CAY10608

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).¹ 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.¹ 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.¹

1. Tahirovic, Y.A., Geballe, M., Gruszecka-Kowalik, E., et al. Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists J. Med. Chem. 51,5506-5521(2008).