glun2b

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor, demonstrating negative modulation by inhibiting receptor activity and exhibiting high selectivity towards the GluN2B subunit, with an IC50 value of 31 nM.

GluN2B-NMDAR Antagonist-1, an orally active compound, functions as a GluN2B-NMDAR antagonist with neuroprotective properties. It is applicable in the research of ischemic injury [1].

TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, protecting neurons against oxidative stress and NMDAR-mediated excitotoxicity, making it valuable for neuroprotection research studies [1].

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

BMS-986169 is a high-affinity and selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 24 nM in oocytes, and exhibits antidepressant-like activity in mice, making it a potential treatment for treatment-resistant depression.

BMT-108908 FA is a selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 4.2 nM in oocytes and antidepressant-like activity in mice, and can be used for treatment-resistant depression.

(S)-BMT 108908 FA is the enantiomer of BMT 108908. BMT-108908 FA is a selective negative allosteric modulator of the NMDA receptor GluN2B subunit.

Ifenprodil (RC61-91) is an inhibitor of the NMDA receptor, specifically of GluN1 (glycine-binding NMDA receptor subunit 1) and GluN2B (glutamate-binding NMDA receptor subunit 2) subunits. Additionally, Ifenprodil inhibits GIRK channels and interacts with alpha1 adrenergic, serotonin, and sigma receptors.

Rislenemdaz (CERC-301) (CERC-301) is an antagonist of the N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B).

BMS-986163, a negative allosteric modulator of GluN2B, rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM) as a prodrug.

Lu AF90103 (Compound 42e) is the methyl ester prodrug of compound 42d, capable of crossing the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1 GluN2B complex, with an efficacy of 24% and an EC50 value of 78 nM. Lu AF90103 plays a significant role in neuropsychiatric disorder research.

NMDA agonist 1 (compound 42d) is a potent NMDA agonist with a Ki value of 96 nM. It acts as a partial agonist of the GluN1 GluN2B complex, exhibiting an EC50 value of 78 nM.

GluN2A Allosteric modulator 1 (Compound 11) is an orally bioavailable compound that effectively crosses the blood-brain barrier and functions as a highly selective negative allosteric modulator of GluN2A. It exhibits an IC50 of 0.042 μM for GluN2A and 13 μM for GluN2B. This compound is useful for research in neurological disorders.

(3S,6R)-NML is an NMDA receptor antagonist with pIC50 values of 4.8 [GluN1-GluN2A], 4.6 [GluN1-GluN2B], 5.0 [GluN1-GluN2C], and 5.0 [GluN1-GluN2D]. It is applicable in the study of depression.

MDAR IN-1 (Compound 5m) is a brain-penetrant acetylcholinesterase (AChE) inhibitor and an antagonist of the NMDAR receptor GluN1/GluN2B subtype. It effectively inhibits AChE activity, enhances cholinergic neurotransmission, and blocks NMDAR to reduce excitotoxicity. MDAR IN-1 shows potential for Alzheimer’s disease research.

EU 1622-240 is an allosteric modulator with a preference for GluN2B, GluN2C, and GluN2D, exhibiting EC50 values of 0.57, 0.82, and 1.1 μM, respectively. It possesses favorable physicochemical properties, along with in vitro stability and permeability.

FLY26 is a selective partial antagonist of GluN2B, with an IC50 value of 0.64 μM. FLY26 inhibits the GluN2B subunit of NMDA receptors, reducing calcium ion influx and reactive oxygen species (ROS) production. It also activates the BDNF/TrkB/CREB neuroprotective signaling pathway, mitigating excitotoxicity and mitochondrial dysfunction. FLY26 holds potential for treating neurological deficits caused by cerebral ischemia-reperfusion injury.

DQP 1105 is a NMDA receptor antagonist.

NR2B-containing NMDA receptors antagonist

GNE-3476 is an NMDA receptor PAM. Ge-3476 has different degrees of activity on different receptors.GNE-3476 has relatively low efficacy on GluN2A, some activity as an AMPAR PAM, and weak activity at GluN2B-containing receptors.

NAB-14 is a powerful and selective chemical compound that acts as a non-competitive antagonist for GluN2C and GluN2D receptors. With an IC50 value of 580 nM for GluN1 GluN2D, NAB-14 demonstrates high potency. This compound exhibits a remarkable selectivity of more than 800-fold towards recombinant GluN2C and GluN2D when compared to GluN2A and GluN2B. Furthermore, NAB-14 possesses the ability to penetrate the blood-brain-barrier effectively [1].

PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1 GluN2A receptors vs. GluN1 GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1 GluN2A vs. GluN1 GluN2B receptors. It is also a potent anticonvulsant in animal tests.

1. Praeruptorin C has been widely used as an antioxidant and a calcium antagonist to treat diseases. 2. Praeruptorin C partially protects cortical neurons by inhibiting the expression of GluN2B-containing NMDA receptors and regulating the Bcl-2 family. 3.

EVT-101 is a GluN2B antagonist, binding at the same GluN1 GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.