2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. Monoamine Transporter

Monoamine Transporter

Monoamine Transporter

Related Products

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Monoamine transporters (MATs) belong to the solute carrier 6 (SLC6) family of human transporters, which, in turn, is a subfamily of the broader neurotransmitter:sodium symporters (NSSs) that comprise transporters from prokaryotic to human. MATs comprise three main members-the dopamine (DA) transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). MATs regulate neurotransmission via the reuptake of dopamine, serotonin and norepinephrine from extra-neuronal regions and thus maintain neurotransmitter homeostasis.

MATs are transmembrane proteins located in plasma membranes of monoaminergic neurons. These proteins use ion (Na+, Cl−) gradients as energy sources to move monoamines into or out of neurons. In the membrane of intracellular synaptic vesicles is the vesicular monoamine transporters 1 and 2 (VMAT1 and VMAT2), which use a proton gradient as the energy source to sequester cytosolic monoamines into the vesicles and then release the monoamines into synaptic cleft by exocytosis. Dysregulation of MATs has been linked to depression, anxiety disorder, attention-deficit-hyperactivity disorder, obsessive-compulsive disorder, substance-use disorders, epilepsy, Parkinson’s disease and autism-spectrum disorder. Thus, MATs serve as pharmacological targets for several neuropsychiatric and neurodegenerative disorders.

Monoamine Transporter Related Products (70):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161433
    VMAT2-IN-3
    		Inhibitor
    VMAT2-IN-3 (compound 10) is a potent vesicular monoamine transporter-2 (VMAT2) inhibitor with a Ki of 0.71 nM. VMAT2-IN-3 has the potential for neurological or psychiatric disease research.
    VMAT2-IN-3
  • HY-153472
    VMAT2-IN-2 tosylate
    		Inhibitor
    VMAT2-IN-2 tosylate is a potent VMAT2 inhibitor. VMAT2-IN-2 tosylate can be used in research of tardive dyskinesia.
    VMAT2-IN-2 tosylate
  • HY-116062
    JNJ-7925476 hydrochloride
    		Inhibitor
    JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
    JNJ-7925476 hydrochloride
  • HY-106604
    Lortalamine
    		Inhibitor
    Lortalamine (LM 1404) is a selective norepinephrine transporter inhibitor with an IC50 of <1 nM. Lortalamine is a non-tricyclic antidepressant. Lortalamine antagonises Reserpine (HY-N0480)-induced ptosis and hypothermia. Lortalamine inhibits norepinephrine uptake.
    Lortalamine
  • HY-15793A
    Trans (2,3)-Dihydrotetrabenazine
    		Inhibitor
    Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
    Trans (2,3)-Dihydrotetrabenazine
  • HY-118064A
    (R)-Thionisoxetine hydrochloride
    (R)-Thionisoxetine hydrochloride (LY-368975 hydrochloride) is a potent and selective central and peripheral norepinephrine (NE) uptake inhibitor. (R)-Thionisoxetine hydrochloride prevents 6-hydroxydopamine-induced hypothalamic NE depletion with an ED50 of 0.21 mg/kg. (R)-Thionisoxetine hydrochloride can be used in the study of a variety of diseases, including depression and urinary incontinence.
    (R)-Thionisoxetine hydrochloride
  • HY-181151
    DLX48
    		Inhibitor
    DLX48 is a LeuBAT (Δ13 mutant) transporter inhibitor that binds to the transporter’s active site. DLX48 can crosses the blood-brain barrier, and has a lower risk of cytochrome P450-related drug-drug interactions. DLX48 can be used for the research of major depressive disorder.
    DLX48
  • HY-16525
    XEN-2174
    		Inhibitor
    XEN-2174 is a noradrenaline transporter (NET) inhibitor. XEN-2174 inhibits the reuptake of noradrenaline through non-competitive inhibition, increasing the concentration of noradrenaline in the synaptic cleft, thereby activating α2-adrenergic receptor at the spinal level and exerting analgesic effects. XEN-2174 exhibits long-lasting analgesic effects in models of neuropathic pain and postoperative pain in rats. XEN-2174 can be used in pain research.
    XEN-2174
  • HY-B0590S3
    Tetrabenazine-d7
    		Inhibitor
    Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
    Tetrabenazine-d<sub>7</sub>
  • HY-119921
    Indatraline
    		Inhibitor
    Indatraline (Lu 19005 free base) is a long-acting monoamine reuptake inhibitor that can be used in the research of neurological diseases.
    Indatraline
  • HY-W703376
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride
    		Agonist
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride (Compound Imp.1) is a non-selective monoamine transporter (DAT/NET/SERT) agonist. tert-Butylcathinone hydrochloride is promising for research of depressive disorders.
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride
  • HY-172421
    Cendifensine
    		Inhibitor
    Cendifensine is the inhibitor for monoamine reuptake that inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT).
    Cendifensine
  • HY-173398
    NMDAR antagonist 5
    		Antagonist
    NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression.
    NMDAR antagonist 5
  • HY-107956
    Imipramine pamoate
    Imipramine pamoate is a potent anti-depressant compound.
    Imipramine pamoate
  • HY-141554A
    (2S,3S,11bR)-Dihydrotetrabenazine
    		Inhibitor
    (2S,3S,11bR)-Dihydrotetrabenazine ((2S,3S,11bR)-DHTBZ) is a highly selective inhibitor of vesicular monoamine transporter 2 (VMAT2) with a Ki value of 593 nM. (2S,3S,11bR)-Dihydrotetrabenazine inhibits vesicular transport of monoamine neurotransmitters like dopamine and serotonin, reducing their synaptic release. (2S,3S,11bR)-Dihydrotetrabenazine is promising for research of Huntington's chorea and other hyperkinetic disorders.
    (2S,3S,11bR)-Dihydrotetrabenazine
  • HY-172029
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT)，serotonin transporter (SERT)，and the norepinephrine transporter (NET).
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride
  • HY-W743021
    4-Methyl-α-ethyltryptamine
    4-Methyl-α-ethyltryptamine is a homolog of α-Ethyltryptamine. α-Ethyltryptamine alters monoamine release and re-uptake in the brain.
    4-Methyl-α-ethyltryptamine
  • HY-120788
    VMAT2-IN-4
    		Inhibitor
    VMAT2-IN-4 (compound 11) is a vesicular monoamine transporter-2 (VMAT2) inhibitor. VMAT2-IN-4 inhibits [3H]-DTBZ binding (Ki = 560 nM). VMAT2-IN-4 inhibits [3H]-DA (Ki = 45 nM) from entering vesicles and being taken up by cells. VMAT2-IN-4 can be used in methamphetamine addiction research.
    VMAT2-IN-4
  • HY-103465B
    FFN511 hydrochloride
    		Inhibitor
    FFN511 (hydrochloride) is a potent fluorescent false neurotransmitters (FFNs) that targets neuronal vesicular monoamine transporter 2 (VMA T2). FFN511 (hydrochloride) inhibits serotonin binding to VMA T2-containing membranes with an IC50 of 1 µM. FFN511 (hydrochloride) directly images the dynamics of release during exocytosis, can be used to label dopamine terminals in live cortical-striatalacute slices.
    FFN511 hydrochloride
  • HY-W680886
    6-APDB
    		Modulator
    6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse.
    6-APDB