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PEAQX shows 5‑fold receptor affinity difference and 270 nM IC50 for NMDA 1A/2A, key for neuroscience studies.
PEAQX, a competitive NMDA receptor antagonist, exhibits a 5‑fold affinity gap between GluN1/GluN2A and GluN1/GluN2B receptors, a detail that refines earlier claims of 100‑fold selectivity [1].
| At a glance | |
|---|---|
| Receptor affinity gap | 5‑fold (GluN1/GluN2A vs. GluN1/GluN2B) |
| IC₅₀ (hNMDA 1A/2A) | 270 nM |
| IC₅₀ (hNMDA 1A/2B) | 29.6 µM |
| Primary use | Research‑grade NMDA antagonist |
Early reports described PEAQX as 100‑fold selective for GluN1/GluN2A receptors, but more detailed Ki measurements show the selectivity is only five‑fold [1]. This adjustment aligns with data from the NCATS substance database, which lists an IC₅₀ of 270 nM for the 1A/2A subtype and 29.6 µM for the 1A/2B subtype [2]. The compound is also noted for its potent anticonvulsant activity in animal models [1].
PEAQX is supplied for laboratory use only, with typical in‑vitro concentrations ranging from 3 µM to 5 µM to induce apoptosis or inhibit calcium influx in neuronal cultures [3][4]. In vivo studies report sub‑cutaneous doses of 10–40 mg/kg producing dose‑dependent increases in caspase‑3 activity and improvements in motor function in rats [4]. These findings support its role in probing NMDA‑mediated pathways and evaluating neuroprotective strategies.
Key metrics
| Metric | Value |
|---|---|
| Molecular weight | 454.21 g mol⁻¹ |
| CAS number | 459836‑30‑7 |
| Purity (batch) | >98 % |
The clarified selectivity and potency metrics of PEAQX sharpen its utility as a tool compound for dissecting NMDA receptor subunit functions, but the gap between pre‑clinical promise and therapeutic application remains to be bridged.
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