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) 在 SH-SY5Y 细胞中对 NMDA 诱导的细胞损伤显示出 35.7%、48.8%、55.8% 的神经保护百分比[1].
GluN2B-NMDAR antagonist-1 (5 μM) 减少 NMDA (500 μM) 诱导的 SH-SY5Y 细胞中的 Ca2+ 内流[1]。
GluN2B-NMDAR antagonist-1 (0.05-5 μM, 6 h) 增加 NMDA 诱导的 SH-SY5Y 细胞中 p-ERK1/2 表达的下调[1]。
GluN2B-NMDAR antagonist-1 具有良好的血浆稳定性，半衰期值大于 289.1 分钟[1]。
Western Blot Analysis[1]
| Cell Line: | SH-SY5Y cells |
| Concentration: | 0.05, 0.5, 5 μM |
| Incubation Time: | 6 h |
| Result: | Increased NMDA-induced down-regulation of p-ERK1/2 expression, and reached the same level as Ifenprodil at 0.5 μM. |
GluN2B-NMDAR antagonist-1 (Compound Z25) (20-80 mg/kg，灌胃) 改善 ICV-ET1 诱导的血管性痴呆小鼠模型中小鼠的认知能力[1]。
| Animal Model: | ICV-ET1-induced vascular dementia mice model[1] |
| Dosage: | 20, 40, and 80 mg/kg |
| Administration: | Intragastric administration, daily. |
| Result: | Decreased escape latency and swimming distance. |
| Animal Model: | Mouse (PK Assay)[1] | |||||||||||||||
| Dosage: | i.v. (1 mg/kg) and p.o. (10 mg/kg) | |||||||||||||||
| Administration: | i.v., p.o. | |||||||||||||||
| Result: | Pharmacokinetic profile of Nemvaleukin alfa.
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[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.