Effect of NIP-142 on potassium channel alpha-subunits Kv1.5, Kv4.2 and Kv4.3, and mouse atrial repolarization.
Effects of NIP-142, a benzopyran compound which terminates experimental atrial arrhythmia, on potassium channel alpha-subunits and mouse atrial repolarization were examined. NIP-142 concentration-dependently blocked the outward current through potassium channel alpha subunits Kv1.5, Kv4.2 and Kv4.3 expressed in Xenopus oocytes. In isolated mouse atrial myocardia, NIP-142 prolonged the action potential duration and effective refractory period, and increased the contractile force. These results suggest that NIP-142 blocks the potassium channels underlying the transient and sustained outward currents, which may contribute to its antiarrhythmic activity.
Tanaka
Hikaru
H
Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences, Funabashi, Chiba 274-8510, Japan. htanaka@phar.toho-u.ac.jp
Namekata
Iyuki
I
Hamaguchi
Shogo
S
Kawamura
Taro
T
Masuda
Hiroyuki
H
Tanaka
Yoshio
Y
Iida-Tanaka
Naoko
N
Takahara
Akira
A
D000200:Action Potentials / Q000187:drug effects; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001281:Atrial Fibrillation / Q000188:drug therapy*; D001578:Benzopyrans / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D006325:Heart Atria / Q000187:drug effects*; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects*; D009206:Myocardium / Q000737:chemistry*; D009865:Oocytes; D051637:Shaker Superfamily of Potassium Channels / Q000037:antagonists & inhibitors*; D014981:Xenopus
D000889:Anti-Arrhythmia Agents; D001578:Benzopyrans; C427584:NIP142; D051637:Shaker Superfamily of Potassium Channels