Pharmacological modulation of NMDA receptor activity and the advent of negative and positive allosteric modulators.

ABSTRACT: The NMDA receptor (NMDAR) family of l-glutamate receptors are well known to have diverse roles in CNS function as well as in various neuropathological and psychiatric conditions. Until recently, the types of agents available to pharmacologically regulate NMDAR function have been quite limited in terms of mechanism of action and subtype selectivity. This has changed significantly in the past two years. The purpose of this review is to summarize the many drug classes now available for modulating NMDAR activity. Previously, this included competitive antagonists at the l-glutamate and glycine binding sites, high and low affinity channel blockers, and GluN2B-selective N-terminal domain binding site antagonists. More recently, we and others have identified new classes of NMDAR agents that are ei

SUBMITTER: Monaghan DT 

PROVIDER: S-EPMC3360989 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature