Catalog No.
Product Name
Application
Product Information
Citations
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Gly/NMDA Receptor Antagonist
CGP-78608 is a highly selective antagonist targeting the glycine-binding site of the NMDA receptor, exhibiting a formidable IC50 of 6 nM. This compound acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Additionally, CGP-78608 demonstrates significant anticonvulsant properties, making it a valuable research tool for studies involving excitatory neurotransmission and seizure disorders. -
NMDAR Antagonist
Kaitocephalin acts as an antagonist of the N-methyl-D-aspartate receptor (NMDAR) with Ki values of 7.8 nM for NMDAR, 590 nM for AMPA receptors (AMPAR), and 14,000 nM for kainate receptors (KAR). This compound exhibits neuroprotective effects by inhibiting excitotoxicity, thereby providing a protective mechanism for neurons. Kaitocephalin is valuable for research into neurological diseases, particularly Alzheimer's disease, making it a significant tool for studying excitotoxic pathways and neurodegenerative processes. -
NMDA Receptor Antagonist
CEB-1604 is a selective NMDA receptor antagonist that effectively inhibits NMDA-induced currents in oocytes expressing various NMDA receptor isoforms, including NR1/NR2A, NR1/NR2B, NR1/NR2C, and NR1/NR2D, with IC50 values between 5 to 12 μM. This compound attenuates NMDA-dependent epileptiform discharges in rat cortical wedge preparations and mitigates NMDA's depolarizing effects. CEB-1604 is useful for research into neurological disorders and contributes to the understanding of excitotoxicity-related mechanisms. -
NMDA Antagonist
L-AP5 (L-2-Amino-5-phosphonovaleric acid) is an NMDA receptor antagonist, acting primarily by blocking the NMDA-mediated synaptic transmission. It exhibits weak activity in inhibiting amino acid uptake and synaptic transmission, making it a useful tool in neuropharmacological research. L-AP5 is commonly employed to investigate the roles of NMDA receptors in various neurological processes and disorders, providing insights into excitotoxicity and synaptic plasticity. -
NMDA Receptor Antagonis
GPI-3000 is an NMDA receptor antagonist that demonstrates neuroprotective effects and has the potential to ameliorate metabolic injury. This compound is relevant for research applications focused on metabolic and neurological diseases, providing insights into therapeutic strategies for these conditions. -
NMDAR Modulator
Rapastinel acetate is a modulator of the N-methyl-D-aspartate (NMDA) receptor, exhibiting potent and long-acting antidepressant effects. It enhances long-term potentiation (LTP) of synaptic transmission by transiently increasing NMDA receptor-mediated currents in hippocampal and medial prefrontal cortex pyramidal neurons. Notably, Rapastinel acetate enhances NMDA receptor currents at low concentrations while decreasing them at higher concentrations, reflecting its unique interaction with distinct sites on the NMDA receptor complex. This modulation is associated with a reduced affinity to intracellular calcium inactivation sites, providing insights into its mechanism for augmenting NMDA receptor conductance. -
NMDA Receptor Antagonist
Ro 8-4304 is a non-competitive antagonist of the NMDA receptor, exhibiting voltage-independent and state-dependent inhibition. This compound effectively inhibits NMDA-induced currents with IC50 values of 2.3 μM at 10 μM and 0.36 μM at 100 μM concentrations. Ro 8-4304 is a valuable tool for investigating the role of NMDA receptors in neuropharmacology and related research applications. -
NMDA Antagonist
Neramexane mesylate is a potent antagonist of N-methyl-D-aspartate (NMDA) receptors and α9α10 cholinergic nicotinic receptors. This compound demonstrates significant neuroprotective effects and has been investigated for its potential to alleviate symptoms of moderate to severe tinnitus. Its unique mechanism makes it a valuable tool in neurological research, particularly in studies focusing on auditory disorders and neuroprotection. -
NMDAR Antagonist
NMDA receptor antagonist 5 is a potent antagonist of the NMDA receptor, exhibiting brain permeability and non-toxicity. This compound is particularly useful for investigating neurological disorders and studying synaptic transmission and plasticity. Its ability to modulate NMDA receptor activity makes it a valuable tool for researchers focusing on excitatory neurotransmission and related pathologies. -
L-HCA Antagonist, NMDA Antagonist
(2R,3S)-Chlorpheg is a weak antagonist of L-homocysteic acid (L-HCA) and acts on NMDA receptors. It exhibits inhibitory effects on L-HCA-induced depolarization, making it useful for studying excitatory neurotransmission. Additionally, its role as an NMDA antagonist provides insights into the modulation of synaptic plasticity and various neurological conditions. This compound is valuable for researchers investigating glutamate receptor signaling and related pathways. -
