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).
Potent and orally active NR2B-/GluN2B-subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist with in vitro and in vivo efficacy.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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N-methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play key roles in brain physiology and pathology. Because numerous pathologic conditions involve NMDAR overactivation, subunit-selective antagonists hold strong therapeutic potential, although clinical successes remain limited. Among the most promising NMDAR-targeting drugs
European journal of pharmacology, 766, 1-8 (2015-09-02)
N-methyl-D-aspartate (NMDA) receptor antagonists, including open channel blockers and GluN2B receptor subtype selective antagonists, have been developed for the treatment of depression. The current study investigated effects of systemically administered NMDA channel blockers and GluN2B receptor antagonists on NMDA receptor
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 60(8), 1167-1173 (2019-01-27)
The study aims to investigate the performance characteristics of the enantiomers of 11C-Me-NB1, a recently reported PET imaging probe that targets the GluN2B subunit of N-methyl-d-aspartate (NMDA) receptors. Methods: Reference compound Me-NB1 (inhibition constant for hGluN1/GluN2B, 5.4 nM) and the
Journal of nuclear medicine : official publication, Society of Nuclear Medicine (2018-07-22)
The previously reported carbon-11 labeled GluN2B PET radioligand 11C-Me-NB1 served as a starting point for derivatization and led to the successful development of a radiofluorinated analogue designated (R)-18F-OF-Me-NB1. Given the short physical half-life of 20.3 min for carbon-11, (R)-18F-OF-Me-NB1 with
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