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Action of tocainide and mexiletine on the excitation threshold of myelinated nerves.

Eur. J. Pharmacol. 141, 225-233 (1987)
DOI PMC
Open Access Green möglich sobald Postprint bei der ZB eingereicht worden ist.
The antiarrhythmic drugs tocainide and mexiletine increase the excitation threshold and decrease the Na permeability (P(Na)) in nerves. Hodgkin-Huxley model calculations suggest that the P(Na) decrease is not sufficient to explain the threshold increase at low concentrations (<0.7 mM tocainide; < 0.1 mM mexiletine). On the other hand, a drug action on the membrane surface potential would be consistent with results of recent experiments. To clarify this point electrophysiological experiments on single nerve fibres (Rana esculenta) were carried out. Changes of the threshold interval (difference between membrane and threshold potential; V(m) - V(s)) were measured and compared with the corresponding changes of V(m) and V(s) (V(s) was measured by means of the transition voltage V(Tr)). The quantitatively good agreement between changes of V(m) - V(s) and those of V(Tr) suggests that at low concentrations tocainide and mexiletine decrease nerve excitability by acting mainly on the membrane surface charge. This possibility was supported by an independent electrophoresis experiment with myelin vesicles from the same nerve material.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Korrespondenzautor
ISSN (print) / ISBN 0014-2999
e-ISSN 0014-2999
Quellenangaben Band: 141, Heft: 2, Seiten: 225-233 Artikelnummer: , Supplement: ,
Verlag Elsevier
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed