Nowa wersja platformy jest już dostępna.
Przejdź na https://bibliotekanauki.pl

PL EN


Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników
2008 | 59 | 3 | 409-423
Tytuł artykułu

Evidence for state-dependent block of DPI 201-106, a synthetic inhibitor of Na+ channel inactivation, on delayed-rectifier K+ current in pituitary tumor (GH3) cells

Treść / Zawartość
Warianty tytułu
Języki publikacji
EN
Abstrakty
EN
DPI 201-107 (DPI), a diphenylpiperazinylindole derivative, was reported to be a cardio-selective modifier of voltage-gated Na+ channels. It remains unclear whether DPI has any effects on ion currents. The effects of DPI on ion currents and membrane potential in pituitary tumor (GH3) cells were investigated in this study. DPI (1-100 µM) suppressed the amplitude of delayed-rectifier K+ current (IK(DR)) in a concentration-dependent manner with an IC50 value of 9.4 µM. The presence of DPI also enhanced the rate and extent of IK(DR) inactivation. Recovery from block by DPI (10 µM) was fitted by a single exponential. Crossover of tail currents during the exposure to DPI was also observed. Under current-clamp recordings, DPI prolonged action potential duration in GH3 cells. With a minimal binding scheme, DPI-induced block of IK(DR) was quantitatively provided. The exposure to DPI also blocked IK(DR) with a concomitant increase in current inactivation in NG108-15 neuronal cells. Taken together, the results imply that DPI acts as an open-channel blocker of delayed-rectifier K+ channels in these cells. The widening of action potentials induced by DPI in these cells may be explained mainly by its block of IK(DR) in a state-dependent manner.
Wydawca
-
Rocznik
Tom
59
Numer
3
Strony
409-423
Opis fizyczny
p.409-423,fig.,ref.
Twórcy
autor
  • National Cheng Kung University Medical College, No.1, University Road, Tainan 70101, Taiwan
autor
autor
autor
autor
Bibliografia
Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.agro-article-ced681bf-d329-4739-bf36-4dff40a3c510
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.