Catalog No.
Product Name
Application
Product Information
Citations
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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. -
FFNs
FFN511 is a potent fluorescent false neurotransmitter targeting the vesicular monoamine transporter 2 (VMAT2). With an IC50 of 1 µM, FFN511 effectively inhibits serotonin binding to VMAT2-containing membranes. This compound enables direct imaging of neurotransmitter release dynamics during exocytosis and is particularly useful for labeling dopamine terminals in live cortical-striatal acute slices, facilitating in-depth studies of synaptic function and neurotransmission. -
Monoamine Transporter Inhibitor
(+)-Tetrabenazine is a reversible inhibitor of the vesicular monoamine transporter 2 (VMAT-2). It exhibits a potency that is 10-fold greater for VMAT-2 than for VMAT-1, effectively restricting monoamine transport. This compound is primarily utilized in research focused on neurochemical pathways and the treatment of movement disorders, such as Huntington's disease and tardive dyskinesia, by regulating dopamine levels in the synaptic cleft. -
VMAT2 Substrate
FFN200 dihydrochloride is a fluorescent substrate targeting the vesicular monoamine transporter 2 (VMAT2). This compound enables the selective tracing of monoamine exocytosis in neuronal cell cultures and brain tissue, making it a valuable tool for neuropharmacological studies. With fluorescence excitation and emission maxima at 352 nm and 451 nm, respectively, FFN200 dihydrochloride is well-suited for applications requiring high sensitivity and specificity in monitoring neurotransmitter release. -
TBZ Metabolite
(R,S,S)-Dihydrotetrabenazine is a secondary alcohol metabolite derived from Tetrabenazine, functioning primarily as a poor inhibitor of the vesicular monoamine transporter 2 (VMAT2) with a Ki value of 690 nM. This compound is utilized in neuropharmacological studies to investigate the modulation of monoamine transporters and their role in diseases such as Parkinson's and Huntington's. Its unique isomeric structure allows for in-depth research into the pharmacokinetics and pharmacodynamics of related compounds. -
VMAT2 Inhibitor
Dihydrotetrabenazine (DHTBZ) is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2). By decreasing the monoamine content in presynaptic neurons, it plays a crucial role in the study of movement disorders. DHTBZ is essential for investigating the mechanisms underlying neurotransmitter regulation and offers potential insights into therapeutic strategies for neurological diseases. -
Drug Derivative
4-Ethyl-N,N-Dmc hydrochloride is a drug derivative acting as a non-selective substrate for monoamine transporters, which enhances the release of neurotransmitters. This compound is primarily utilized in research focused on the pharmacological effects of amphetamines and related substances. Its structural modifications offer insights into the development of novel psychoactive compounds and their interactions within the central nervous system. -
VMAT2 Inhibitor
(-)-Tetrabenazine is a specific inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound exhibits notable biological activity in the modulation of monoamine neurotransmitter levels, making it valuable for research in neuropharmacology and the study of movement disorders. Its role as a VMAT2 inhibitor can aid in the investigation of drug development for conditions such as Huntington's disease and other neurodegenerative disorders. -
Deuterated (+)-Tetrabenazine
(+)-Tetrabenazine-d6 is a deuterated form of the reversible inhibitor (+)-Tetrabenazine, which targets the vesicular monoamine transporter 2 (VMAT-2). This compound is utilized in research to investigate neurochemical processes and the role of monoamines in neurological disorders. Its isotopic labeling facilitates advanced metabolic studies and pharmacokinetic evaluations in biological systems. -
VMAT2 Inhibitor
Tetrabenazine mesylate is a potent reversible inhibitor of the vesicular monoamine transporter VMAT2, with a Kd value of 1.34 nM. This compound is primarily used in research focused on hyperactive movement disorders, including Huntington's disease, due to its ability to modulate monoamine neurotransmitter release. Tetrabenazine mesylate serves as a valuable tool for studying the underlying mechanisms of these neurological conditions and evaluating potential therapeutic approaches. -
VMAT2 Inhibitor
Tetrabenazine Metabolite is a potent vesicular monoamine transporter 2 (VMAT2) inhibitor, exhibiting high affinity with a Ki of 13.4 nM. This active metabolite plays a crucial role in the modulation of monoamine neurotransmitter levels and is primarily investigated for its therapeutic potential in chorea associated with Huntington’s disease and other hyperkinetic disorders. Its mechanism of action supports ongoing research in neurological disease management and treatment strategies. -
VMAT2 Inhibitor
VMAT2-IN-2 tosylate is a potent inhibitor of the vesicular monoamine transporter 2 (VMAT2). This compound is essential for investigating the pathophysiology of conditions such as tardive dyskinesia, where dysregulation of neurotransmitter storage and release plays a critical role. VMAT2-IN-2 tosylate may provide valuable insights into therapeutic strategies and the development of treatment options for related neurological disorders. -
Metabolite of Tetrabenazine
