Catalog No.
Product Name
Application
Product Information
Citations
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AMPA Antagonist
BDZ-g is a potent and selective antagonist of the AMPA receptor, a key component in excitatory neurotransmission. This compound demonstrates significant biological activity in modulating synaptic transmission, making it valuable for research related to neurological disorders characterized by excessive AMPA receptor activity, such as epilepsy and neurodegenerative diseases. BDZ-g can serve as an important tool in understanding the role of AMPA receptors in various pathophysiological conditions. -
AMPAR Inhibitor.
D15 is an AMPA receptor (AMPAR) endocytosis inhibitor derived from a 15 amino acid segment of dynamin. It inhibits the interaction of dynamin with amphiphysin 1 and 2, leading to a significant increase in AMPAR excitatory postsynaptic potential (EPSC) amplitude in medium spiny neurons (MSNs) within Sapap3 knockout mice. This peptide has valuable applications in the investigation of neuropsychiatric disorders and related signaling pathways. -
AMPA Receptor Modulator
AMPA Receptor Modulator-3 is an allosteric modulator of the AMPA receptor, exhibiting an EC50 of 4.4 μM. This compound is valuable for investigating the role of AMPA receptors in the mammalian nervous system, particularly in studies related to learning and memory processes. Its modulation of glutamatergic signaling makes it a pertinent tool for neurological research and drug development targeting cognitive functions. -
GluR1/2/AMPA Receptor Agonist
Cl-HIBO is a highly selective agonist for the GluR1 and GluR2 subtypes of AMPA receptors, exhibiting EC50 values of 4.7 μM and 1.7 μM, respectively. This compound demonstrates potent activity as an AMPA receptor agonist with an IC50 of 0.22 μM. Additionally, Cl-HIBO displays desensitizing properties, making it a valuable tool for research in neuropharmacology and studies of synaptic transmission. -
AMPA Receptor Activator
NPEC-caged-(S)-AMPA is a photolabile caged analog of (S)-AMPA, specifically designed to target and activate AMPA receptors. This compound utilizes the NPEC photoprotecting group to selectively release (S)-AMPA upon illumination, enabling precise spatial and temporal control of receptor activation. It serves as a valuable tool in neuroscience research, facilitating studies on synaptic transmission and signal transduction pathways mediated by glutamate receptors. -
AMPA Receptor Modulator
AMPA receptor modulator-11 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and promoting excitatory neurotransmission. This compound plays a significant role in research related to neuropsychiatric disorders such as depression, schizophrenia, Alzheimer’s disease, and attention deficit hyperactivity disorder (ADHD). Its ability to selectively target AMPA receptors makes it an essential tool for exploring therapeutic strategies in these conditions. -
AMPA Receptor Modulator
JNJ-56022486 is a potent negative modulator of the AMPA receptor, exhibiting a Ki value of 19 nM and selective antagonism for TARP-γ8. This compound demonstrates effective blood-brain barrier permeability, making it suitable for in vivo studies. JNJ-56022486 is primarily utilized in research focused on epilepsy and related neurological disorders, providing a valuable tool for investigating synaptic transmission and excitability in the central nervous system. -
AMPA Receptor Antagonist
CP-465022 hydrochloride is a selective noncompetitive antagonist of the AMPA receptor, exhibiting significant anticonvulsant activity. It effectively inhibits kainate-induced responses in rat cortical neurons with an IC50 of 25 nM. This compound serves as a valuable tool for exploring the physiological and pathophysiological roles of AMPA receptors in various neurological contexts. -
NMDA Receptor Antagonist
Remacemide hydrochloride is a weak uncompetitive antagonist of the NMDA receptor, exhibiting IC50 values of 68 μM for MK-801 binding and 76 μM for NMDA-induced currents. As a moderate inhibitor of sodium channels, this compound demonstrates anticonvulsant properties, making it a valuable tool in the study of neuropharmacology. Research applications include investigating mechanisms underlying seizure disorders and testing potential therapeutic approaches for neurological conditions. -
AMPA Receptor Antagonist
