Catalog No.
Product Name
Application
Product Information
Citations
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NMDA Receptor Antagonist
CGP 37849 is a potent competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound exhibits anticonvulsant properties in rodent models, as well as demonstrating antidepressant and anxiolytic-like effects. It serves as a valuable tool in research focused on neurological disorders and the modulation of synaptic transmission. -
Glycine/NMDA Partial Agonist/Antagonist
(R)-(+)-HA-966 functions as a partial agonist/antagonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. This compound selectively inhibits the activation of the mesolimbic dopamine system induced by amphetamine, making it relevant for studying addiction and dopamine-related disorders. Its ability to traverse the blood-brain barrier suggests potential applications in addressing conditions such as neuropathic and acute pain. -
NMDA Receptor Antagonist
SDZ 220-040 is a competitive antagonist of the NMDA receptor, exhibiting a pKi of 8.5. This compound is primarily employed in research investigating neurological diseases, offering insights into the mechanisms underlying neurodegeneration and synaptic dysfunction. Its specific targeting of NMDA receptors makes it a valuable reagent for pharmacological studies and the development of novel therapeutic strategies. -
NMDA Receptor Antagonist
Arcaine sulfate is a potent NMDA receptor antagonist that selectively inhibits glutamate signaling at this critical synaptic target. Its ability to modulate excitatory neurotransmission makes Arcaine sulfate a valuable tool for studying neurophysiological processes and evaluating the role of NMDA receptors in various neurological disorders. This compound is widely utilized in research exploring synaptic plasticity, neuroprotection, and the mechanisms underlying excitotoxicity. -
NMDA Agonist
(RS)-(Tetrazol-5-yl)glycine is a potent and selective agonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits effective stimulation with EC50 values of 99 nM and 1.7 μM for the GluN1/GluN2D and GluN1/GluN2A subtypes, respectively. This compound is utilized in research involving seizure activity and neuronal activation, as evidenced by its ability to induce Fos expression in mice models. -
NMDARs Negative Allosteric Modulator
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. -
NMDA Receptor Modulator
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. -
GluN1/GluN2A NMDAR Antagonist
TCN 213 is a selective, surmountable antagonist of the GluN1/GluN2A subunits of the N-methyl-D-aspartate receptor (NMDAR), exhibiting IC50 values of 0.55, 3.5, and 40 μM in the presence of 75, 750, and 7500 nM glycine, respectively. This compound serves a critical role in studying the pharmacological modulation of NMDAR expression in developing cortical neurons, making it a valuable tool for research in neurodevelopment and synaptic plasticity. -
NMDA Antagonist
L-689560 is a potent antagonist of the N-methyl-D-aspartate (NMDA) receptor, specifically targeting the GluN1 glycine binding site. This compound is utilized extensively in radiolabeled ligand binding studies and is essential for investigating the roles of NMDA receptors in both normal neurological functions and various neurological disorders. L-689560 aids in advancing our understanding of synaptic transmission and neurotoxicity linked to excitatory neurotransmission. -
NMDA Receptor Antagonist
(S)-(-)-HA 966 is a γ-Hydroxybutyrate-like compound that functions as a weak NMDA receptor antagonist. It exhibits muscle relaxant properties and has been shown to prevent increased mesocorticolimbic dopamine metabolism associated with behavioral responses to restraint stress and conditioned fear. This reagent can be utilized in studies investigating neuropharmacology and stress-related behavioral models. -
NMDA receptor antagonist
Neramexane hydrochloride is an NMDA receptor antagonist that exhibits neuroprotective properties. This compound is primarily utilized in research related to central nervous system disorders, including Alzheimer's disease, as well as investigations into drug and alcohol dependence and pain mechanisms. Its ability to modulate excitatory neurotransmission makes it a valuable tool for studying neurodegenerative processes and addiction pathways. -
NMDAR Antagonist
NMDAR antagonist 3 is a selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. This compound exhibits weak inhibitory activity against the NR1A/2B subtype, making it valuable for studies investigating the modulation of NMDA receptor signaling. Research applications include exploration of neurological conditions and behavioral studies involving synaptic plasticity and excitotoxicity. -
NMDA Receptor Modulator
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. -
NR2B-Selective NMDA Antagonist
NMDA receptor antagonist 2 is a potent NR2B-selective NMDA receptor antagonist with an IC50 of 1.0 nM and a Ki of 0.88 nM. This compound is utilized to investigate the mechanisms underlying neuropathic pain and Parkinson's disease. Its selectivity for the NR2B subtype makes it a valuable tool for exploring potential therapeutic strategies in these neurological disorders. -
NMDA Antagonist
Midafotel is a potent and competitive NMDA antagonist, exhibiting an ED50 value of 39 nM. This compound induces pronounced stereotyped behaviors and demonstrates neuroprotective properties, making it valuable for studies focused on neurodegenerative diseases and synaptic plasticity. Its unique pharmacological profile positions Midafotel as a relevant tool for investigating NMDA receptor modulation in various research applications. -
NMDA NR2B Negative Allosteric Modulator
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. -
NMDAR Agonist
TP-050 is a potent, orally active NMDAR agonist, selectively targeting the GluN2A and GluN2D subtypes with EC50 values of 0.51 μM and 9.6 μM, respectively. This compound effectively crosses the blood-brain barrier, facilitating its role in enhancing hippocampal long-term potentiation and promoting neuronal signal transmission. TP-050 offers valuable applications in neuroscience research, particularly in studies involving synaptic plasticity and cognitive function. -
NMDA NR2B Inhibitor
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. -
NMDA Receptor Antagonist
3-Methoxy PCE hydrochloride is an NMDA receptor antagonist, classified as an arylcyclohexylamine. With a pKi value of 7.22, it effectively inhibits NMDA receptor activity. This compound is primarily utilized in neuropharmacological studies and research focused on synaptic transmission and excitotoxicity pathways. -
NMDA Receptor Modulator
NMDA receptor modulator 2 is a potent modulator of the NMDA receptor, playing a critical role in glutamatergic neurotransmission. This compound exhibits significant neuroprotective properties and has potential applications in the study of neurological disorders, including Alzheimer's disease and other cognitive impairments. Its use in research can provide insights into synaptic plasticity and the mechanisms underlying neurodegeneration. -
NMDA Agonist
N-Phthaloylglutamic acid functions as a partial agonist of the NMDA receptor, specifically targeting the glutamate binding site with an affinity characterized by a Ki of 13 μM. Its biological activity contributes to the modulation of excitatory neurotransmission and may serve as a valuable tool in neuropharmacological research. This reagent is useful for studies investigating NMDA receptor dynamics and related neurological processes. -
NMDAR Blocker
NMDA receptor antagonist 4 is a uncompetitive, voltage-dependent antagonist of the N-methyl-D-aspartate receptor (NMDAR) with an IC50 of 1.93 μM. This orally active compound exhibits favorable blood-brain barrier permeability, making it suitable for in vivo studies. It is particularly relevant for research applications related to neurodegenerative diseases such as Alzheimer's disease. -
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. -
nAChR Inhibitor
Meclofenoxate, a nAChR inhibitor, is an ester derived from dimethylaminoethanol (DMAE) and para-chlorophenylalanine (pCPA). It is known for its potential to enhance memory and cognitive function. Meclofenoxate is commonly utilized in neurological research to investigate mechanisms underlying cognitive enhancement and memory improvement. -
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.
