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December 9, 1997Proceedings of the National Academy of SciencesOpen Access

Sodium channel selectivity filter regulates antiarrhythmic drug binding

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Population

Adult rat skeletal muscle Na+ channel (micro1) model

Comparison

Mutation of selectivity filter residues and… vs Wild-type channels or alternative mutations

Design

Preclinical

Authors

ASAkihiko SunamiInternational University of Health and WelfareSDSamuel C. DudleyElectrophysiologyHFHarry A. FozzardUniversity of Vermont

Discussion

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Overview

May inform Na+ channel-targeted antiarrhythmic design; extends molecular insights but leaves open human translation.

Structured PICO

P
Population
Adult rat skeletal muscle Na+ channel (micro1) model
I
Intervention
Mutation of selectivity filter residues (K1237E, K1237S, K1237R, D400A, E755A, A1529D) and application of lidocaine, neutral analogs, QX314, QX222, neo-saxitoxin, and tetrodotoxin
C
Comparator
Wild-type channels or alternative mutations
O
Outcome
Na+ channel block characteristics (resting block, recovery from block)surrogate

The Na+ channel selectivity filter interacts with the hydrophilic part of local anesthetic antiarrhythmic drugs, regulating their binding and access.

Cite This Study

Sunami et al. (1997) studied this question.

synapsesocial.com/papers/69dee28b5e217d93a5558e72https://doi.org/10.1073/pnas.94.25.14126
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1A calcium-dependent transient outward current in Xenopus laevis oocytes1982 · 471 citations
  2. 2The Ionic Channels in Excitable Membranes1975 · 1,669 citations
  3. 3A Classification of Antiarrhythmic Actions Reassessed After a Decade of New Drugs1984 · 819 citations
  4. 4Common molecular determinants of local anesthetic, antiarrhythmic, and anticonvulsant block of voltage-gated Na+ channels.1996 · 507 citations
  5. 5On the structural basis for ionic selectivity among Na+, K+, and Ca2+ in the voltage-gated sodium channel1996 · 264 citations