Overview
- Frizelle, P.A. et al. (2006) Mol. Pharmacol. 70, 1022.
Alomone Labs PEAQX tetrasodium hydrate inhibits NMDA (NR1+NR2A) receptors expressed in Xenopus oocytes.A. Time course of NMDA currents elicited with 25 µM glutamate and 25 µM Glycine, every 50 sec, while membrane potential was held at -80 mV. 0.1 µM PEAQX tetrasodium hydrate (#P-255), applied for 2.5 min as indicated, inhibited current amplitude. B. Superimposed current traces taken from the experiment described in A.
PEAQX tetrasodium hydrate (NVP-AAM007) is a competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound shows higher selectivity for NR2A over NR2B subunit-containing receptor. PEAQX IC50 values are strongly dependent on agonist concentration used to evoke response. IC50 for NR1/NR2A were 31 ± 2 nM for EC50 of glutamate, and 214 ± 10 nM for 10-times the EC50 of glutamate. IC50 values for NR1/NR2B were significantly higher: 215 ± 13 nM and 2.2 ± 0.14 μM for EC50 and 10-times the EC50 of glutamate, respectively1.
Several studies claim that PEAQX has the ability to cause a blockade of adult long-term potentiation while only moderately affecting juvenile long-term potentiation. It was shown that subsaturating concentrations of APV (a NMDAR antagonist) can imitate the effects of PEAQX on long-term potentiation. These findings suggest that the synaptic plasticity affected by PEAQX can be explained by nonspecific blockade of NMDA receptors2.
NMDA receptors play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. NMDA receptors mediate several physiological functions including learning and memory formation; they play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease3.
