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. 2019 Feb 1;10:104–111. doi: 10.1016/j.reth.2018.12.002

Table 2.

IC50 values of pirmenol, mexiletine and pilsicainide block of INa and ICaL in iCell cardiomyocytes, with those of Nav 1.5-mediated currents in transfected cells and clinical concentrations of the agents.

iCell cardiomyocytes (present study)
 Expression systems
 Clinical concentrations (Cmax)
 MW
INa block (μM) ICaL block (μM) Nav 1.5 block (μM) (ng/mL) (μM) (g/mol)
pirmenol 0.87 ± 0.37 2.00 ± 0.39 ND 1770 ± 200 5.23 ± 0.59 338.4864
mexiletine 30 ± 3.0 5.0 ± 0.1 159a 1090 ± 200 6.08 ± 1.12 179.2588
pilsicainide 0.88 ± 0.16 7.7 ± 2.5 307 ± 19b 566.8 ± 145.2 2.08 ± 0.53 272.3853

ND: not determined.

a

Determined at a holding potential of −120 mV [Ref. [30]].

b

Determined at a holding potential of −90 mV [Ref. [31]].