nr2b n-methyl-d-aspartate

Rislenemdaz (CERC-301) (CERC-301)是 N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) 的拮抗剂。

Sepimostat 通过 NR2B 亚基的 Ifenprodil 结合位点的 NR2B N-甲基-D-天冬氨酸受体拮抗作用表现出神经保护活性。它抑制 Ifenprodil 结合的 Ki 值为27.7 µM。

Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 μM[1]. Sepimostat (1 to 100 nmol eye, intravitreal injection) exhibits significant neuroprotective effect[1]. Animal Model: Male Sprague Dawley rats weighing 150-300 g[1]. [1]. Masahiro Fuwa, et al. Nafamostat and Sepimostat Identified as Novel Neuroprotective Agents via NR2B N-methyl-D-aspartate Receptor Antagonism Using a Rat Retinal Excitotoxicity Model. Sci Rep. 2019 Dec 31;9(1):20409.

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.

Nelonemdaz potassium (also known as Salfaprodil) is a potent NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). This compound exhibits remarkable neuroprotection against cell death induced by both NMDA and free radicals, in addition to its role as a free radical scavenger.

CJ 036878 was developed as an antagonist of the N-methyl-D-aspartate receptor NR2B subunit.

HSD17B13-IN-7（compound 1）是一种含氟苯酚化合物和高效的HSD17B13抑制剂，对 β-雌二醇和白三烯 B4 的 IC50 分别为 0.18 μM 和 0.25 μM。此外，HSD17B13-IN-7 也是 N-甲基-D-天冬氨酸（NMDA）NR2B 受体拮抗剂，具有在非酒精性脂肪肝研究中的应用潜力。

Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit.