Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers
Population
Cloned human cardiac potassium channel, hKv1.5, studied under whole cell voltage-clamp conditions
Comparison
Racemic terfenadine, R-terfenadine… vs Control conditions
Design
Preclinical
Authors
Discussion
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Member takes
Implication
Terfenadine enantiomers equipotently block hKv1.5; leaves open whether chiral separation reduces clinical cardiotoxicity.
Structured PICO
P
Population
Cloned human cardiac potassium channel, hKv1.5, studied under whole cell voltage-clamp conditions
I
Intervention
Racemic terfenadine, R-terfenadine, S-terfenadine, and an acid metabolite
C
Comparator
Control conditions
O
Outcome
Mechanism of action and EC50 of hKv1.5 current blocksurrogate
Racemic terfenadine and its enantiomers are equipotent blockers of the human cardiac potassium channel hKv1.5, suggesting that using a single enantiomer would not reduce its cardiac toxicity.
Cite This Study
Yang et al. (1995) studied this question.