Key result
NNC 55-0396 selectively inhibits T-type calcium channels (IC50 ~7 μM) without detectable effects on high voltage-activated currents at 100 μM, avoiding the L-type channel inhibition seen with mibefradil.
Population
Recombinant Cav3.1 T-type channels expressed in HEK293 cells and INS-1 cells
Design
Preclinical
Authors
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Advances selective T-type blockade as a research tool; leaves open clinical translation in cardiovascular disease.
NNC 55-0396 is a stable analog of mibefradil that selectively inhibits T-type calcium channels without producing the metabolite that inhibits L-type channels.
Li et al. (2006) studied this question. NNC 55-0396 was evaluated on Inhibition of recombinant Cav3.1 T-type channels and high voltage-activated currents. NNC 55-0396 selectively inhibits T-type calcium channels (IC50 ~7 μM) without detectable effects on high voltage-activated currents at 100 μM, avoiding the L-type channel inhibition seen with mibefradil.
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