Irampanel is an AMPA receptor antagonist that selectively blocks excitatory neurotransmission by inhibiting AMPA receptor activity. Additionally, it acts as a voltage-dependent sodium channel blocker, leading to a decrease in neuronal excitability. This compound has demonstrated efficacy in reducing kainate-induced currents in rat cortical neurons, making it a valuable tool for research applications related to neuropharmacology and the investigation of excitatory synaptic transmission. -
AMPA Receptor Antagonist
ZK 187638 is an AMPA receptor antagonist that effectively inhibits kainate-induced currents in cultured hippocampal neurons, demonstrating noncompetitive antagonism with an IC50 of 3.4 μM. This compound is valuable for research applications focused on synaptic transmission, neuroprotection, and the study of excitotoxicity in neurodegenerative disorders. -
AMPA Receptor Antagonist
YM928 is a noncompetitive antagonist of the α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. This compound effectively inhibits AMPA receptor-mediated neurotoxicity in primary rat hippocampal cultures with an IC50 of 2 μM. Additionally, YM928 blocks AMPA-induced intracellular calcium influx (IC50 of 3 μM) and antagonizes AMPA-induced inward currents (IC50 of 1 μM). It holds potential for research into various neurological disorders. -
AMPA Receptor Antagonist
AMPA receptor antagonist-3 is a selective antagonist of the AMPA receptor, which plays a critical role in excitatory neurotransmission in the central nervous system. This compound is valuable for studying neurological disorders that involve dysregulation of glutamate signaling, such as epilepsy, Alzheimer's disease, and neurodegenerative conditions. Its utility in research enables the exploration of therapeutic strategies targeting excitatory neurotransmission. -
AMPA Receptor Antagonist
LY 215490 is a selective, competitive antagonist of the AMPA receptor, exhibiting inhibitory potency with IC50 values of 4.8 μM against AMPA, 26.4 μM against CGS 19755, and 247 μM against kainate. This compound demonstrates neuroprotective effects, particularly in the context of focal ischaemia. LY 215490 serves as a valuable tool in studying excitatory neurotransmission and its implications in neurodegenerative diseases. -
AMPA Receptor Antagonist
CP-465022 maleate is a potent, selective noncompetitive antagonist of the AMPA receptor, exhibiting anticonvulsant properties. It effectively inhibits kainate-induced responses in rat cortical neurons with an IC50 of 25 nM. This compound serves as a valuable research tool to explore the role of AMPA receptors in both physiological and pathophysiological contexts. -
AMPA Receptor Antagonist
Irampanel hydrochloride is a potent antagonist of the AMPA receptor, acting primarily on excitatory glutamate signaling pathways. This compound effectively blocks voltage-dependent sodium channels and inhibits kainic acid-induced currents in rat cortical neurons. It is primarily used in research applications focused on neuroprotection, synaptic plasticity, and the study of neurodegenerative diseases. -
AMPA Receptor Modulator
AMPA Receptor Modulator-5 functions as a modulator of AMPA receptors, which are critical for fast excitatory synaptic transmission in the central nervous system. This compound has demonstrated potential in the research of neurological diseases by influencing synaptic plasticity and neurotransmission. Its application extends to studies focused on cognitive functions and neurodegenerative disorders, making it a valuable tool for exploring therapeutic strategies in neuroscience. -
AMPA Receptor Blocker
Gamma-DGG acetate is a competitive antagonist of the AMPA receptor, exerting its effects by inhibiting excitatory glutamatergic neurotransmission. By blocking AMPA receptors, this compound modulates excitatory post-synaptic potentials (e.p.s.p.s) and is valuable in research focused on neurological processes, synaptic plasticity, and related disorders. Its reversible action makes it an essential tool for studying receptor dynamics and synaptic function in various experimental settings. -
AMPA Antagonist
EGIS-8332 is a non-competitive antagonist of the AMPA receptor, effectively inhibiting AMPA-mediated currents in rat cerebellar Purkinje cells. It demonstrates a potent capability to block AMPA- and Quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons, with an IC50 ranging from 5.1 to 9.0 μM. EGIS-8332 exhibits notable anticonvulsant and neuroprotective properties, making it a valuable tool for research in neurological diseases. -