NMDA Receptor Antagonist
Conantokin G is a 17-amino-acid peptide that acts as a potent and selective competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. It effectively inhibits NMDA-evoked currents in murine cortical neurons with an IC50 value of 480 nM. This compound exhibits neuroprotective properties, making it valuable for research in neurobiology and the study of excitotoxicity. -
NMDA Antagonist
DL-AP7 is a competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, playing a significant role as an anticonvulsant. It effectively blocks NMDA-induced convulsions and is utilized in research to explore its effects on learning and memory, particularly in passive avoidance tasks in murine models. This compound serves as a valuable tool for studying neurological conditions and the underlying mechanisms of synaptic plasticity. -
NMDA Receptor Channel Blocker
NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM, characterized by rapid on-off kinetics and strong voltage dependence, without competing with glutamate or glycine. This reagent effectively prevents glutamate/NMDA-induced intracellular Ca2+ overload and modulates the glutamate-nitric oxide-cGMP signaling pathway. NMDAR blocker 1 has been demonstrated to impede excitotoxic neurodegeneration in cultured cerebellar and hippocampal neurons, as well as mitigate excitotoxic effects in a mouse model of hyperammonemia-induced toxicity. It serves as a valuable tool for research into neurodegenerative diseases. -
NMDA Receptor Antagonist
Ro 8-4304 hydrochloride is a selective antagonist targeting the NMDA receptor, specifically inhibiting the NR2B subunit. This compound exhibits non-competitive and voltage-independent antagonistic properties. It is utilized in research applications related to neuropharmacology and studies of synaptic plasticity, providing insights into mechanisms underlying neurological disorders. -
NMDAR Inhibitor
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. -
GluN2B-NMDAR Positive Allosteric Modulator
GluN2B-NMDAR Allosteric Modulator 1 is a selective positive allosteric modulator of the GluN2B subunit of the NMDA receptor. It enhances glutamate- and aspartate-induced GluN2B-NMDAR-mediated currents, exhibiting EC50 values of 43.7 nM and 18 nM, respectively. This compound demonstrates significant potential in reversing anxiety-like behaviors and cognitive impairments in murine models. It serves as a valuable tool for researching neurological disorders, particularly those related to anxiety. -
NMDA-Receptor Antagonist
LY 233053 is a potent competitive antagonist of the NMDA receptor. It exhibits significant anticonvulsant and antiepileptic properties, making it valuable for research in neuronal excitability and seizure-related disorders. This compound is suitable for studies investigating synaptic transmission, neuroprotection, and the underlying mechanisms of various neurological conditions. -
NMDA Antagonist
Traxoprodil mesylate is a potent and selective NMDA receptor antagonist, exhibiting protective effects on hippocampal neurons with an IC50 of 10 nM. This compound is primarily utilized in neuropharmacological research to investigate mechanisms of neuroprotection and the modulation of excitatory neurotransmission. Its specific action makes it a valuable tool for studying various neurological disorders linked to NMDA receptor activity. -
NMDA antagonist
Indantadol hydrochloride is a potent, non-selective NMDA antagonist that also exhibits monoamine oxidase (MAO) inhibitory activity. It effectively inhibits the binding of [³H]-MK-801 to NMDA receptors in a non-competitive manner, with an IC50 of 8.1 μM, and completely abolishes NMDA-induced dopamine release. Additionally, Indantadol hydrochloride demonstrates neuroprotective properties with an ED₅₀ of 35 μM, and displays valuable anticonvulsant and analgesic effects, making it relevant for studies in pain hypersensitivity and seizure disorders. -
NMDA Receptor Antagonist
LY 233536 is a competitive antagonist of the NMDA receptor, acting to inhibit excitatory neurotransmission in the central nervous system. This compound is primarily used in neuroscience research to explore the role of NMDA receptors in synaptic plasticity, neurodegenerative diseases, and pain signaling mechanisms. Its efficacy in modulating receptor activity makes it valuable for investigating various neurological conditions and potential therapeutic strategies. -
NMDA Receptor Inhibitor
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. -
Positive Allosteric Modulator of NMDAR
