Blocking Effect of NIP-142 on the KCNQ1/KCNE1 Channel Current Expressed in HEK293 Cells

• Published in: Biological & Pharmaceutical Bulletin Vol. 34; no. 1; pp. 153 - 155
• Main Authors: Namekata, Iyuki, Tsuruoka, Noriko, Tsuneoka, Yayoi, Matsuda, Tomoyuki, Takahara, Akira, Tanaka, Yoshio, Suzuki, Takeshi, Takahashi, Tetsuo, Iida-Tanaka, Naoko, Tanaka, Hikaru
• Format: Journal Article
• Language: English; Japanese
• Published: Japan The Pharmaceutical Society of Japan 01.01.2011; Pharmaceutical Society of Japan; Japan Science and Technology Agency
• Subjects: Anti-Arrhythmia Agents - administration & dosage; Anti-Arrhythmia Agents - pharmacology; atrial fibrillation; Benzopyrans - administration & dosage; Benzopyrans - pharmacology; Chromans - administration & dosage; Chromans - pharmacology; Dose-Response Relationship, Drug; HEK293 Cells; Humans; KCNE1; KCNQ1; KCNQ1 Potassium Channel - metabolism; Membrane Potentials - drug effects; NIP-142; Patch-Clamp Techniques; Potassium Channels, Voltage-Gated - metabolism
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.34.153

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.