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. -
AMPA Receptor Antagonist
YM 900 is an AMPA receptor antagonist that selectively inhibits excitatory neurotransmission mediated by AMPA receptors. Its primary mechanism involves blocking the receptor's ion channel, thereby reducing the influx of sodium ions. This compound is valuable in research applications focused on neuroprotection, synaptic plasticity, and the study of neurological disorders related to glutamatergic signaling. Researchers may utilize YM 900 to investigate the role of AMPA receptors in various models of brain function and pathology. -
AMPA Receptor Antagonist
AMPA Receptor Antagonist-2 is a potent antagonist of the AMPA receptor, a subtype of glutamate receptor involved in synaptic transmission. By inhibiting AMPA receptor activity, this compound plays a crucial role in research related to excitatory neurotransmission, neuroprotection, and various neurodegenerative diseases. Its application extends to studying synaptic plasticity and the mechanisms underlying conditions such as epilepsy and chronic pain. -
AMPA Receptor Antagonist
Ro 48-8587 is a selective antagonist of the AMPA receptor, exhibiting an IC50 of 8 nM. This compound functionally inhibits AMPA receptor activity and effectively blocks AMPA-induced depolarization in rat cortical wedges. Ro 48-8587 is utilized in research related to ischemia and seizure disorders. -
AMPA positive allosteric modulator
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPA receptors (AMPARs). It effectively enhances AMPAR activity in both human and rat models, exhibiting an EC2x value of 0.96 μM in rat embryonic cortical primary neurons. Additionally, BPAM363 promotes the upregulation of brain-derived neurotrophic factor (BDNF) protein expression in rat primary cortical neuronal cultures and increases AMPA-mediated excitatory postsynaptic responses in rat and mouse models. This compound is valuable for researching cognitive disorders and related neurological conditions. -
AMPA/kainate Receptor Antagonist
UBP-282 is a potent and selective competitive antagonist of AMPA and kainate receptors. It effectively inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. In addition, UBP-282 antagonizes kainate-induced depolarizations of dorsal roots, exhibiting a pA2 value of 4.96. This compound serves as a valuable tool for investigating excitatory neurotransmission and related neurological pathways. -
AMPA-R Antagonist
KRP-199 is a potent antagonist of the α-amino-3-hydroxy-5-methylisoxazolepropionic acid receptor (AMPA-R), exhibiting a Ki of 16 nM. This compound demonstrates high selectivity for AMPA-R, contributing to significant neuroprotective effects in vivo. KRP-199 is useful for investigating mechanisms underlying neurodegenerative diseases and evaluating potential therapeutic approaches. -
AMPA Receptor Activator
Leptin (116-130) is a bioactive fragment of the leptin protein, known to activate AMPA receptors. This compound enhances AMPA receptor trafficking to synapses, facilitating activity-dependent synaptic plasticity in the hippocampus. Furthermore, Leptin (116-130) exhibits protective effects against synaptic disruption and neuronal cell death in amyloid toxicity models, making it valuable for research into Alzheimer's disease mechanisms. -
AMPA Receptor Antagonist
LY-300168 is a non-competitive antagonist of the AMPA receptor, capable of crossing the blood-brain barrier. This compound has demonstrated the ability to attenuate hippocampal injury and mitigate sound-induced clonic and tonic convulsions. Its pharmacological properties make it a valuable tool for research into neurological disorders and the modulation of excitatory neurotransmission. -
AMPA Receptor Inhibitor
AMPA-IN-1 is a potent inhibitor of the AMPA receptor, which is critical for fast excitatory synaptic transmission and synaptic plasticity in the brain. By modulating AMPA receptor activity, AMPA-IN-1 demonstrates potential for research into various central nervous system disorders, including epilepsy. This compound may provide valuable insights into therapeutic strategies targeting excitatory neurotransmission. -
AMPA Receptor PAM
AMPA receptor modulator-6 is a positive allosteric modulator (PAM) of the AMPA receptor, enhancing its activity and facilitating synaptic transmission. This compound is instrumental for studying neurological diseases and disorders, making it valuable for research into cognitive function, excitotoxicity, and synaptic plasticity. Its ability to modulate AMPA receptor activity offers insight into potential therapeutic strategies for conditions like Alzheimer's disease and multiple sclerosis. -
