EVT-101 DIHYROCHLORIDE

Biochem/physiol Actions

EVT-101 is a potent and orally active NR2B-subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist (IC₅₀ = 17 nM against 5 nM Ro 25-6981 for binding rat brain membrane) that targets the GluN1/GluN2B dimer interface with a distinctly different binding mode as ifenprodil. EVT 101 potently inhibits current induction by Glu/Gly (100 µM each) in rat GluN1-1a/mouse GluN2B co-expressing xenopus in vitro (IC₅₀ = 12 nM) and blocks MK-801 binding in mouse brain in vivo (3 mg EVT-101/kg p.o. & 0.2 µCi [3H]MK-801/g i.v. administered 55 min and 10 min prior to brain removal, respectively).