Key result
Amlodipine ionization directly regulates the onset and recovery of L-type calcium channel block.
Why the study?
The electrophysiologic properties of amlodipine on cardiac L-type calcium channels and the effect of drug ionization on channel block were not fully understood.
Population
Single guinea-pig ventricular cells
Comparison
Ionized vs neutral forms of amlodipine
Design
Preclinical electrophysiologic study
Authors
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May alter amlodipine efficacy in pH-variable states; leaves open human cardiac translation.
The degree of ionization of amlodipine limits its access to the dihydropyridine receptor, providing mechanistic insights into its interaction with cardiac L-type calcium channels.
Kass et al. (1989) studied this question. Amlodipine was evaluated on L-type calcium channel block development and recovery. The degree of ionization of amlodipine affects both the development of and recovery from L-type calcium channel block in guinea-pig ventricular cells.
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