SGE-301 is a positive allosteric modulator of the N-methyl-D-aspartate receptor (NMDAR). It effectively restores NMDAR density and normalizes long-term potentiation, making it a valuable tool in the study of neurological disorders. SGE-301 is particularly useful for researchers investigating the role of NMDAR in synaptic plasticity and neurophysiology. -
NMDA Receptor Agonist
trans-ACBD (trans-1-Aminocyclobutane-1,3-dicarboxylic acid) is a potent and selective agonist of the NMDA receptor, primarily targeting glutamatergic neurotransmission. Its ability to modulate NMDA receptor activity makes trans-ACBD a valuable tool in the study of neurobiology, synaptic plasticity, and related disorders. This compound is suitable for diverse research applications involving excitatory neurotransmission pathways. -
NMDA Receptor Antagonist
Neramexane is an oral N-methyl-D-aspartate (NMDA) receptor antagonist with potential neuroprotective properties. It has been investigated for its role in addressing various central nervous system disorders, including Alzheimer's disease, as well as the treatment of drug and alcohol dependence and pain management. This compound is valuable for research into neuroprotection and synaptic modulation. -
NMDA Receptor Blocker
Caged MK801 is a selective, non-competitive, irreversible blocker of the NMDA receptor, targeting the open-channel state. It is designed to release MK801 upon photolysis, providing a tool for precise temporal control in neuronal studies. This compound is compatible with neuropharmacological applications, enabling exploration of synaptic plasticity and neurodegeneration mechanisms. -
NMDAR Modulator
NMDAR Modulator 2 is an NMDA receptor modulator that alters NMDA receptor activity. This compound serves as a valuable tool for investigating psychiatric disorders associated with dysregulated glutamatergic transmission, such as treatment-resistant depression. Its targeted action on NMDA receptors makes it suitable for exploring therapeutic strategies in conditions where glutamate signaling is implicated. -
NMDA Receptor Antagonist
DL-AP5 lithium is a competitive antagonist of the NMDA (N-methyl-D-aspartate) receptor. It demonstrates notable antinociceptive properties, making it a valuable tool in pain research. This compound has been shown to specifically inhibit ion channels in the rabbit retina, providing insights into its potential applications in neuropharmacology and retinal studies. -
NMDA Inhibitor
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. -
NMDAR Antagonist
Delucemine hydrochloride is a selective N-methyl-D-aspartate receptor (NMDAR) antagonist, known for its role in modulating glutamatergic signaling. This compound exhibits potential antidepressant properties, making it a valuable tool for researching treatments for mood disorders. Additionally, Delucemine hydrochloride may be utilized to explore the underlying mechanisms of NMDAR-related neuropsychiatric conditions. -
NMDA Receptor Modulator
NMDA Receptor Modulator 8 is an NMDA receptor modulator that exhibits 50%-100% potentiation of the NMDA receptor activity at a concentration of 10 μM. This compound can play a significant role in studies related to synaptic plasticity, neuroprotection, and various neurodegenerative diseases. Its modulation of NMDA receptor function makes it a valuable tool for researchers investigating excitatory neurotransmission and associated pathways. -
NMDAR Antagonist
NMDAR antagonist 4 is a specific antagonist of the NMDA receptor, targeting the glycine site with a binding affinity characterized by a Ki value exceeding 100 μM. This compound has been utilized in biological research to investigate the role of NMDA receptors in various neurological pathways and disorders. Its utility spans studies on excitotoxicity, synaptic plasticity, and potential therapeutic applications in neurodegenerative diseases. -
NMDA Receptor Antagonist
LY 235959 is a competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound enhances the anticonvulsant effects of various antiepileptic agents, making it valuable in the research of epilepsy and related neurological disorders. Its ability to modulate NMDA receptor activity positions LY 235959 as a critical tool for studying synaptic transmission and excitotoxicity. -
NMDA Antagonist
Etoxadrol is a potent NMDA antagonist, exhibiting high affinity for the N-methyl-D-aspartic acid receptor. It is primarily utilized in anesthetic research to modulate pain mechanisms and examine neuroprotective effects. This compound is of particular interest in studies related to pain management and the exploration of anesthetic protocols. -
Glycine/NMDA Receptor Antagonist
ZD 9379 sodium acts as a competitive antagonist at the glycine-binding site of the NMDA receptor, exhibiting an IC50 value of 75 nM for the glutamate site. This compound inhibits glycine binding, mitigating excitotoxicity and demonstrating therapeutic potential in conditions such as acute ischemic stroke. ZD 9379 sodium reduces the frequency of cortical spreading depression, decreases infarct volume, and enhances neurological function in preclinical mouse models, making it a valuable tool for research in neuroprotection and stroke mechanisms. -
Positive Allosteric Modulator Of GluN1/GluN3 NMDA Receptors
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. -
NMDA Receptor Antagonist
Dizocilpine is a potent, non-competitive antagonist of the NMDA receptor, characterized by a Kd of 37.2 nM in rat brain membranes. By binding to a specific site within the NMDA-associated ion channel, it effectively inhibits calcium ion (Ca2+) influx. This compound is widely used in research focused on epilepsy, neurotoxicity, and neurodegenerative diseases, making it a valuable tool for studying excitotoxicity and synaptic function. -
NMDA Receptor Antagonist
Cycloleucine is a selective NMDA receptor antagonist that targets the glycine site, exhibiting a Ki value of 600 μM. This compound inhibits S-adenosyl-methionine-mediated methylation and acts as a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine demonstrates anxiolytic and cytostatic properties, making it a valuable tool for research in neurobiology and cancer studies. Its unique mechanism of action provides insights into the underlying pathways of excitotoxicity and cellular regulation. -
NMDA Receptor Antagonist
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine binding site on the NMDA receptor, exhibiting a KB value of 65 nM. This compound effectively reduces NMDA-induced neuronal injury and enhances social interaction and exploration behaviors in rodent models. Additionally, 5,7-DCKA demonstrates anxiolytic-like effects, facilitating research into the role of glycine in NMDA receptor-mediated synaptic activity and associated psychiatric disorders. -
NMDAR Agonist
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. -
NMDA Antagonist
Orphenadrine is a skeletal muscle relaxant that acts as an NMDA antagonist, primarily inhibiting the binding of [3H]MK-801 to the PCP binding site of the NMDA receptor. This compound exhibits a range of biological activities including antiparkinsonian, antihistaminic, antitremor, antispasmodic, and analgesic effects. Additionally, Orphenadrine has been shown to induce oxidative stress through CAR nuclear translocation and may have implications in pro-tumor activities. It also demonstrates neuroprotective properties by safeguarding rat cerebellar granule cells from 3-NPA-induced cytotoxicity, suggesting potential therapeutic applications in neurodegenerative diseases associated with NMDA receptor overactivation. -
Gly/NMDA Receptor Antagonist
CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, exhibiting an IC50 of 6 nM. This compound acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). CGP 78608 hydrochloride is primarily employed in research investigating its anticonvulsant activity and the modulation of excitatory neurotransmission. -
NMDA Receptor Agonist
L-Homocysteic acid is an endogenous excitatory amino acid functioning as a NMDA receptor agonist, with an effective concentration (EC50) of 14 μM. Its neurotoxic properties make it a valuable tool in the investigation of neurological disorders. L-Homocysteic acid enables researchers to explore the roles of excitatory neurotransmission and contribute to the understanding of related pathophysiological conditions. -
NMDA Receptor PAM
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. -
NMDA Antagonist
Fluoroethylnormemantine is an N-methyl-D-aspartate (NMDA) receptor antagonist, serving as a derivative of Memantine. This compound showcases neuroprotective, anti-amnesic, and antidepressant-like properties, making it valuable in neurological research. Additionally, [18F]-Fluoroethylnormemantine is utilized as a positron emission tomography (PET) tracer, enhancing imaging studies related to NMDA receptor activity and its implications in various mental health disorders. -
NMDA Receptor Inhibitor
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. -
NMDA Receptor Modulator
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. -
NMDA Agonist
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. -
NMDAR Allosteric Modulator
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. -
NMDA Receptor Partial Agonist
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. -
GluN2B-NMDAR Antagonist
GluN2B-NMDAR antagonist-1 is an orally active antagonist of the GluN2B subtype of the N-methyl-D-aspartate receptor (NMDAR). This compound exhibits neuroprotective properties, making it a valuable tool in studying ischemic injury and related neurodegenerative conditions. It is primarily used in research to explore mechanisms of neuronal damage and potential therapeutic interventions.
