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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. -
AchE Inhibitor/NMDAR Antagonist
Memagal is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 1.16 nM and acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist with a Ki of 4.6 μM. This compound effectively inhibits neurotoxicity triggered by NMDA, demonstrating an IC50 value of 0.28 nM. Memagal serves as a valuable tool for research focused on Alzheimer's disease, providing insights into mechanisms and potential therapeutic approaches. -
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. -
P2X Receptor Antagonist
PPADS tetrasodium is a non-selective antagonist of P2X receptors, effectively inhibiting recombinant P2X1, -2, -3, and -5 with IC50 values ranging from 1 to 2.6 μM. Additionally, it shows inhibitory effects on native P2Y2-like receptors (IC50 ~0.9 mM) and recombinant P2Y4 receptors (IC50 ~15 mM). This compound also acts as an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle, making it a valuable tool for research on purinergic signaling and related physiological processes. -
α-isomer of Nicotine
α-Nicotine is the α-isomer of nicotine and functions as an agonist of nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable biological activity that may be beneficial for understanding neuropsychiatric disorders, including schizophrenia and attention deficit hyperactivity disorder (ADHD). Its potential applications in research make it a valuable tool for exploring the pharmacological effects of nAChR activation. -
Endogenous Metabolite
Cotinine, a primary metabolite of nicotine, acts as an endogenous biomarker for tobacco exposure. This alkaloid exhibits vasodepressor activity and has demonstrated antiproliferative effects when combined with nicotine against conditions such as pterygium. Additionally, (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, facilitating dopamine release. Due to its diverse biological activities, cotinine is employed in research focused on cardiovascular and inflammatory diseases. -
nAChRs Antagonist
Dihydro-β-erythroidine hydrobromide is a competitive antagonist specifically targeting neuronal nicotinic acetylcholine receptors (nAChRs). It demonstrates notable selectivity for the α4β4 and α4β2 nAChR subtypes, with IC50 values of 0.19 μM and 0.37 μM, respectively. This compound is utilized in research exploring its potential antidepressant-like effects and its role in understanding nAChR-mediated signaling pathways. -
Acetylcholine Agonist
Spinosad is an acetylcholine agonist that acts primarily on the nicotinic acetylcholine receptors (nAChRs) in the insect nervous system. Derived from the fermentation products of the soil actinomycete Saccharopolyspora spinosa, Spinosad exhibits potent biological neurotoxic activity, making it effective as a broad-spectrum insecticide. Its favorable environmental and mammalian safety profile, along with its larvicidal properties, supports its use in various pest control applications. -
Insecticide
Acetamiprid is a neonicotinoid insecticide that acts as a selective agonist of nicotinic acetylcholine receptors (nAChRs). It disrupts normal synaptic transmission, leading to paralysis and death in target pests. Research applications include studies on neuromuscular function, insect behavior, and potential reproductive impacts in non-target organisms. -
α7 nAChR Agonist
PHA-543613 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound demonstrates significant selectivity for the α7 nAChR compared to other nicotinic and serotonergic receptors, including α3β4, α1β1γδ, α4β2, and 5-HT3. PHA-543613 is applicable in research focused on cognitive deficits associated with Alzheimer's disease and schizophrenia, making it a valuable tool for neuropharmacological studies. -
Insecticide
Flupyradifurone is a systemic agonist of nicotinic acetylcholine receptors (nAChRs) that disrupts signal transduction in the central nervous system of sap-sucking insects. It functions as a butenolide insecticide, effectively targeting pest populations while offering low toxicity to non-target organisms. Research applications include studying insect neurobiology and developing pest management strategies. -
nAChR Agonist
Tebanicline dihydrochloride is a selective agonist of nicotinic acetylcholine receptors (nAChRs), particularly targeting the α4β2 subtype. It exhibits strong analgesic properties and demonstrates oral bioavailability. This compound is valuable for research into pain management and the modulation of cholinergic signaling in neurological studies. -
nAChR Antagonist
Coclaurine is a tetrahydroisoquinoline alkaloid and a potent antagonist of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticancer activity by downregulating EFHD2-related NOX4-ABCC1 signaling, thereby enhancing the sensitivity of cancer cells to Cisplatin. Coclaurine also suppresses the stemness and metastatic potentials of non-small cell lung cancer (NSCLC) cells through the disruption of the FOXG1-EFHD2 promoter interaction, leading to reduced EFHD2 transcription. This compound serves as a valuable tool for research focused on cancer therapy and the modulation of nAChR signaling.

