Anti-anginal arylalkylamines and sodium channels: [3H]-batrachotoxinin-A 20-alpha-benzoate and [3H]-tetracaine binding.

British journal of pharmacology ·Vol. 89 ·No. 4 ·1986-12-00 ·Pages 641-6

Grima M, Schwartz J, Spach MO, Velly J

Abstract

[3H]-batrachotoxinin-A 20-alpha-benzoate ([3H]-BTX-B) and [3H]-tetracaine are useful ligands for the study of sodium channels. Inhibition of their binding by various anti-anginal drugs was tested on a rat synaptosomal preparation and on a heart membrane preparation. Diphenylalkylamines and structurally related drugs inhibited [3H]-BTX-B binding in both the synaptosomal preparation and heart membrane preparation. They were almost inactive on [3H]-tetracaine binding. These results suggest that activity of arylalkylamines could be mediated by an interaction on the sodium channel.

MeSH Terms

Angina Pectoris/drug therapy Animals Batrachotoxins In Vitro Techniques Ion Channels/drug effects Male Membranes/metabolism Myocardium/metabolism Rats Rats, Inbred Strains Synaptosomes/metabolism Tetracaine

Chemicals

Batrachotoxins Ion Channels Tetracaine batrachotoxinin A 20-alpha-benzoate

Authors & Affiliations

4 authors, click to expand affiliations / ORCID

Grima M

Schwartz J

Spach M O

Velly J

References (14)

14 references, click to expand

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Article Info

Journal

British journal of pharmacology

Abbr.

Br J Pharmacol

ISSN

0007-1188

DOI

10.1111/j.1476-5381.1986.tb11168.x

Published

1986-12-00

Pages

641-6

Language

English

Region

England

NLM ID

7502536

PMCID

PMC1917242

Subset

External Links

PubMed source DOI: 10.1111/j.1476-5381.1986.tb11168.x PMC Full Text View journal details

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Anti-anginal arylalkylamines and sodium channels: [3H]-batrachotoxinin-A 20-alpha-benzoate and [3H]-tetracaine binding.

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