EU1794-27

Non disponible en dehors du Royaume-Uni et de l'Irlande

Biochem/physiol Actions

NMDA receptor is important for glutamate neurotransmission. It is associated with learning ability and memory. NMDA receptor possesses two different subunits NMDAR1 and NMDAR2. Tyrosine phosphorylation controls the actions of NMDA receptors. It is also known to influence neuronal function.

EU1794-27 is an N-methyl-d-aspartate (NMDA) receptor (NMDAR) positive allosteric modulator (PAM) toward GluN2A/B/C subtypes (EC50/Emax = 1.4 µM/130%/GluN2B, 2.8 µM/230%/GluN2C, 2.4 µM/250%/GluN2D with Glu/Gly = ECmax = 100/30 µM using xenopus oocytes co-expressing rat GluN1 and respective GluN2 subtype; EC50/Emax = 6.3 µM/400%/GluN2B, 5.0 µM/680%/GluN2C with Glu/Gly = 1/0.3 µM &,;2.4 µM/580%/GluN2D with Glu/Gly = 0.6/0.2 µM), while it exhibits Glu/Gly level-dependent GluN1-GluN2A-modulating activities (EC50/Emax = 7.4 µM/52%/GluN2A with Glu/Gly = 100/30 µM; 8.1 µM/340% with Glu/Gly = 2/0.6 µM).