nr2b-nmda

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.

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).

Ifenprodil is a selective NMDA receptor (glutamate) antagonist.

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.

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).

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.

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.

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.

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.

NR2B-containing NMDA receptors antagonist

σ receptor agonist and NR2B subunit-selective NMDA receptor antagonist

BMT-108908 is a Negative Allosteric Modulator. It is selective for the NR2B Subtype of The NMDA Receptor Impair Cognition in Multiple Domains.

Ro 25-6981 HCl is an effective and selective NMDA glutamate receptors containing the NR2B subunit antagonist.

Besonprodil is a drug that acts as an NMDA antagonist and is selective for the NR2B subunit.

CP-283097 is an N-methyl-D-aspartic acid (NMDA) receptor antagonist with NR2B subunit.

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, 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.

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.

EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.

Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and partially inhibited by competitive glutamate recognition site antagonists. Complementary high-resolution autoradiographic images using [3H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low.