NMDA/AMPA Antagonist
Caroverine is a competitive and reversible antagonist of NMDA and AMPA glutamate receptors. It also possesses antioxidant properties and acts as a calcium-blocking agent, demonstrating vasorelaxant effects. This compound is primarily utilized in research applications related to inner ear tinnitus. -
AMPA Agonist
(S)-CPW 399 is a subtype-selective full agonist of AMPA receptors, demonstrating a 20-fold higher affinity for GluA1 and GluA2 subunits compared to GluA3 and GluA4 subunits. By activating AMPA receptors with GluA1 subunits, (S)-CPW 399 significantly enhances the spontaneous firing rate of locus coeruleus noradrenergic neurons. This compound is valuable for research into neurological diseases, providing insights into synaptic transmission and neuronal excitability. -
AMPA Receptor Antagonist
AMPA receptor antagonist-1 is a selective antagonist of the AMPA receptor, functioning to inhibit excitatory neurotransmission in the central nervous system. This compound demonstrates potential therapeutic activity in the study of various neurological disorders, such as epilepsy and neurodegenerative diseases. Its application facilitates the exploration of AMPA receptor modulation and its role in synaptic plasticity and neuronal signaling. -
AMPA Inhibitor
AMPA-IN-2 is a potent orally active inhibitor of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, efficiently crossing the blood-brain barrier. This compound demonstrates significant anti-epileptic effects by reducing neuronal excitability and attenuating glutamatergic transmission. AMPA-IN-2 is effective in the pentylenetetrazol model of epilepsy, making it a promising candidate for research in the field of epilepsy and related neuronal excitability disorders. -
AMPA Receptor Antagonist
GYKI-47261 dihydrochloride is a selective, orally active antagonist of the AMPA receptor, exhibiting an IC50 of 2.5 μM. This compound demonstrates a wide range of anticonvulsive activity and offers neuroprotective effects, making it valuable for neurological research. Additionally, GYKI-47261 serves as a potent inducer of the cytochrome P450 enzyme CYP2E1, further expanding its potential applications in pharmacological studies. -
AMPA Receptor Antagonist
(R,S)-3,4-Dicarboxyphenylglycine is an AMPA receptor antagonist that inhibits AMPA-mediated depolarization in motor neurons. This compound is useful for investigating the role of AMPA receptors in various neurological diseases. Its application in research allows for a better understanding of synaptic transmission and excitotoxicity in neurobiology. -
AMPA Receptor Antagonist
GYKI-47261 is a selective, competitive antagonist of the AMPA receptor, exhibiting an IC50 of 2.5 μM. This compound demonstrates significant anticonvulsive activity and provides neuroprotective effects, making it valuable in neurological research. Additionally, GYKI-47261 is a potent inducer of CYP2E1, highlighting its potential implications in drug metabolism studies. -
AMPA/NMDA Antagonist
(R)-3,4-DCPG is a selective antagonist of AMPA and NMDA receptors, demonstrating a Kd of 77 μM for AMPA. At a concentration of 500 μM, it fully antagonizes NMDA-induced depolarization, while exhibiting weaker antagonistic effects on kainate-induced depolarizations. This compound is valuable for research exploring synaptic transmission and neuropharmacology, particularly in studies investigating excitotoxicity and related neurological disorders. -
AMPAR PAM
AMPA Receptor Modulator-4 is an orally active positive allosteric modulator targeting AMPA receptors (AMPAR PAM). This compound, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, effectively crosses the blood-brain barrier. Research indicates that AMPA Receptor Modulator-4 enhances cognitive function and improves working memory performance in murine models, making it a valuable tool for studies on cognitive enhancement and neurological disorders. -
AMPAR Positive Allosteric Modulator
JAMI1001A is a positive allosteric modulator of the AMPA receptor, which plays a crucial role in synaptic transmission and plasticity. This compound effectively enhances receptor activation by modulating the deactivation and desensitization processes of both flip and flop isoforms. JAMI1001A is primarily utilized in neurological research to investigate synaptic function and potential therapeutic strategies for cognitive disorders. -
