of NIP-142 on the KCNQ1/KCNE1 channel current expressed in HEK293 cells

AU - Namekata, Iyuki

AU - Tsuruoka, Noriko

AU - Tsuneoka, Yayoi

AU - Matsuda, Tomoyuki

AU - Takahara, Akira

AU - Tanaka, Yoshio

AU - Suzuki, Takeshi

AU - Takahashi, Tetsuo

AU - Iida-Tanaka, Naoko

AU - Tanaka, Hikaru

PY - 2011

Y1 - 2011

N2 - We examined the effect of NIP-142, a benzopyran compound with terminating effect on experimental atrial arrhythmia, on the KCNQ1/KCNE1 channel, which underlies the slow component of the cardiac delayed rectifier potassium channel (IKs). NIP-142, as well as chromanol 293B, showed concentration-dependent blockade of the current expressed in HEK293 cells; the EC50 value of NIP-142 and chromanol 293B for the inhibition of tail current was 13.2 μM and 4.9 μM, respectively. These results indicate that NIP-142 has blocking effect on the KCNQ1/KCNE1 channel current.

AB - We examined the effect of NIP-142, a benzopyran compound with terminating effect on experimental atrial arrhythmia, on the KCNQ1/KCNE1 channel, which underlies the slow component of the cardiac delayed rectifier potassium channel (IKs). NIP-142, as well as chromanol 293B, showed concentration-dependent blockade of the current expressed in HEK293 cells; the EC50 value of NIP-142 and chromanol 293B for the inhibition of tail current was 13.2 μM and 4.9 μM, respectively. These results indicate that NIP-142 has blocking effect on the KCNQ1/KCNE1 channel current.

KW - Atrial fibrillation

KW - KCNE1

KW - KCNQ1

KW - NIP-142

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Blocking effect of NIP-142 on the KCNQ1/KCNE1 channel current expressed in HEK293 cells

Abstract

Keywords

ASJC Scopus subject areas

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