Open channel and competitive block of nicotinic receptors by pancuronium and atracurium

Cristopher V. Löwenick, Klaus Krampfl, Hajo Schneck, Eberhard Kochs, Johannes Bufler

Publikation: Beitrag in FachzeitschriftArtikelBegutachtung

15 Zitate (Scopus)

Abstract

Mouse myotubes were used to investigate effects of the nondepolarizing neuromuscular blocking drugs pancuronium and atracurium on embryonic-type nicotinic acetylcholine receptor channels. Experiments were performed using patch-clamp techniques in combination with devices for ultra-fast solution exchange at outside-out patches. Application of 0.1 mM acetylcholine resulted in a fast current transient. When the peak amplitude was achieved, the current decayed monoexponentially due to desensitization. After application of drugs (pancuronium or atracurium), two different mechanisms of block were observed: (1) open channel block of embryonic-type nicotinic acetylcholine receptor channels after coapplication of blocker and acetylcholine, characterized by decrease of the time constant of current decay; (2) competitive block of embryonic-type nicotinic acetylcholine receptor channels by pancuronium or atracurium after preincubation of outside-out patches with the respective blocker. Different affinities of pancuronium (KB≈0.01 μM) and atracurium (KB≈1 μM) to embryonic-type nicotinic acetylcholine receptor channels were observed.

OriginalspracheEnglisch
Seiten (von - bis)31-35
Seitenumfang5
FachzeitschriftEuropean Journal of Pharmacology
Jahrgang413
Ausgabenummer1
DOIs
PublikationsstatusVeröffentlicht - 9 Feb. 2001

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