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Anti‐anginal arylalkylamines and sodium channels: [ 3 H]‐batrachotoxinin‐A 20‐α‐benzoate and [ 3 H]‐tetracaine binding
Author(s) -
Grima M.,
Schwartz J.,
Spach M.O.,
Velly J.
Publication year - 1986
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1986.tb11168.x
Subject(s) - tetracaine , chemistry , sodium channel , sodium , sodium benzoate , membrane , binding site , sodium salicylate , stereochemistry , biophysics , biochemistry , anesthesia , organic chemistry , biology , medicine , lidocaine
1 [ 3 H]‐batrachotoxinin‐A 20‐α‐benzoate ([ 3 H]‐BTX‐B) and [ 3 H]‐tetracaine are useful ligands for the study of sodium channels. 2 Inhibition of their binding by various anti‐anginal drugs was tested on a rat synaptosomal preparation and on a heart membrane preparation. 3 Diphenylalkylamines and structurally related drugs inhibited [ 3 H]‐BTX‐B binding in both the synaptosomal preparation and heart membrane preparation. They were almost inactive on [ 3 H]‐tetracaine binding. 4 These results suggest that activity of arylalkylamines could be mediated by an interaction on the sodium channel.