hnmda 1a/2a receptors

PEAQX (NVP-AAM077)(NVP-AAM 077) is an effective and orally available NMDA antagonist. It can inhibit human NMDA receptors for 1A/2A(IC50: 270 nM), rather than 1A/2B(29, 600 nM).

PEAQX tetrasodium hydrate (PEAQX tetrasodium hydrate (459836-30-7 free base)) is an orally available NMDA antagonist that is potent and selective. The IC50 value of PEAQX tetrasodium hydrate (459836-30-7 free base) against hNMDAR 1A/2A was 270 nM and 29600 nM against hNMDAR 1A/2B, respectively.

PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests.

(Rac)-PEAQX acts as an antagonist to NMDA receptors. It promotes the activation of caspase-3 and induces apoptosis in cortical striatal slice cultures.