GluN2B-NMDAR antagonist-1

• CAT Number: I041224
• Molecular Formula: C26H23BrN2O2
• Molecular Weight: 475.38
• Purity: ≥95%
• Synonyms: (E)-N-[2-[1-[(3-bromophenyl)methyl]indol-3-yl]ethyl]-3-(4-hydroxyphenyl)prop-2-enamide
• InChI: InChI=1S/C26H23BrN2O2/c27-22-5-3-4-20(16-22)17-29-18-21(24-6-1-2-7-25(24)29)14-15-28-26(31)13-10-19-8-11-23(30)12-9-19/h1-13,16,18,30H,14-15,17H2,(H,28,31)/b13-10+
• InChIKey: CQRLHYONIXGPET-JLHYYAGUSA-N
• SMILES: C1=CC=C2C(=C1)C(=CN2CC3=CC(=CC=C3)Br)CCNC(=O)C=CC4=CC=C(C=C4)O

GluN2B-NMDAR antagonist-1 is an orally active GluN2B-NMDAR antagonist. GluN2B-NMDAR antagonist-1 has neuroprotective activity. GluN2B-NMDAR antagonist-1 can be used for research of ischemic injury[1].
GluN2B-NMDAR antagonist-1 (Compound Z25) (0.05 μM, 0.5 μM, 5 μM) shows neuroprotection percentage of 35.7%, 48.8%, 55.8% against NMDA-induced cell injury in SH-SY5Y cells[1].
GluN2B-NMDAR antagonist-1 (5 μM) reduces Ca2+ influx in SH-SY5Y cells induced by NMDA (500μM)[1].
GluN2B-NMDAR antagonist-1 (0.05-5 μM, 6 h) increases NMDA-induced down-regulation of p-ERK1/2 expression in SH-SY5Y cells[1].
GluN2B-NMDAR antagonist-1 shows favorable plasma stability, with a half-life value greater than 289.1 min[1].
GluN2B-NMDAR antagonist-1 (Compound Z25) (20-80 mg/kg, intragastric administration) improves cognitive ability in ICV-ET1-induced vascular dementia mice model[1].

Reference

[1]. Quan J,et al. Discovery of novel tryptamine derivatives as GluN2B subunit-containing NMDA receptor antagonists via pharmacophore-merging strategy with orally available therapeutic effect of cerebral ischemia. Eur J Med Chem. 2023 May 5;253:115318.
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