Catalog No.
Product Name
Application
Product Information
Citations
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NMDAR Antagonist
Delucemine is an NMDAR antagonist that selectively modulates glutamatergic neurotransmission. Its primary biological activity lies in its potential antidepressant effects, making it a valuable tool for investigating mood disorders and their underlying mechanisms. This compound may also be utilized in research focused on neuroprotection and synaptic plasticity. -
NMDA Receptor Blocker
(S)-Alaproclate is a potent NMDA receptor blocker that exhibits superior activity compared to its R-(+)-enantiomer. It effectively inhibits NMDA receptor currents in vitro and significantly antagonizes cGMP elevation in vivo. This compound is valuable for research applications involving excitatory neurotransmission and the modulation of neurophysiological processes. -
NMDA Receptor Antagonist
Tezampanel hydrate is a potent and selective competitive antagonist of the NMDA receptor. It has demonstrated efficacy in producing postoperative analgesia in rat models, making it valuable for studying pain mechanisms. This compound is applicable in research on neuropathic pain, providing insight into potential therapeutic strategies targeting NMDA receptor activity. -
NMDAR/SERT Inhibitor
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. -
NMDA Receptor Modulator
UBP710 is a selective modulator of the NMDA receptor, specifically targeting GluN2B-containing subtypes with enhanced efficacy compared to GluN2A-containing receptors. This compound is useful in research focused on synaptic plasticity and neuroprotection, making it a valuable tool for studying neurodegenerative diseases and related neurological disorders. Its distinctive mechanism enables deeper insights into NMDA receptor function and its implications in various neurological pathways. -
NMDAR Antagonist
Nitromemantine is a selective NMDAR antagonist that acts through a dual mechanism, effectively blocking ion channels while also modulating receptor function via nitric oxide and redox pathways. It demonstrates significant therapeutic potential in rodent models of cerebral infarction, particularly in targeting ischemic neurons under hypoxic conditions. With an IC50 of 2.4 μM for inhibiting NMDA-induced current, Nitromemantine is a valuable tool for investigating the mechanisms and treatment strategies related to cerebral ischemic stroke. -
NMDA Receptors Positive Modulator
R-(+)-EU-1180-453 is a positive allosteric modulator that targets NMDA receptors containing GluN2C and GluN2D subunits, demonstrating a pEC50 value of 5.5 for both rat receptor subtypes. This compound enhances the potency of glutamate, amplifying receptor responses to agonists while acting selectively on receptors co-bound with both necessary co-agonists. R-(+)-EU-1180-453 is suitable for research into neurological conditions, including Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain. -
NMDA Receptor Antagonist
(3S,6R)-NML is an NMDA receptor antagonist that demonstrates pIC50 values of 4.8 for GluN1-GluN2A, 4.6 for GluN1-GluN2B, and 5.0 for both GluN1-GluN2C and GluN1-GluN2D. This compound is instrumental in studying the role of NMDA receptors in neurological disorders, particularly in depression research. Its specific antagonistic properties make it a valuable tool for investigating synaptic plasticity and related therapeutic approaches. -
NMDA Receptor Antagonist
CGP 39551 is a potent, orally active competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits significant anticonvulsant activity and effectively inhibits L-[3H]-glutamate binding with a Ki value of 8.4 μM. This compound is valuable for research aimed at understanding NMDA receptor-related neurological conditions and investigating potential therapeutic interventions for epilepsy. -
NMDA Receptor Antagonist
PMPA, an NMDA receptor antagonist, selectively inhibits the NMDA receptor subtypes NR2A, NR2B, NR2C, and NR2D with Ki values of 0.84, 2.74, 3.53, and 4.16 μM, respectively. This compound plays a critical role in research related to excitotoxicity and neurodegenerative diseases. Its ability to modulate synaptic transmission makes it valuable for studies investigating the pathophysiology of various neurological disorders. -
NMDA Receptor Modulator
NMDA receptor modulator 5 is a potent modulator of the NMDA receptor, facilitating its function in neural signaling pathways. This compound exhibits significant potential for the study of neurological disorders, offering insights into synaptic plasticity and excitotoxicity. It serves as a valuable tool for researchers investigating therapeutic strategies for various neurodegenerative conditions. -
NMDA Receptor Antagonist
L-687414 is an orally active glycine-site NMDA receptor antagonist, exhibiting low-potency partial agonist properties. This compound demonstrates anticonvulsant activity, making it valuable for research in epilepsy and neuropharmacology. Its action on the NMDA receptor can provide insights into synaptic transmission and neurodegenerative disease mechanisms. -
NMDA Inhibitor
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 Subtype NMDA Antagonist
CP-283097 is a selective NR2B subtype NMDA antagonist that acts competitively to inhibit [³H]CP-101,606 binding, with an IC50 of 18 nM. This compound effectively blocks NR2B-mediated currents (IC50 = 206 nM) while demonstrating minimal impact on NR2A and NR2C receptors, highlighting its specificity. CP-283097 possesses strong central nervous system permeability and has shown in vivo efficacy in preclinical models. It is suitable for research applications targeting neurological disorders associated with excessive NMDA receptor activation. -
NMDA Blocker
N20C hydrochloride is a selective, noncompetitive antagonist of the NMDA receptor that targets the open channel state. It exhibits micromolar affinity and demonstrates rapid on-off blockade kinetics, along with pronounced voltage dependence. This compound is notable for its neuroprotective properties, making it valuable for research in neurodegenerative diseases and synaptic function studies. -
NMDA Receptor Channel Blocker
Ensaculin is an NMDA receptor channel blocker that exhibits neuroprotective properties in models of NMDA toxicity. This compound promotes neuronal growth in primary cultures of rat brain cells, suggesting its potential for application in neurodegenerative research. Furthermore, Ensaculin holds promise as a candidate for anti-dementia therapies by modulating various neurotransmitter systems. -
NR1/NR2B NMDA Receptor Inhibitor
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. -
NMDA Antagonist
Besonprodil is a selective NMDA antagonist that effectively inhibits the N-methyl-D-aspartate receptor activity. Its primary mechanism involves blocking excitatory neurotransmitter signaling, which can have significant implications in neuroprotection and treatment of neurological disorders. This compound is primarily utilized in research focused on understanding synaptic transmission and potential therapeutic avenues for conditions such as chronic pain and anxiety disorders. -
NMDA Antagonist
D-AP4 (D-2-Amino-4-phosphonobutyric acid) is a broad-spectrum NMDA receptor antagonist, functioning as a phosphono analogue of glutamate. This compound also acts as an agonist for a quisqualate-sensitized AP6 site in the hippocampus. D-AP4 effectively inhibits AMPA receptor-mediated 57Co2+ influx in cultured cerebellar granule cells, with an IC50 value of approximately 100 μM. This makes D-AP4 a valuable tool for investigating glutamatergic signaling and its implications in neurobiology and related research applications. -
NMDA Antagonist
Conantokin R is a peptide antagonist of the NMDA receptor, exhibiting an IC50 value of 93 nM. This compound demonstrates binding affinity for Zn2+ and Mg2+ ions with dissociation constants of 0.15 μM and 6.5 μM, respectively. Conantokin R is noted for its anticonvulsant properties and has potential applications in studies related to excitotoxicity and neuroprotection. -
NMDA Receptor Potentiator
NMDA receptor potentiator-1 is a selective modulator targeting the NMDA receptor, specifically enhancing the activity of NR2C and NR2D subunits with IC50 values of 4 μM and 5 μM, respectively. This compound shows promise in increasing synaptic transmission and may serve as a valuable tool in studies related to neuropharmacology, synaptic plasticity, and neurodegenerative diseases. Its selective mechanism of action makes it a suitable candidate for investigating receptor-specific pathways and potential therapeutic applications. -
NMDA Antagonist
UK-315716 is a potent NMDA receptor antagonist that exhibits neuroprotective properties. It plays a significant role in research related to neurological disorders, including stroke and headache. This compound is valuable for investigating the mechanisms underlying excitotoxicity and may contribute to therapeutic strategies for neurodegenerative diseases. -
NMDA Receptor Modulator
NMDA receptor modulator 4 is a potent modulator of the NMDA receptor, which plays a critical role in synaptic plasticity and memory function. This compound exhibits significant effects on neurotransmission related to various neurological disorders. It is suitable for research applications focused on neuropharmacology and the exploration of therapeutic strategies for conditions such as Alzheimer's disease and schizophrenia. -
NMDAR2 Receptor Agonist
Homoquinolinic acid is a selective agonist of the NMDAR2 receptor. It is known to enhance excitatory neurotransmission and has implications in studies related to neurodegenerative disorders and synaptic plasticity. This compound is valuable for investigating the role of NMDAR2 signaling in various neurological research applications. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
NMDA Receptor Modulator
NMDA receptor modulator 3 is a potent modulator of NMDA receptors, which play a critical role in synaptic plasticity and memory function. This compound is valuable for research into neurological disorders, enabling studies on excitatory neurotransmission and associated pathophysiologies. Its unique pharmacological profile facilitates investigations into potential therapeutic strategies for conditions such as Alzheimer's disease and schizophrenia. -
NMDA Receptor Antagonist
L-703717 is a selective NMDA receptor antagonist that preferentially binds to cerebellar-specific NMDA receptors featuring the GluRepsilon3 subunit. This compound exhibits prominent accumulation in the rodent cerebellum, making it a valuable tool for investigating neurological diseases. Its unique selectivity and mechanism of action facilitate research into the underlying mechanisms of neurotransmission and potential therapeutic targets in neurological disorders. -
NMDAR Antagonist
Ro 25-6981 hydrochloride is a selective NMDA receptor antagonist that specifically targets the NR2B subunit. This compound exhibits anticonvulsant and anti-parkinsonian properties, making it a valuable tool in neurological research. Ro 25-6981 hydrochloride is particularly relevant for studying mechanisms underlying Parkinson's disease and may contribute to the development of therapeutic strategies for this condition. -
