PT  - JOURNAL ARTICLE
AU  - K R Courtney
TI  - Sodium channel blockers: the size/solubility hypothesis revisited.
DP  - 1990 Jun 01
TA  - Molecular Pharmacology
PG  - 855--859
VI  - 37
IP  - 6
4099  - http://molpharm.aspetjournals.org/content/37/6/855.short
4100  - http://molpharm.aspetjournals.org/content/37/6/855.full
SO  - Mol Pharmacol1990 Jun 01; 37
AB  - 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.