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Identification of a Class of Novel, Selective, Structurally Distinct GluN2A Negative Allosteric Modulators Through

Carlos M Martínez Viturro¹, Robert A Neff², Scott D Bembenek³

¹Johnson & Johnson, Toledo, Spain.

|July 13, 2026

Summary

Researchers developed novel GluN2A-selective negative allosteric modulators for neuropsychiatric disorders. Compound 6m shows promise as a tool for studying GluN2A

Keywords:

GluN2A NAM NMDA PAM allosteric depression glutamate ionotropic virtual screening

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Area of Science:

Neuroscience
Pharmacology

Background:

N-methyl-D-aspartate receptors containing GluN2A subunits are implicated in neuropsychiatric disorders.
Previous GluN2A antagonists faced challenges with specificity and pharmacological profiles, limiting therapeutic development.

Purpose of the Study:

To identify and develop novel, selective GluN2A antagonists.
To overcome limitations of existing compounds, such as poor solubility, glycine sensitivity, and efflux liability.

Main Methods:

Virtual screening of the MPX-007 binding site.
In vitro characterization of novel negative allosteric modulators.
Optimization of a lead compound (6m) for improved properties.

Main Results:

A novel class of GluN2A-selective negative allosteric modulators was identified.
Compound 6m demonstrated an advanced in vitro profile, representing a structurally unique molecule.
The identified compounds address limitations of prior GluN2A antagonists.

Conclusions:

Compound 6m is a promising tool for mechanistic studies of GluN2A.
This novel class of modulators holds potential for exploring therapeutic strategies targeting GluN2A in neuropsychiatric conditions.