NMDA Receptor Antagonist
LY 274614 is a competitive antagonist of the NMDA receptor, known for its oral bioactivity. This compound is essential for investigating neurological diseases, as it modulates excitatory neurotransmission and can help elucidate mechanisms underlying various neurological conditions. Its application in research supports the study of NMDA receptor-mediated pathways in both in vitro and in vivo models. -
NMDA Receptor Antagonist
MDL 27266 is a potent orally active NMDA receptor antagonist that exhibits neuroprotective properties. This compound serves as a versatile anticonvulsant agent, making it valuable for studies related to seizure disorders and neuroprotection. Its ability to modulate excitatory neurotransmission positions it as a significant research tool in the fields of neurology and pharmacology. -
NMDA Receptor Antagonist
Fluorofelbamate is a potent NMDA receptor antagonist that demonstrates significant anticonvulsant and antiepileptogenic properties. In experimental models, it has shown effectiveness in mitigating self-sustaining status epilepticus (SSSE). This compound is suitable for research applications focused on epilepsy and related neurological conditions. -
NMDA Antagonist
Aptiganel is a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, exhibiting cerebroprotective properties. This compound is primarily utilized in research focused on neuroprotection and stroke models, contributing to the understanding of excitotoxicity and potential therapeutic interventions in neurological disorders. Its mechanism of action may help elucidate pathways involved in neurodegeneration and recovery following ischemic events. -
NMDA Receptor Modulator
NMDA receptor modulator 6 is a potent modulator of the NMDA receptor, an essential component in synaptic transmission and plasticity in the central nervous system. It plays a significant role in addressing neurological disorders by influencing excitatory neurotransmission. Research applications include studying neurodegenerative diseases, cognitive function, and synaptic mechanisms related to NMDA receptor activity. -
NMDA Agonist
Benzylaspartic acid, a derivative of aspartic acid, functions as an NMDA agonist. It exhibits significant antidepressant activity and has been shown to inhibit the development of alcohol-abstinence syndrome in chronic alcohol consumption rat models. This compound is particularly suited for use in research focused on depression and its underlying mechanisms. -
NMDA Receptor Antagonist
(R)-3C4HPG is a selective NMDA receptor antagonist known for its capacity to modulate glutamatergic signaling. This compound exhibits significant biological activity by inhibiting excitatory neurotransmission, making it a valuable tool in neuropharmacological research. It is often employed in studies investigating the pathophysiology of neurological disorders, as well as in the assessment of synaptic plasticity and learning processes. -
NMDA Agonist
NMDA Agonist 1 is a potent NMDA receptor agonist targeting the GluN1/GluN2B complex. It exhibits a Ki value of 96 nM and acts as a partial agonist with an EC50 of 78 nM. This compound is valuable for researching the functional roles of NMDA receptors in neuropharmacology and studying their implications in neurological disorders. -
NMDA Receptor Antagonist
CGP 43487 is an NMDA receptor antagonist that plays a critical role in modulating glutamatergic neurotransmission. This compound has been shown to significantly influence the structural development of the dentate gyrus, making it valuable for research in neurodevelopment and synaptic plasticity. CGP 43487 serves as an important tool for studying therapeutic approaches to neurological disorders associated with NMDA receptor activity. -
NMDA Antagonist
Indantadol is a non-selective NMDA receptor antagonist and MAO inhibitor, demonstrating a non-competitive blockade of [³H]-MK-801 binding with an IC50 of 8.1 μM. It effectively inhibits NMDA-induced dopamine release and exhibits neuroprotective effects, with an ED₅₀ value of 35 μM. Additionally, Indantadol displays significant anticonvulsant properties and mitigates high pain hypersensitivity, making it a valuable reagent for research in neuropharmacology and pain modulation. -
NMDA Inhibitor
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. -
NMDA Antagonist
ADCI is a noncompetitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, demonstrating anticonvulsant properties. This compound is widely utilized in research focused on neurological disorders, particularly for its potential to modulate excitatory neurotransmission in various models of epilepsy and neurodegeneration. -
NMDAR Antagonist
Withaphysalin D is a selective antagonist of the N-methyl-D-aspartate receptor (NMDAR) subtype containing GluN2B. Isolated from water lilies, this compound exhibits neuroprotective properties and has been shown to effectively cross the blood-brain barrier. It is valuable for research applications involving neurobiology and the study of excitatory neurotransmission. -
NMDA Receptor Antagonist
5,7-Dichlorokynurenic acid sodium serves as a selective and competitive antagonist at the glycine site of the NMDA receptor, exhibiting a KB of 65 nM. This compound effectively reduces neuron injury induced by NMDA and demonstrates significant anxiolytic-like effects in rodent models, including increased social interaction and open arm exploration. Its application in research supports investigations into the role of glycine in NMDA receptor-mediated synaptic transmission and associated behavioral outcomes. -
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.
