- Signaling Pathways
- Membrane Transporter/Ion Channel
- Monoamine Transporter
Monoamine Transporter
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.
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Monoamine Transporter Related Products (82)
Related Products (82)
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Valbenazine tosylate
0 ImagesSynonyms: NBI-98854 tosylateValbenazine tosylate (NBI-98854 tosylate) is a vesicular monoamine transporter 2 (VMAT2) inhibitor with the Ki of 110-190 nM. -
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Tetrabenazine Metabolite
0 ImagesCat. No.: HY-G0025CAS No.: 924854-60-4Synonyms: (-)-β-Dihydrotetrabenazine; (-)-β-HTBZTetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders. -
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Vanilpyruvic acid (Standard)
0 ImagesCat. No.: HY-101416RCAS No.: 1081-71-6Synonyms: Vanylpyruvic acid (Standard)Vanilpyruvic acid (Standard) is the analytical standard of Vanilpyruvic acid. This product is intended for research and analytical applications. Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid. -
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VMAT2-IN-3
0 ImagesCat. No.: HY-161433CAS No.: 3033475-58-7VMAT2-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. -
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VMAT2-IN-2 tosylate
0 ImagesCat. No.: HY-153472CAS No.: 2608770-12-1VMAT2-IN-2 tosylate is a potent VMAT2 inhibitor. VMAT2-IN-2 tosylate can be used in research of tardive dyskinesia. -
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JNJ-7925476 hydrochloride
0 ImagesCat. No.: HY-116062CAS No.: 109085-56-5JNJ-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. -
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Lortalamine
0 ImagesCat. No.: HY-106604CAS No.: 70384-91-7Synonyms: LM 1404 -
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Trans (2,3)-Dihydrotetrabenazine
0 ImagesCat. No.: HY-15793ACAS No.: 171598-74-6Synonyms: (2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZTrans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2). -
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(R)-Thionisoxetine hydrochloride
0 ImagesCat. No.: HY-118064ACAS No.: 222961-65-1Synonyms: LY-368975 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. -
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DLX48
0 ImagesCat. No.: HY-181151CAS No.: 2457357-91-2DLX48 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. -
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XEN-2174
0 ImagesCat. No.: HY-16525CAS No.: 701909-57-1XEN-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. -
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Tetrabenazine-d7
0 ImagesCat. No.: HY-B0590S3CAS No.: 2701977-99-1Synonyms: TBZ-d7-d7; Ro 1-9569-d7Tetrabenazine-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. -
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Indatraline
0 ImagesCat. No.: HY-119921CAS No.: 86939-10-8Synonyms: Lu 19005 free baseIndatraline (Lu 19005 free base) is a long-acting monoamine reuptake inhibitor that can be used in the research of neurological diseases. -
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2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride
0 ImagesCat. No.: HY-W703376CAS No.: 63199-74-62-(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. -
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Cendifensine
0 ImagesCat. No.: HY-172421CAS No.: 1034048-49-1Cendifensine is the inhibitor for monoamine reuptake that inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). -
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Bevantolol
0 ImagesSynonyms: SOM3355 free baseBevantolol (SOM3355 (free base)) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease. -
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NMDAR antagonist 5
0 ImagesCat. No.: HY-173398CAS No.: 3038464-68-2NMDAR 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. -
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Imipramine pamoate
0 ImagesCat. No.: HY-107956CAS No.: 10075-24-8Imipramine pamoate is a potent anti-depressant compound. -
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(2S,3S,11bR)-Dihydrotetrabenazine
0 ImagesCat. No.: HY-141554ACAS No.: 862377-27-3Synonyms: (2S,3S,11bR)-DHTBZ(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. -
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3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride
0 ImagesCat. No.: HY-172029CAS No.: 2748289-38-33,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT),serotonin transporter (SERT),and the norepinephrine transporter (NET). -
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