Title : State- and use-dependent block of muscle Nav1.4 and neuronal Nav1.7 voltage-gated Na+ channel isoforms by ranolazine.

Pub. Date : 2008 Mar

PMID : 18079277






4 Functional Relationships(s)
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1 State- and use-dependent block of muscle Nav1.4 and neuronal Nav1.7 voltage-gated Na+ channel isoforms by ranolazine. Ranolazine sodium voltage-gated channel alpha subunit 9 Homo sapiens
2 Use-dependent block of Na(+) channel isoforms by ranolazine during repetitive pulses (+50 mV/10 ms at 5 Hz) was strong at 100 microM, up to 77% peak current reduction for Nav1.4, 67% for Nav1.5, and 83% for Nav1.7. Ranolazine sodium voltage-gated channel alpha subunit 9 Homo sapiens
3 In addition, we found conspicuous time-dependent block of inactivation-deficient Nav1.4, Nav1.5, and Nav1.7 Na(+) currents by ranolazine with estimated IC(50) values of 2.4, 6.2, and 1.7 microM, respectively. Ranolazine sodium voltage-gated channel alpha subunit 9 Homo sapiens
4 On- and off-rates of ranolazine were 8.2 microM(-1) s(-1) and 22 s(-1), respectively, for Nav1.4 open channels and 7.1 microM(-1) s(-1) and 14 s(-1), respectively, for Nav1.7 counterparts. Ranolazine sodium voltage-gated channel alpha subunit 9 Homo sapiens