Key result
The R(+) enantiomer of IQB-9302 was 3.2-fold more potent than the S(-) enantiomer in blocking hKv1.5 channels (KD 17.8 vs 58.6 microM).
Population
hKv1.5 channels stably expressed in LTK:(-) cells
Design
Preclinical
Authors
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May guide enantiopure Kv1.5 blocker design; leaves open translation to human arrhythmia therapy.
Effect estimate: 3.2-fold more potent
Absolute Event Rate: 17.8% vs 58.6%
The R(+) enantiomer of IQB-9302 is 3.2-fold more potent than the S(-) enantiomer in blocking human cardiac Kv1.5 channels, with potency determined by the length of the N-substituent.
González et al. (2001) studied this question. IQB-9302 enantiomers vs. S(-) enantiomer was evaluated on Potency of hKv1.5 channel block (K(D)) (3.2-fold more potent). The R(+) enantiomer of IQB-9302 was 3.2-fold more potent than the S(-) enantiomer in blocking hKv1.5 channels (KD 17.8 vs 58.6 microM).
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