Trans (2,3)-Dihydrotetrabenazine is a metabolite of Tetrabenazine that primarily targets the vesicular monoamine transporter 2 (VMAT2). It exhibits significant inhibitory activity on VMAT2, contributing to altered monoamine storage and release. This compound is valuable for research applications in neuropharmacology and the study of movement disorders, providing insights into the modulation of neurotransmitter systems. -
Stable Isotope
Tetrabenazine-d7 is a deuterium-labeled derivative of Tetrabenazine, a reversible inhibitor of the vesicular monoamine transporter VMAT2, demonstrating a Kd value of 1.34 nM. This compound is essential in biochemical research focused on hyperkinetic movement disorders, including Huntington's disease. The stable isotope labeling allows for enhanced tracking and analysis in metabolic studies and pharmacokinetic evaluations. -
DAT/NET/SERT Agonist
2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride is a non-selective agonist of monoamine transporters, specifically targeting dopamine (DAT), norepinephrine (NET), and serotonin (SERT). This compound exhibits significant activity in modulating monoamine neurotransmission, making it a valuable tool for investigating the biochemistry underlying depressive disorders. It serves as a useful reagent in pharmacological studies aimed at understanding the mechanisms of mood regulation and potential therapeutic approaches. -
Monoamine Transporter Inhibitor
13-Hydroxyisobakuchiol is a selective inhibitor of monoamine transporters, primarily targeting the dopamine transporter (DAT) and norepinephrine transporter (NET) with IC50 values of 0.58 μM and 0.69 μM, respectively. In contrast, it exhibits significantly lower affinity for the serotonin transporter (SERT), with an IC50 of 312.02 μM. This compound is valuable for research applications related to neurodegenerative diseases, including Parkinson's disease, and mood disorders such as depression. -
Monoamine Transporter Inhibitor
Cendifensine is a monoamine transporter inhibitor that targets the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). It is known for its ability to inhibit the reuptake of these key neurotransmitters, thus enhancing their availability in the synaptic cleft. This compound is primarily utilized in research to study the mechanisms of mood disorders, depression, and other neurological conditions, making it a valuable tool for neuroscientific investigations. -
VMAT2 Inhibitor
(2S,3S,11bR)-Dihydrotetrabenazine is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2), exhibiting a Ki value of 593 nM. This compound disrupts the vesicular transport of monoamine neurotransmitters, including dopamine and serotonin, leading to decreased synaptic release of these neurotransmitters. (2S,3S,11bR)-Dihydrotetrabenazine is valuable for research into Huntington's chorea and other hyperkinetic disorders, providing insights into potential therapeutic strategies. -
Monoamine Transporter
4-Methyl-α-ethyltryptamine functions primarily as a monoamine transporter modulator. This compound is known to influence the release and re-uptake of monoamines within the brain, making it potentially valuable for research into neurochemical pathways. Its structural similarities to α-Ethyltryptamine suggest its utility in studying the effects of tryptamine derivatives on neurotransmitter dynamics and behavior. -
VMAT2 Inhibitor
VMAT2-IN-4 is a selective inhibitor of the vesicular monoamine transporter-2 (VMAT2), demonstrating an affinity with a Ki value of 560 nM for [3H]-DTBZ binding and a more potent inhibition of [3H]-DA uptake into vesicles at a Ki of 45 nM. This compound effectively disrupts monoamine neurotransmitter packaging within vesicles, making it a valuable tool for investigating the mechanisms underlying methamphetamine addiction. VMAT2-IN-4 supports research into the modulation of dopaminergic signaling and its implications in addiction studies. -
FFNs
FFN511 hydrochloride is a potent fluorescent false neurotransmitter (FFN) that selectively targets the vesicular monoamine transporter 2 (VMAT2). With an IC50 of 1 µM, it effectively inhibits serotonin binding to VMAT2-containing membranes. This compound enables real-time imaging of neurotransmitter release dynamics during exocytosis and is particularly useful for labeling dopamine terminals in live cortical-striatal acute slices, making it a valuable tool for studying synaptic transmission and neuropharmacology. -
VMAT2 Inhibitor
GZ-11608 is a potent and selective inhibitor of the vesicular monoamine transporter-2 (VMAT2) with a high affinity (Ki = 25 nM). This compound effectively reduces methamphetamine-induced dopamine release from isolated synaptic vesicles of dopaminergic neurons. Furthermore, GZ-11608 demonstrates rapid penetration into the brain and is characterized by an absence of neurotoxicity. It is a valuable tool for studying methamphetamine use disorder in therapeutic research. -
Monoamine Transporter
3-Bromoamphetamine hydrochloride is a para-substituted amphetamine that functions as a monoamine releasing agent, primarily targeting the monoamine transporters. This compound has been shown to facilitate the release of neurotransmitters such as serotonin, dopamine, and norepinephrine, making it valuable in studies of neuropharmacology and behavior. Its applications in research include investigations of mood disorders, stimulant effects, and the underlying mechanisms of psychoactive substances.
