PEAQX

• CAT Number: I003605
• CAS Number: 459836-30-7
• Molecular Formula: C17H17BrN3O5P
• Molecular Weight: 454.21
• Purity: ≥95%
• Synonyms: [(S)-[[(1S)-1-(4-bromophenyl)ethyl]amino]-(2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid
• Target: NMDA
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 270 nM(hNMDA A1/A2) [1]

PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).IC50 value: 270 nM(hNMDA A1/A2) [1]Target: NR2A antagonistin vitro: PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM) [1].in vivo: PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35 [2].

Reference

1:The effects of an acute challenge with the NMDA receptor antagonists, MK-801, PEAQX, and ifenprodil, on social inhibition in adolescent and adult male rats. Morales M, Spear LP.Psychopharmacology (Berl). 2014 Apr;231(8):1797-807. doi: 10.1007/s00213-013-3278-3. Epub 2013 Sep 17. PMID: 24043344 Free PMC Article2:Low doses of the NMDA receptor antagonists, MK-801, PEAQX, and ifenprodil, induces social facilitation in adolescent male rats. Morales M, Varlinskaya EI, Spear LP.Behav Brain Res. 2013 Aug 1;250:18-22. doi: 10.1016/j.bbr.2013.04.050. Epub 2013 May 4. PMID: 23651880 Free PMC Article