Literature DB >> 1972773

Sodium channel blockers: the size/solubility hypothesis revisited.

K R Courtney1.   

Abstract

The influence that drug size has on the rate of recovery of sodium channels in heart tissue has been reexamined. A drug dimension that looks at the end-on view of the molecule provides a substantially better explanation for the size dependence of repriming kinetics than does molecular weight. A quantitative model for the recovery time is provided that couples proton exchange kinetics with a drug size-dependent process that is related to recovery from inactivation. Drugs having a wider span at their aromatic end produce more slowing of the rate of recovery from inactivation.

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Year:  1990        PMID： 1972773

Source DB:  PubMed          Journal:  Mol Pharmacol        ISSN： 0026-895X            Impact factor:   4.436


  6 in total

1.  Potent and use-dependent block of cardiac sodium channels by U-50,488H, a benzeneacetamide kappa opioid receptor agonist.

Authors:  M K Pugsley; E J Yu; A L Goldin
Journal:  Exp Clin Cardiol       Date:  2001

2.  Inhibition of skeletal muscle sodium currents by mexiletine analogues: specific hydrophobic interactions rather than lipophilia per se account for drug therapeutic profile.

Authors:  Annamaria De Luca; Sophie Talon; Michela De Bellis; Jean-François Desaphy; Carlo Franchini; Giovanni Lentini; Alessia Catalano; Filomena Corbo; Vincenzo Tortorella; Diana Conte-Camerino
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2003-01-25       Impact factor: 3.000

3.  Comparison of pyrrolidinyl and piperidinyl benzamides for their anticonvulsant activity and inhibitory action on sodium channel.

Authors:  Y Zhu; W B Im; R A Lewis; P F VonVoigtlander
Journal:  Br J Pharmacol       Date:  1992-05       Impact factor: 8.739

4.  Evaluation of the pharmacological activity of the major mexiletine metabolites on skeletal muscle sodium currents.

Authors:  M De Bellis; A De Luca; F Rana; M M Cavalluzzi; A Catalano; G Lentini; C Franchini; V Tortorella; D Conte Camerino
Journal:  Br J Pharmacol       Date:  2006-08-21       Impact factor: 8.739

5.  Classification of drugs based on properties of sodium channel inhibition: a comparative automated patch-clamp study.

Authors:  Nora Lenkey; Robert Karoly; Peter Lukacs; E Sylvester Vizi; Morten Sunesen; Laszlo Fodor; Arpad Mike
Journal:  PLoS One       Date:  2010-12-20       Impact factor: 3.240

6.  Different pH-sensitivity patterns of 30 sodium channel inhibitors suggest chemically different pools along the access pathway.

Authors:  Alexandra Lazar; Nora Lenkey; Krisztina Pesti; Laszlo Fodor; Arpad Mike
Journal:  Front Pharmacol       Date:  2015-09-25       Impact factor: 5.810
  6 in total

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