The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca²⁺ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors.

ABSTRACT: NMDA receptors are ligand-gated ion channels that mediate a slow, Ca²⁺-permeable component of excitatory synaptic currents. These receptors are involved in several important brain functions, including learning and memory, and have also been implicated in neuropathological conditions and acute central nervous system injury, which has driven therapeutic interest in their modulation. The EU1794 series of positive and negative allosteric modulators of NMDA receptors has structural determinants of action near the preM1 helix that is involved in channel gating. Here, we describe the effects of the negative allosteric modulator EU1794-4 on GluN1/GluN2A channels studied in excised outside-out patches. Coapplication of EU1794-4 with a maximally effective concentration of glutamate and gl

SUBMITTER: Perszyk RE 

PROVIDER: S-EPMC8058507 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature