NMDA Receptors

Cat. No.

A11842

CAS No.

60-27-5

Creatinine

Synonyms: NSC13123

Creatinine acts as a GABAA and NMDA receptor modulator, demonstrating antioxidant properties and metabolic regulation. It is produced through the non-enzymatic conversion of creatine and phosphocreatine in muscle, making its serum levels an important biomarker for renal function, muscle mass, and clinical outcomes. Creatinine is utilized in evaluating perioperative renal risk and has applications in research on neurodegenerative diseases, psychiatric disorders, acute and chronic kidney injury, and renal failure. Additionally, it can induce specific Cryptococcus species to produce creatinine deiminase, highlighting its role in metabolic studies.

Cat. No.

A12757

CAS No.

1883518-31-7

GNE 0723

GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.

Cat. No.

A15523

CAS No.

486427-17-2

CIQ

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit.

Cat. No.

A16672

CAS No.

7491-74-9

Piracetam

Synonyms: UCB-6215

Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA) that functions as an iGluR modulator. It exhibits significant neuroprotective and cognitive-enhancing properties, making it valuable in the study of various cognitive disorders. Piracetam is widely used in research to investigate mechanisms underlying memory enhancement, learning processes, and neuroplasticity.

Cat. No.

A19770

CAS No.

1801151-09-6

BMS-986163

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

Cat. No.

A20295

CAS No.

2026635-66-3

GNE 5729

GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.

Cat. No.

A22610

CAS No.

380560-89-4

DQP-1105

DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

Cat. No.

A36677

CAS No.

1849603-79-7

SBI-810

SBI-810 is a selective modulator of the neurotensin receptor 1 (NTSR1), characterized by its ability to penetrate the blood-brain barrier. This compound promotes β-arrestin-2 recruitment to NTSR1 while antagonizing Gq-mediated signaling pathways. SBI-810 effectively inhibits NMDA receptor activity and ERK signaling in spinal nociceptive neurons, leading to a reduction in excitatory synaptic transmission, surface expression of Nav1.7, and action potential firing in primary sensory neurons. Its profound effects on C-fiber responses demonstrate its potential in alleviating acute and chronic pain, making it a valuable tool for research into various pain disorders.

Cat. No.

A67060

CAS No.

1210899-51-6

UCM-A86

UCM-A86 is a selective positive allosteric modulator of the GluN1/GluN3 NMDA receptors, exhibiting EC50 values of 21 µM and 19 µM for GluN1/GluN3A and GluN1/GluN3B receptors, respectively. This compound preferentially enhances signaling through GluN1/GluN3A/B receptors while displaying minimal activity at GluN1/GluN2A-D receptors. UCM-A86 serves as a valuable tool for research focused on central nervous system disorders and the modulation of NMDA receptor activity.

Cat. No.

A67082

CAS No.

2480226-07-9

Simufilam hydrochloride

Synonyms: PTI-125 hydrochloride

Simufilam hydrochloride is an orally active modulator of filamin A (FLNA) that targets neuronal signaling pathways. This compound restores NMDAR signaling and Arc expression while inhibiting dysregulated mTOR activity. Additionally, it enhances insulin sensitivity and mitigates Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride is applicable in research related to Alzheimer's disease, particularly in understanding the underlying mechanisms of neurodegeneration.

Cat. No.

A67094

CAS No.

2378285-59-5

Plazinemdor

Synonyms: CAD-9303

Plazinemdor is a positive allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor. This compound enhances NMDA receptor activity, making it a valuable tool for investigating its role in psychiatric, neurological, and neurodevelopmental disorders. Plazinemdor is suitable for research applications focused on understanding the underlying mechanisms of various nervous system diseases.

Cat. No.

A67098

CAS No.

1435786-04-1

Rapastinel Trifluoroacetate

Synonyms: GLYX-13 Trifluoroacetate

Rapastinel Trifluoroacetate is a modulator of the NMDA receptor, functioning as a partial agonist at the glycine site. This compound has shown potential for the treatment of major depressive disorder, contributing to neuroplasticity and synaptic function. It is utilized in research exploring depression and related neurological conditions, providing insights into the therapeutic effects of NMDA receptor modulation.

Cat. No.

A67103

CAS No.

2315311-83-0

GNE-9278

GNE-9278 is a selective positive allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), targeting the GluN1 transmembrane domain. It enhances peak current and agonist affinity in activated NMDARs, offering potential insights into synaptic transmission and plasticity. This compound is valuable for research investigating NMDAR-related neurological disorders and synaptic function.

Cat. No.

A67113

CAS No.

1224591-33-6

Simufilam

Synonyms: PTI-125

Simufilam is an orally active modulator of filamin A (FLNA) that restores NMDA receptor (NMDAR) signaling and Arc expression. It effectively inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, which results in improved insulin sensitivity and a reduction in Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. This compound is particularly valuable for research applications focused on Alzheimer's disease and related neurodegenerative disorders.

Cat. No.

A67120

CAS No.

