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Monoamine transporter inhibitors block reuptake of dopamine, noradrenaline and serotonin into neurons or vesicles. Plasma membrane transporters for dopamine (DAT), noradrenaline (NET) and serotonin (SERT) clear released transmitter from the synapse. Mice lacking DAT show hyperlocomotion and no response to cocaine or amphetamine, which identified this transporter as their main target. Vanoxerine 2HCl and GBR 12783 dihydrochloride are selective dopamine uptake inhibitors. Milnacipran hydrochloride inhibits both serotonin and noradrenaline reuptake at the plasma membrane. Vesicular monoamine transporters (VMAT) load monoamines into synaptic vesicles and are inhibited by reserpine. GZ-793A is a more selective inhibitor of the VMAT2 isoform.
(S)-Viloxazine Hydrochloride is the S-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant.
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.
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.
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Bicifadine is a serotonin/norepinephrine/dopamine reuptake inhibitor that demonstrates oral bioavailability. It exhibits significant antinociceptive properties across various models of acute, persistent, and chronic pain. Bicifadine is primarily utilized in research related to pain mechanisms and therapeutic interventions for pain management.
LY125180 is a selective serotonin uptake inhibitor that competes with serotonin and norepinephrine uptake in cortical synaptosomes, as well as dopamine uptake in striatal synaptosomes. It demonstrates Ki values of 0.06 μM for serotonin, 2.2 μM for norepinephrine, and 2.5 μM for dopamine. This compound is valuable for research applications focusing on neurotransmission and neuropharmacology, providing insights into serotonin-related disorders and the modulation of mood and anxiety.
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.
meta-Fluoxetine hydrochloride is an isomer of Fluoxetine hydrochloride and acts as a serotonin selective reuptake inhibitor (SSRI). It exhibits weak inhibitory activity on the serotonin transporter, influencing serotonin levels in the synaptic cleft. This compound is primarily utilized in research applications focused on the modulation of serotonergic signaling and the investigation of antidepressant mechanisms.
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.
Synonyms: Viloxazin; Emovit
Viloxazine is a selective norepinephrine transporter (NET) inhibitor, exhibiting an IC50 value of 0.26 μM. It demonstrates dual activity as a 5-HT receptor modulator by antagonizing 5-HT2B receptors (Ki = 4.2 μM) and agonizing 5-HT2C receptors (EC50 = 32 μM), thereby enhancing serotonin neurotransmission. Viloxazine effectively increases levels of norepinephrine and dopamine in the synaptic cleft, making it a valuable reagent for researching attention deficit hyperactivity disorder (ADHD) and related neurochemical pathways.
Synonyms: Viloxazin hydrochloride; Emovit hydrochloride
Viloxazine hydrochloride is a selective norepinephrine transporter (NET) inhibitor with an IC50 of 0.26 μM, functioning primarily to elevate norepinephrine levels in the synaptic cleft. Additionally, it modulates serotonin receptor activity by antagonizing 5-HT2B receptors (Ki=4.2 μM) and agonizing 5-HT2C receptors (EC50=32 μM), thereby enhancing serotonin neurotransmission. This compound is utilized in research related to attention deficit hyperactivity disorder (ADHD) and offers insights into the modulation of noradrenergic and serotonergic systems.
Synonyms: Org 4428; ADL 6906
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.
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.
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.
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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.
Synonyms: (±)-Nomifensine; Nomifensin
Nomifensine is a potent norepinephrine and dopamine reuptake inhibitor, demonstrating significant inhibitory effects on the uptake of these neurotransmitters in rat brain synaptosomes with IC50 values of 6.6 nM for norepinephrine, 48 nM for dopamine, and 830 nM for serotonin. With Ki values of 4.7 nM, 26 nM, and 4000 nM respectively, Nomifensine exhibits both antidepressant and analgesic properties. This compound is utilized in research focused on neurodegenerative diseases, substance addiction, and pain management.
Synonyms: (±)-Nomifensine maleate; Nomifensin maleate
Nomifensine maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. It effectively inhibits the uptake of NE, DA, and serotonin (5-HT) in rat brain synaptosomes, showing IC50 values of 6.6 nM, 48 nM, and 830 nM, respectively. This compound exhibits significant antidepressant and analgesic properties, making it valuable in research focused on neurodegenerative diseases, substance addiction, and pain mechanisms.
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.
4-Hydroxyatomoxetine acts as a potent noradrenaline re-uptake inhibitor, primarily targeting the norepinephrine transporter. As an active metabolite of Atomoxetine, it exhibits selective inhibition with Ki values of 5 nM for the norepinephrine transporter, 77 nM for the serotonin transporter, and 1451 nM for the dopamine transporter. This compound is utilized in research applications focused on neuropharmacology and the modulation of noradrenergic signaling pathways.
Synonyms: (R,R)-FCE20124 mesylate; (R,R)-PNU155950E mesylate; (R,R)-(-)-Reboxetine mesylate
(R,R)-Reboxetine mesylate acts as a selective noradrenaline reuptake inhibitor, targeting the norepinephrine system to provide antidepressant effects. This enantiomer exhibits improved bioavailability and low affinity for alpha-adrenergic and muscarinic receptors, contributing to its reduced toxicity profile in animal models. Its primary application lies in the research of mood disorders and the pharmacological assessment of antidepressant therapies.
Synonyms: (Rac)-Levoprotiline
Oxaprotiline is a potent norepinephrine uptake inhibitor, specifically designed to enhance noradrenaline levels in the brain. This compound exhibits significant antidepressant activity, making it a valuable tool in neuropharmacological research. Its ability to modulate neurotransmitter dynamics positions it as an important reagent for studies related to mood disorders and related therapeutic applications.
(1R,2S)-Dihydrobupropion is a norepinephrine-dopamine reuptake inhibitor that serves as an active metabolite of Bupropion. It exhibits significant biological activity by modulating neurotransmitter levels, making it useful for investigating neurological disorders and inflammatory conditions. This compound may facilitate research aimed at understanding the underlying mechanisms of these diseases and evaluating potential therapeutic strategies.
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Synonyms: LY 2216684
Edivoxetine is a potent and selective norepinephrine reuptake inhibitor. Its primary mechanism involves the inhibition of norepinephrine reuptake, thereby enhancing noradrenergic neurotransmission. This compound is utilized in research concerning major depressive disorder (MDD) and attention-deficit/hyperactivity disorder (ADHD), making it valuable for investigating therapeutic approaches in these conditions.
Synonyms: (S,S)-(+)-Reboxetine
Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor that targets norepinephrine transporters in both the central and peripheral nervous systems. This compound has demonstrated efficacy in increasing urethral resistance and has been investigated for its therapeutic potential in stress urinary incontinence, as evidenced by a Phase IIa clinical study. Its peripheral selectivity allows for enhanced urethral closure while minimizing central nervous system penetration, making Esreboxetine a valuable tool for researchers exploring treatments for urinary incontinence and related conditions.
PF-184298 is a dual serotonin and noradrenaline reuptake inhibitor, exhibiting IC50 values of 6 nM for serotonin and 21 nM for noradrenaline. This compound demonstrates significant potential in modulating neurotransmitter levels, making it valuable for research into mood disorders and related neuropharmacological studies. Its mechanism of action provides insights into therapeutic strategies for conditions such as depression and anxiety.
Reboxetine is a potent and selective noradrenaline uptake blocker. It primarily inhibits the reuptake of norepinephrine, leading to increased concentrations of this neurotransmitter in the synaptic cleft. Reboxetine has demonstrated efficacy in antidepressant research and is utilized in studies investigating mood disorders and related mechanisms of action.