NMDAR Antagonist
NMDAR antagonist 5 (Compound A17) is a selective antagonist targeting the N-methyl-D-aspartate receptor (NMDAR) with an IC50 of 0.3 µM. This compound also inhibits monoamine transporters, including the serotonin transporter (SERT, IC50 = 1.1 µM), dopamine transporter (DAT, IC50 = 0.7 µM), and norepinephrine transporter (NET, IC50 = 2.7 µM). With a favorable safety profile and low toxicity across multiple organ systems, NMDAR antagonist 5 demonstrates potential antidepressant effects, making it a valuable tool for research into depression and related neurological disorders. -
AMPA Receptor Potentiator
PF-04701475 is a potent AMPA receptor potentiator with an EC50 of 123 nM. This compound enhances synaptic transmission mediated by AMPA receptors, making it valuable for investigating mechanisms underlying neurological disorders. PF-04701475 can aid in the exploration of potential therapeutic strategies for conditions such as depression and cognitive decline. -
AMPA Antagonist
DL-Willardiine is an AMPA receptor antagonist with an IC50 of 2 μM. It is employed in neuropharmacology research to investigate excitatory neurotransmission and its implications in various neurological disorders. This compound serves as a valuable tool in studying the mechanisms of synaptic transmission and the effects of glutamatergic signaling. -
AMPAR Antagonist
Philanthotoxin 74 diTFA is a selective AMPA receptor antagonist, primarily targeting the GluR3 and GluR1 subunits with IC50 values of 263 nM and 296 nM, respectively. This compound is instrumental in studies focused on synaptic transmission and neuropharmacology, providing valuable insights into excitatory neurotransmission and potential therapeutic interventions for neurological disorders. Its specificity makes it a useful tool for researchers investigating the role of AMPA receptors in various biological contexts. -
AMPA Receptor PAM
UoS12258 is a selective positive allosteric modulator of the AMPA receptor, enhancing AMPA receptor-mediated synaptic transmission. This compound demonstrates significant potential in improving cognitive performance in various rat models, particularly in scenarios involving scopolamine-induced impairment and water maze tasks in aged rats. UoS12258 serves as a valuable tool for research in cognitive enhancement and synaptic function. -
Anti-parkinson Agent
Budipine hydrochloride functions primarily as an anti-Parkinson agent, targeting the central nervous system. It acts as a substrate of P-glycoprotein (P-gp), facilitating its uptake into the brain. Additionally, Budipine hydrochloride serves as an NMDA antagonist and exhibits indirect dopaminergic effects by enhancing dopamine release and inhibiting monoamine oxidase type B (MAO-B). This compound is valuable for research focused on CNS disorders, particularly Parkinson's disease. -
AMPA receptor PAM
LY-503430 is an orally active positive allosteric modulator of the AMPA receptor. This compound enhances AMPA receptor activity, making it useful for investigating synaptic transmission and neuronal excitability. LY-503430 is particularly relevant in research focused on neurological disorders, including Parkinson's disease. -
Transporter Inhibitor
Pseudoisocyanine iodide, also known as 1,1'-Diethyl-2,2'-cyanine iodide, functions as an inhibitor of organic cation transporters (OCT1, OCT2, OCT3) and the plasma membrane monoamine transporter (PMAT). This compound exhibits antidepressant activity, making it valuable for research in mental health and neuropharmacology. Its ability to modulate transporter function positions it as a useful tool for studying mechanisms of neurotransmitter regulation and potential therapeutic interventions in mood disorders. -
Deuterium Substitute
Tetrabenazine-d6 is a deuterium-labeled analogue of Tetrabenazine, designed for improved stability and pharmacokinetic profiles in research. This compound primarily targets the vesicular monoamine transporter 2 (VMAT2), leading to decreased monoamine release and significant reduction in hyperkinetic movements. Tetrabenazine-d6 is instrumental in the study of Huntington's disease and various other hyperkinetic movement disorders, providing a valuable tool for understanding disease mechanisms and therapeutic interventions. -
NET Inhibitor
Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways.
