Abstract
Background and Purpose Voltage sensitivity is a common feature of many
membrane proteins, including some G-protein coupled receptors (GPCRs).
However, the functional consequences of voltage sensitivity in GPCRs are
not well understood. Experimental approach In this study, we
investigated the voltage sensitivity of the post-synaptic metabotropic
glutamate receptor mGlu5 and its impact on synaptic transmission. Using
biosensors and electrophysiological recordings in non-excitable HEK293T
cells or neurons. Key Results We found that mGlu5 receptor function is
optimal at resting membrane potentials. We observed that membrane
depolarization significantly reduced mGlu5 receptor activation,
Gq-PLC/PKC stimulation, Ca2+ release, and mGlu5 receptor-gated currents
through TRPC6 channels or NMDA receptors. Notably, we report a
previously unknown activity of the NMDA receptor at the resting
potential of neurons, enabled by mGlu5. Conclusions & Implications Our
findings suggest that mGlu5 receptor activity is directly regulated by
membrane voltage which may have a significant impact on synaptic
processes and pathophysiological functions.