nr2c

QNZ46 is a non-competitive antagonist of NMDA receptors, selectively targeting NR2C/NR2D subunits.

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit, with EC50 values of 2.7 μM for NR2C and 2.8 μM for NR2D.

NMDA agonist 2 (compound 8d) effectively inhibits NMDA receptors, exhibiting an EC50 of 0.034 μM for GluN1/2C. It plays a significant role in neurological and psychiatric disorders.

NMDA receptor potentiator-1 (Compound 1368) is a subunit-selective NMDA receptor enhancer with IC50 values of 4 μM for NR2C and 5 μM for NR2D expression.

Eliprodil (SL-820715)(SL-820715), a non-competitive NR2B-NMDA receptor antagonist(IC50: 1 uM), less effective for NR2A- and NR2C-containing receptors(IC50> 100 uM). It has been used in trials studying the treatment of Parkinson Disease and Movement Disorders.

TCN 237 serves as an antagonist of NR2B subunit-containing NMDA receptors, with a Ki value of 0.85 nM. It specifically blocks glutamate and glycine-induced currents in whole-cell patch-clamp assays when using L-M(TK-) cells expressing NR2B subunit-containing NMDA receptors. This is in contrast to its effect on L-M(TK-) cells with NR2A- or NR2D subunit-containing receptors and HEK293 cells with NR2C subunit-containing receptors. Additionally, TCN 237 at 3 mg/kg dosage mitigates carrageenan-induced mechanical hyperalgesia in rats.

CEB-1604 is an NMDA receptor antagonist. It inhibits NMDA-induced currents in oocytes transfected with NMDA receptor subtypes (NR1/NR2A, NR1/NR2B, NR1/NR2C, NR1/NR2D), showing an IC50 range of 5 to 12 μM. CEB-1604 also abolishes NMDA-dependent epileptiform discharges in rat cortical wedge preparations and mitigates NMDA-induced depolarization effects. This compound is applicable in the research of neurological injury diseases.

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.