NMDA Receptors

Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.

IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation.

ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.

MN-05 is a dual neuroprotective and vasodilatory inhibitor of the NMDA receptor. By blocking calcium influx, it reduces free radical production and preserves mitochondrial membrane potential in cortical neurons exposed to glutamate. Additionally, MN-05 exhibits vasodilatory effects by dilating aortic rings in response to phenylephrine-induced contraction. This compound demonstrates protective properties against glutamate-induced neuronal injury in vitro, making it valuable for research in neurodegenerative diseases.

TAT-CBD3 is a 15-amino acid peptide derived from CRMP2 that incorporates the TAT cell-penetrating motif from HIV-1, enabling efficient cellular uptake. This peptide disrupts the interaction between CRMP2 and NMDA receptors (NMDAR) while maintaining NMDAR localization. TAT-CBD3 is valuable for research applications focused on neurobiology and synaptic signaling, particularly in studies investigating the role of CRMP2 in neuronal function and related disorders.

(R)-CPP is a potent antagonist of the NMDA receptor, effectively inhibiting its activity. It is utilized in various research applications related to neuropharmacology and the study of excitatory neurotransmission. This compound is important for exploring the role of NMDA receptors in neurological disorders and for evaluating potential therapeutic interventions.

BZAD-01 is a selective inhibitor of the NMDA NR2B subunit, exhibiting a Ki value of 72 nM. This compound demonstrates significant biological activity by improving postural asymmetry and reducing Apomorphine-induced rotation. BZAD-01 is utilized in research applications focused on neurological disorders and synaptic transmission modulation.

Antidepressant agent 9 is an orally active NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. This compound demonstrates good metabolic stability and significant plasma exposure, making it suitable for in vivo studies. Antidepressant agent 9 has been shown to exhibit antidepressant-like effects in the mouse forced swim test, highlighting its potential application in depression research.

5-Chloro-1,4-dihydro-2,3-quinoxalinedione is a weak inhibitor of the NMDA receptor, exhibiting an IC50 value of 56.3 μM. This compound is relevant for investigations into neurological disorders, particularly in understanding excitotoxicity and synaptic plasticity. Its role in modulating NMDA receptor activity makes it a valuable tool for research in neuropharmacology.

NR2B-selective NMDA receptor antagonist 1 is a potent inhibitor of the NR1/NR2B NMDA receptor with an IC50 of 0.05 μM. It demonstrates selectivity against other targets such as hERG and α1-AdR, with IC50 values of 0.73 μM and 2.4 μM, respectively. This compound exhibits excellent permeability across the blood-brain barrier, making it a valuable tool for research into neuropharmacology and the therapeutic exploration of NMDA receptor-related disorders.

Fluorolintane is a potent NMDA receptor inhibitor, with a Ki value of 87.92 nM. This compound effectively disrupts prepulse inhibition in rat models, demonstrating its capacity to modulate synaptic transmission. Additionally, Fluorolintane inhibits NMDA receptor-induced field excitatory postsynaptic potentials in rat hippocampal slices, making it a valuable tool for studying excitatory neurotransmission and its implications in neurological research.

AChE-IN-53 is a potent inhibitor of the NMDA receptor (NMDAR), which plays a key role in mediating excitatory synaptic transmission and is implicated in various neurological disorders. This compound exhibits significant neuroprotective effects and has shown potential in behavioral research applications related to cognitive decline and neurodegenerative conditions. AChE-IN-53 can be utilized to explore therapeutic strategies targeting NMDAR dysregulation in various models of neural injury and disease.

NMDA-IN-2 is a selective NMDA receptor 2B subtype inhibitor derived from Procaine. It demonstrates potent inhibitory effects on NMDA receptor activity, making it valuable for studying synaptic transmission and neurotoxicity. This compound has applications in researching neurological disorders and may aid in the development of therapeutic strategies for conditions associated with NMDA receptor dysregulation.

UBP618 is a non-selective N-methyl-D-aspartate (NMDA) receptor inhibitor. This compound exhibits significant modulation of NMDA receptor activity, making it valuable for studying excitatory neurotransmission and various neurological disorders. UBP618 is utilized in research addressing conditions such as Alzheimer's disease, schizophrenia, and other neurodegenerative disorders, providing insights into synaptic plasticity and neuroprotection mechanisms.

Pregnanolone sulfate (pyridinium) is an endogenous neurosteroid that functions as an inhibitor of NMDA receptors. This compound exhibits neuroprotective properties, making it a valuable tool for investigating neurodegenerative disorders and synaptic plasticity. Its ability to modulate excitatory neurotransmission highlights its potential applications in both basic research and therapeutic development.

Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions.

Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management.