Sodium ions allosterically modulate the M2 muscarinic receptor

Sheli Friedman, Merav Tauber, Yair Ben-Chaim

Research output: Contribution to journalArticlepeer-review


G protein coupled receptors (GPCRs) play a key role in the vast majority of cellular signal transduction processes. Previous experimental evidence has shown that sodium ion (Na+) allosterically modulate several class A GPCRs and theoretical studies suggested that the same also holds true for muscarinic receptors. Here we examined, using Xenopus oocytes as an expression system, the effect of Na+ on a prototypical GPCR, the M2 muscarinic receptor (M2R). We found that removal of extracellular Na+ resulted in a decrease in the potency of ACh toward the M2R and that a conserved aspartate in transmembrane domain 2 is crucial for this effect. We further show that this allosteric effect of Na+ does not underlie the voltage-dependence of this receptor.

Original languageEnglish
Article number11177
JournalScientific Reports
Issue number1
StatePublished - 1 Dec 2020

Bibliographical note

Funding Information:
This work was supported by an internal Grant from the Open University of Israel.

Publisher Copyright:
© 2020, The Author(s).


Dive into the research topics of 'Sodium ions allosterically modulate the M2 muscarinic receptor'. Together they form a unique fingerprint.

Cite this