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.

A13144

CAS No.

169274-78-6

Ro 25-6981

Ro 25-6981 is a high-affinity, potent and selective blocker of N-methyl- D-aspartate (NMDA) receptors.

Cat. No.

A13576

CAS No.

117928-94-6

Rapastinel (GLYX-13)

Synonyms: GLYX 13

GLYX-13 is a selective weak partial agonist of the glycine site of the NMDA receptor which is under development by Naurex as adjunctive therapy for treatment-resistant depression.

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.

A16083

CAS No.

1312991-76-6

RO 25-6981 maleate

Synonyms: Ro25-6981

Ro 25-6981 Maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 uM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.

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.

A19339

CAS No.

153322-05-5

Lanicemine

Synonyms: AZD6765

Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1 μM.

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.

A20075

CAS No.

1421866-48-9

Apimostinel

Synonyms: NRX-1074; AGN-241660

Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.

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.

A67069

CAS No.

1118-68-9

N,N-Dimethylglycine

Synonyms: Dimethylglycine; DMG; N-Methylsarcosine

N,N-Dimethylglycine is a natural N-methylated glycine that serves as a partial agonist at the N-methyl-D-aspartate receptor (NMDAR) glycine site. It functions as a methyl donor, enhancing immune response and exhibiting antioxidant properties to mitigate oxidative stress by scavenging free radicals. Additionally, N,N-Dimethylglycine has demonstrated antidepressant-like effects and surfactant activity, making it valuable for various research applications in neuropharmacology and immunology.

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.

A67102

CAS No.

46026-75-9

cis-Piperidine-2,3-dicarboxylic acid

Cis-Piperidine-2,3-dicarboxylic acid primarily targets NMDA receptors and acts as a partial agonist. This compound is known for its ability to block general excitatory synaptic transmission by interfering with NMDA, AMPA, and kainate ionotropic receptors. Cis-Piperidine-2,3-dicarboxylic acid is valuable for research applications related to neuropharmacology and the study of synaptic plasticity.

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.

A67104

CAS No.

2151842-64-5

Zelquistinel

Synonyms: AGN-241751; GATE-251

Zelquistinel (AGN-241751) is a potent orally active partial agonist of the N-methyl-D-aspartate (NMDA) receptor. It has demonstrated significant biological activity relevant to the research of neuropsychiatric conditions, including depression and anxiety. Zelquistinel serves as a valuable tool for studying the pharmacological mechanisms underlying these disorders and evaluating potential therapeutic interventions.

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.