NMDA Receptor Modulators in QPatch - Sophion

NMDA Receptor Modulators in QPatch

Author(s): Ezio Bettini, Laura Aldegheri, Laura Castelletti, Mauro Corsi and Caterina Virginio

N-methyl-D-aspartate receptors (NMDARs) are ionotropic glutamate receptors permeable to Ca2+, Na+ and K+. To be activated, they need to bind to glutamate (via GluN2 subunits), glycine (via GluN1) and release the Mg2+ blockade by
membrane depolarization. The majority of NMDARs are tetrameric complexes, consisting of two glycine-binding GluN1 subunits and two glutamate-binding GluN2 subunits. GluN1 is coded by a single gene with at least eight different splice variants; four different GluN2 genes originate GluN2A, GluN2B, GluN2C, and GluN2D subunits. NMDARs containing different GluN2 subunits have different pharmacological and kinetic properties.

NMDA receptor modulators can be studied using a variety of techniques.