Quantitative modeling of 4-aminopyridine block of transient outward current

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216305%3A26220%2F99%3A4360033" target="_blank" >RIV/00216305:26220/99:4360033 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Quantitative modeling of 4-aminopyridine block of transient outward current
Original language description
The 4-aminopyridine (4-AP) sensitive component of transient outward current (Ito) is a prominent modulator of repolarization phase of cardiac action potential. The inhibition of cardiac Ito is characterised by reverse use dependency which has been tentatively explained as a result of high affinity of the drug to the open and the resting channel and unattainability of block in the inactivated state [1]. With the aim to explain the experimental data, we have proposed a quantitative model (see the kineticscheme) based on the following presumptions: 1. Only charged (protonated) 4-AP molecules have access to their receptor through the open channel and bind in a voltage dependent manner (O-B0+). 2. The protonation and deprotonation of the drug molecule canoccur even in the blocked open channel (B0+-B0). 3. The effect of block on the operation of activating gates is negligible. 4. The drug-receptor interaction in the closed channels is voltage ndependent (B1-C1)
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
BO - Biophysics
OECD FORD branch
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Project
<a href="/en/project/GA305%2F97%2F0043" target="_blank" >GA305/97/0043: The role of membrane currents in electrical and mechanical restitution of cardiac cells.</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
1999
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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