The action of flecainide acetate and its enantiomers on mammalian non-myelinated nerve fibres
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The effects of flecainide acetate racemate and its two enantiomers on voltage-operated sodium and potassium channels and on the sodium pump activity of non-myelinated fibres of the guinea-pig vagus nerve were studied with the sucrose-gap method. The racemic mixture as well as theR enantiomer andS enantiomer in a concentration range of 3·10−5−3·10−4M caused suppression of the compound action potential, a diminished propagation velocity and a reduction of the post-tetanic potential (PTH), which was also observed with lidocaine. There was no significant difference in the effect caused by the enantiomers seperately. TheR enantiomer tended to evoke a stronger effect compared with theS enantiomer. However, the magnitude of the action is concentration-dependent. At a concentration<10−4M the action of the racemate was stronger than an equimolar concentration of the enantiomers. The activity of the sodium pump, defined by the time constant of post-tetanic potential decay, was affected at a concentration of 10−4M of the racemate, in contrast to lidocaine. The racemate and both enantiomers of flecainide acetate possess a similar local anaesthetic action, as reflected by the inhibition of voltage-operated sodium channels.
KeywordsAction potentials Enantiomers Flecainide acetate Nerve fibres, non-myelinated Sodium pump, electrogenic Structure-activity relationship
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