2377187-09-0

DQP-997-74

DQP-997-74 is a selective negative allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), specifically targeting the GluN2C and GluN2D subunits with IC50 values of 0.069 μM and 0.035 μM, respectively. This compound exhibits blood-brain barrier penetrability and demonstrates synergistic effects with glutamate, resulting in enhanced inhibition of hypersynchronous neural activity under high-frequency excitatory synaptic transmission. DQP-997-74 has shown potential to reduce epileptogenesis in murine models of tuberous sclerosis complex (TSC)-induced epilepsy, making it a valuable tool for research on NMDAR-related neurological disorders.

Cat. No.

A67126

CAS No.

2759182-59-5

Neboglamine hydrochloride

Synonyms: CR-2249 hydrochloride; XY-2401 hydrochloride

Neboglamine hydrochloride is a positive modulator of the glycine site on the NMDA receptor, facilitating increased receptor activity. This compound has demonstrated potential in addressing aspects of schizophrenia and related neurological disorders. Researchers can utilize Neboglamine hydrochloride to explore its effects on synaptic transmission and neuroplasticity, contributing to a deeper understanding of NMDA receptor dynamics in psychiatric conditions.

Cat. No.

A67145

CAS No.

1698901-76-6

GNE-8324

GNE-8324 is a selective positive allosteric modulator of the GluN2A subtype of NMDA receptors. This compound enhances NMDA receptor-mediated synaptic responses specifically in inhibitory neurons, while sparing excitatory neurons. GNE-8324 has potential applications in studying synaptic function and neuropharmacology, particularly in the context of cognitive disorders and neurodegenerative diseases.

Cat. No.

A67148

CAS No.

2012536-16-0

NYX-2925

NYX-2925 is an orally active NMDAR modulator that specifically restores activated Src and its phosphorylation sites on GluN2A and GluN2B in the medial prefrontal cortex. This compound does not affect CAMKII and is devoid of addictive, sedative, or ataxic side effects. NYX-2925 is a valuable tool for investigating NMDA receptor-related central nervous system disorders.

Cat. No.

A67153

CAS No.

1449373-99-2

DQP-26

DQP-26 is an effective negative allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR), specifically targeting the GluN2C and GluN2D subunits with IC50 values of 0.77 μM and 0.44 μM, respectively. This compound is valuable for investigating the role of NMDAR in neurological diseases, providing insights into potential therapeutic avenues for treating conditions associated with dysregulation of this receptor.

Cat. No.

A67167

CAS No.

1698900-69-4

GNE 6901

GNE 6901 is a potent positive allosteric modulator (PAM) of the GluN2A subunit of the NMDA receptor (NMDAR), exhibiting an EC50 value of 382 nM. This compound enhances NMDAR activity and is valuable for research into neurological disorders, synaptic plasticity, and cognitive function. GNE 6901 can be utilized in studies aimed at understanding the role of GluN2A in synaptic transmission and the potential therapeutic effects in various neurodegenerative conditions.

Cat. No.

A67172

CAS No.

1892581-29-1

Onfasprodil

Synonyms: MIJ-821

Onfasprodil is a selective negative allosteric modulator (NAM) of the NMDA receptor NR2B subunit. It effectively diminishes the activity of NR2B-containing NMDA receptors, contributing to its rapid antidepressant effects. This compound is primarily utilized in research focused on treatment-resistant depression (TRD).

Cat. No.

A67190

CAS No.

2199-87-3

UBP608

UBP608 is a potent negative allosteric modulator of N-Methyl-D-aspartate receptors (NMDARs). This compound has demonstrated significant biological activity in modulating NMDAR function, making it a valuable tool for investigating neurological disorders. Its mechanism of action offers insights into synaptic transmission and neuroplasticity, facilitating research into therapeutic strategies for various cognitive and behavioral conditions.

Cat. No.

A67191

CAS No.

163000-63-3

Neboglamine

Synonyms: CR-2249; XY-2401

Neboglamine is an N-methyl-D-aspartate (NMDA) receptor modulator that enhances neuronal activity in key brain regions including the prefrontal cortex, nucleus accumbens, and lateral septal nucleus. This compound has been shown to increase the levels of fos-like immunoreactivity (FLI)-positive cells and effectively restores NMDA-mediated neurotransmitter release. Additionally, Neboglamine demonstrates the ability to inhibit hyperlocomotion induced by phencyclidine, highlighting its potential for research in neuropharmacology and neuropsychiatric disorders.

Cat. No.

A67200

CAS No.

1560894-05-4

PYD-106

PYD-106 is a selective positive allosteric modulator of GluN2C-containing NMDA receptors. This compound enhances the frequency and duration of single-channel currents induced by full agonists while displaying only modest modulation of glutamate and glycine efficacy. Notably, PYD-106 specifically boosts the activity of diheteromeric GluN1/GluN2C receptors without affecting triheteromeric GluN1/GluN2A/GluN2C receptors. Its unique mechanism holds promise for research focused on synaptic transmission and neuropharmacology.

Cat. No.

A67210

CAS No.

2416269-15-1

Satoprodil

Satoprodil is a potent negative allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor, specifically targeting the NR2B subunit with an IC50 value of 123 nM. This compound exhibits significant biological activity in regulating glutamatergic neurotransmission and has potential research applications in neuropharmacology, particularly in the study of pain, mood disorders, and neurodegenerative diseases.