EU1794-4

Biochem/physiol Actions

EU1794-4 is an N-methyl-d-aspartate (NMDA) receptor (NMDAR) allosteric modulator that prevents large degree receptor activation in the presence of high level Glu/Gly (IC50/Emax = 2.2 µM/32%/GluN2A, 2.6 µM/67%/GluN2B, 0.42 µM/52%/GluN2C, 0.36 µM/51%/GluN2D with Glu/Gly = ECmax = 100/30 µM using xenopus oocytes co-expressing rat GluN1 and respective GluN2 subtype), while augmenting receptor activation at low level Glu/Gly (EC50/Emax = 3.9 µM/500%/GluN2A, 4.3 µM/210%/GluN2B, 15 µM/220%/GluN2C with Glu/Gly = 1/0.3 µM; 14 µM/540%/GluN2D with Glu/Gly = 300/9 nM).

EU1794-4 consists of an ethyl ester and lacks a methyl substituent on the tetrahydrobenzothiophene core.