Catalog No.
Product Name
Application
Product Information
Citations
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Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. -
VMAT-2 inhibitor
Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). -
Autophagy Inhibitor
Reserpine acts as an inhibitor of vesicular monoamine transporter 2 (VMAT2), thereby influencing neurotransmitter storage and release. This compound is widely utilized in research studies focusing on autophagy inhibition and its implications in various neurodegenerative disorders. Additionally, reserpine's effects on monoamine levels make it a valuable tool in the investigation of psychiatric conditions and the biochemical pathways involved in these diseases. -
VMAT2 Inhibitor
Reserpine hydrochloride is a potent inhibitor of the vesicular monoamine transporter 2 (VMAT2). It is primarily utilized in research to study neurotransmitter release and its implications in neurodegenerative diseases and mental health disorders. By inhibiting VMAT2, Reserpine hydrochloride disrupts the storage of monoamines, allowing for investigation into their effects on various physiological and pathological processes. -
Histone Methyltransferase
Lobelane hydrochloride selectively inhibits the vesicular monoamine transporter-2 (VMAT2). This compound demonstrates an affinity for VMAT2 with a K(i) value of 630 nM, while exhibiting low interaction with nicotinic acetylcholine receptors (nAChR). The unique mechanism of action of lobelane hydrochloride makes it a valuable tool for studying neurotransmitter dynamics and offers potential in the development of therapeutic agents aimed at addressing methamphetamine abuse. Its structural analogs may further expand its applications in neuropharmacological research. -
Monoamine Transporter Modulator
6-APDB is a monoamine transporter modulator that selectively influences human monoamine transporters while acting as a partial agonist at 5-HT2 family receptors. It demonstrates potent inhibition of norepinephrine and serotonin reuptake, with IC50 values of 0.56 μM for norepinephrine transporters (NET) and 2.3 μM for serotonin transporters (SERT). Additionally, 6-APDB mediates the release of multiple monoamine neurotransmitters, exhibiting a dose-dependent, biphasic locomotor effect in mice. This compound also has potential empathogenic properties along with behavioral effects relevant to research on monoamine signaling and neuropsychopharmacology, with no significant cytotoxicity observed at high concentrations. -
Stable Isotope
Reserpine-d9 is a deuterated form of Reserpine that serves as an inhibitor of the vesicular monoamine transporter 2 (VMAT2). This stable isotope-labeled compound is valuable for studies in neuropharmacology and metabolism, allowing for precise tracking and quantification of Reserpine interactions in various biological systems. It enables researchers to explore its effects on neurotransmitter release and potential applications in psychiatric and neurological disorders. -
SERT/VMAT2 probe
FFN246 is a fluorescent probe that selectively targets the serotonin transporter (SERT) and vesicular monoamine transporter 2 (VMAT2), exhibiting excitation and emission spectra of 392 nm and 427 nm, respectively. This compound is ideal for labeling serotonergic neurons in mouse brain tissue, facilitating the study of serotonergic signaling and neuronal activity. Its dual substrate properties make FFN246 a valuable tool in neurobiological research and the exploration of neurotransmitter dynamics. -
Noradrenalin Reuptake Inhibitor
Beloxepin is a synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. It demonstrates selective inhibition with approximately 100-fold lower affinity for other monoamine transporters. Beloxepin exhibits significant antidepressant and analgesic properties, making it useful for research centered on mood disorders and pain management. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Adrenergic Receptor
FFN270 hydrochloride is a fluorescent tracer that specifically targets adrenergic receptors, functioning as a substrate for norepinephrine and vesicular monoamine transporters. This compound displays distinct absorption and excitation maxima at either 320 nm or 365 nm depending on the solvent pH, with an emission wavelength of 475 nm. FFN270 hydrochloride is valuable in research applications that involve monitoring norepinephrine dynamics and can also serve as a ratiometric pH sensor for various biological studies. -
Serotonin And Norepinephrine Reuptake Inhibitor
Milnacipran is an orally active serotonin and norepinephrine reuptake inhibitor that primarily targets the monoamine transporters responsible for neurotransmitter reuptake. It demonstrates high affinity for the norepinephrine transporter and serotonin transporter, with Ki values of 31 nM and 8.5 nM, respectively. Milnacipran exhibits antidepressant, anxiolytic, and analgesic properties, and has been shown to inhibit pERK1/2 activation. This compound is applicable in the study of major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. -
