Interactions of quinidine and lidocaine with rat brain and heart muscarinic receptors

Malca Cohen-Armon*, Yoav I. Henis, Yoel Kloog, Mordechai Sokolovsky

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

We have studied the effect of quinidine and lidocaine on binding to rat brain and cardiac muscarinic receptors. Both drugs had a higher affinity to brain stem and cardiac receptors, as compared with cerebral cortex, coinciding with the distribution of high-affinity agonist binding sites in the above tissues. The effects of the drugs on muscarinic antagonist and agonist binding did not fit simple competition to one receptor site, suggesting either preferential binding to high affinity agonist binding sites, or allosteric interactions. Batrachotoxin, which opens voltage sensitive sodium channels, had an opposite effect on agonist binding. The possibility of allosteric interactions between the muscarinic receptors and a site analogous to the sodium channel is discussed.

Original languageEnglish
Pages (from-to)326-332
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume127
Issue number1
DOIs
StatePublished - 28 Feb 1985

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