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 (I(Ks)). NIP-142, as well as chromanol 293B, showed concentration-dependent blockade of the current expressed in HEK293 cells; the EC(50) 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.
authors.affiliation: Department of Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, Funabashi, Chiba 274–8510, Japan.
authors.forename: Iyuki
authors.initials: I
authors.lastname: Namekata
authors.forename: Noriko
authors.initials: N
authors.lastname: Tsuruoka
authors.forename: Yayoi
authors.initials: Y
authors.lastname: Tsuneoka
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Matsuda
authors.forename: Akira
authors.initials: A
authors.lastname: Takahara
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Tanaka
authors.forename: Takeshi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Takahashi
authors.forename: Naoko
authors.initials: N
authors.lastname: Iida-Tanaka
authors.forename: Hikaru
authors.initials: H
authors.lastname: Tanaka
mesh_terms: D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000494:pharmacology*; D001578:Benzopyrans / Q000008:administration & dosage / Q000494:pharmacology*; D002839:Chromans / Q000008:administration & dosage / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D051657:KCNQ1 Potassium Channel / Q000378:metabolism*; D008564:Membrane Potentials / Q000187:drug effects*; D018408:Patch-Clamp Techniques; D024642:Potassium Channels, Voltage-Gated / Q000378:metabolism*
chemical_list: D000889:Anti-Arrhythmia Agents; D001578:Benzopyrans; D002839:Chromans; C489622:KCNE1 protein, human; D051657:KCNQ1 Potassium Channel; C496909:KCNQ1 protein, human; C427584:NIP142; D024642:Potassium Channels, Voltage-Gated; C029141:2,2,5,7,8-pentamethyl-1-hydroxychroman