nr2b

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

BZAD01 is a selective NMDA NR1A/2B receptor antagonist.

Co 101244 hydrochloride (4-Piperidinol, 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-Methylphenyl)Methyl]-,hydrochloride) is an NR2B-containing NMDA receptor antagonist.

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

Ro 25-6981 is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit with IC50s of 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Ro 25-6981 can be used in studies about Parkinson's disease.

Eliprodil (SL-820715)(SL-820715), a non-competitive NR2B-NMDA receptor antagonist(IC50: 1 uM), less effective for NR2A- and NR2C-containing receptors(IC50> 100 uM). It has been used in trials studying the treatment of Parkinson Disease and Movement Disorders.

NR1A/NR2B NMDA receptor antagonist,orally active

Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

Sepimostat 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.

Tat-NR2B9c acetate (NA-1 acetate) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c acetate disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c acetate also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

Tat-NR2BAA is an inactive control peptide of Tat-NR2B9c. It shares a similar sequence with Tat-NR2B9c, but possesses a double-point mutation in the COOH terminal tSXV motif. This mutation renders Tat-NR2BAA unable to bind PSD-95. Tat-NR2B9c, on the other hand, is a membrane-permeable peptide that interferes with PSD-95/NMDAR binding. This interference leads to the decoupling of NR2B- and/or NR2A-type NMDARs from PSD-95[1][2].

Tat-NR2BAA TFA serves as the inactive control peptide for Tat-NR2B9c, featuring a comparable sequence with a crucial distinction: a double-point mutation in its COOH-terminal tSXV motif. This alteration renders Tat-NR2BAA TFA unable to bind to PSD-95, in contrast to Tat-NR2B9c. The latter is a membrane-permeant peptide that impedes PSD-95/NMDAR interaction, specifically detaching NR2B- and/or NR2A-type NMDARs from PSD-95 [1].

Tat-HA-NR2B9, comprising an HIV-1 Tat transduction domain fragment, an influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c), has demonstrated efficacy in reducing infarct size and enhancing neurological function following ischemia-induced cerebral injury in rats [1].

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy.

EMD-95885 is a selective antagonist of NMDA receptors containing NR2B subunits, with an IC50 of 3.9 nM. It does not interact with other sites on the NMDA receptor.

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

NMDA-IN-1 is a potent and NR2B-selective antagonist of NMDA, with an NMDA Ki of 0.85 nM and an NR2B Ca2+ influx IC50 of 9.7 nM.

TCN 213 is an antagonist of NMDA receptor that has a selective for NR1/NR2A over NR1/NR2B

Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptor blocker, specifically targeting the NR2B subunit (IC50 values are 0.009 μM for NR1C/NR2B and 52 μM for NR1C/NR2A receptor subunit combinations).

WMS-1405 is a derivative of ifenprodil. As a potent NR2B-selective NMDA receptor antagonist, it exhibits a Ki value of 5.4 nM. Synthesized through a central building block approach, WMS-1405 displays high NR2B affinity due to the specific distance between its basic nitrogen atom and phenyl residue. WMS-1405 has the potential to serve as an NMDA antagonist for excitotoxicity treatment.

TCN 237 serves as an antagonist of NR2B subunit-containing NMDA receptors, with a Ki value of 0.85 nM. It specifically blocks glutamate and glycine-induced currents in whole-cell patch-clamp assays when using L-M(TK-) cells expressing NR2B subunit-containing NMDA receptors. This is in contrast to its effect on L-M(TK-) cells with NR2A- or NR2D subunit-containing receptors and HEK293 cells with NR2C subunit-containing receptors. Additionally, TCN 237 at 3 mg/kg dosage mitigates carrageenan-induced mechanical hyperalgesia in rats.

Satoprodil (example 2) is a potent negative allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor, with an IC50 value of 123 nM specifically targeting NR2B.

NR2B-containing NMDA receptors antagonist