Stable Isotope
Milnacipran-d5 hydrochloride is a deuterated form of Milnacipran hydrochloride, a potent serotonin and norepinephrine reuptake inhibitor. It targets monoamine transporters, exhibiting Ki values of 31 nM for the norepinephrine transporter and 8.5 nM for the serotonin transporter. With notable antidepressant, anxiolytic, and analgesic properties, Milnacipran-d5 hydrochloride is valuable for research on major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. Additionally, it has been shown to affect behavior in preclinical models, providing insights into its pharmacological mechanisms. -
Stable Isotope
Milnacipran-d10 hydrochloride is a deuterium-labeled form of the serotonin and norepinephrine reuptake inhibitor, Milnacipran hydrochloride. It effectively inhibits monoamine transporters, targeting the norepinephrine and serotonin transporters with reported Ki values of 31 nM and 8.5 nM, respectively. This compound exhibits antidepressant, anxiolytic, and analgesic properties, and has demonstrated efficacy in reducing biting behavior in murine models. Milnacipran-d10 hydrochloride is valuable for research applications focused on major depressive disorder, anxiety disorders, and neuropathic pain syndromes, such as fibromyalgia. -
Tricyclic Antidepressant Trimipramine Active Metabolite
Trimipramine N-oxide is the active metabolite of the tricyclic antidepressant trimipramine, primarily targeting human monoamine transporters. It effectively inhibits noradrenaline (hNAT), serotonin (hSERT), and dopamine (hDAT) transporters, along with human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. This compound is valuable for research focused on depression and anxiety, contributing to the understanding of mood disorders and the pharmacological mechanisms of antidepressants. -
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. -
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. -
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. -
Monoamine Transporter Inhibitor
Indatraline hydrochloride is a non-selective monoamine transporter inhibitor, primarily targeting the reuptake of dopamine, serotonin, and norepinephrine. This compound is relevant for research focused on antidepressant mechanisms. Additionally, Indatraline hydrochloride induces autophagy and inhibits cell proliferation, suggesting potential applications in the study of autophagy-related diseases, including atherosclerosis and restenosis. -
Biochemical Assay Reagent
Florbenazine is a diagnostic imaging agent that selectively targets the vesicular monoamine transporter 2 (VMAT2) in the central nervous system. The fluorine-18 labeled derivative is utilized in positron emission tomography (PET) scanning to assess neuromodulatory functions. Research has demonstrated a significant biodistribution profile in mice, with a high striatum-to-cerebellum ratio, supporting its application in the diagnostic investigation of neurodegenerative disorders, such as dementia with Lewy bodies and Parkinson’s disease. -
Amphetamine Derivative
N-Ethyl-3,4-DMA hydrochloride is an amphetamine derivative that primarily targets the monoamine transporters, particularly the serotonin and dopamine transporters. This compound exhibits psychoactive properties and is explored for its potential effects on mood and cognition. Its unique profile makes it a valuable reagent for studies in neuropharmacology and the investigation of amphetamine-like substances. -
Drug Derivative
1-(4-Methylphenyl)-2-(propylamino)propan-1-one hydrochloride is a drug derivative that primarily targets monoamine transporters. This compound exhibits significant biological activity as a stimulant and may influence neurotransmitter release. Its applications in research include investigating the mechanisms of action of psychoactive substances and studying mood disorders. -
Drug Derivative
N-Demethyl methylone hydrochloride is a drug derivative that primarily targets monoamine transporters, including the serotonin and dopamine transporters. This compound exhibits stimulatory effects and is often utilized in research focused on psychoactive substances and their metabolic pathways. Its biological activity is relevant for studies exploring the pharmacological properties of substituted cathinones and their effects on neurotransmitter systems. -
α-Pyrrolidinopropiophenone Derivative
4'-Fluoro-α-pyrrolidinopropiophenone hydrochloride is a derivative of α-Pyrrolidinopropiophenone, primarily acting on the monoamine transporters. This compound exhibits stimulant properties, making it relevant for research in neuropharmacology and the study of addiction mechanisms. Its applications also extend to the exploration of dopamine and norepinephrine reuptake inhibition, aiding in the development of potential therapeutic agents targeting these neurotransmitter systems.
