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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Reserpine-d9
0 ImagesCat. No.: HY-N0480SCAS No.: 84759-11-5Reserpine-d9 is the deuterium labeled Reserpine. Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
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(+)-Tetrabenazine
0 ImagesSynonyms: (+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine(+)-Tetrabenazine ((+)-TBZ) is the enantiomer of Tetrabenazine (HY-B0590) and is also a Vesicular Monoamine Transporter 2 (VMAT2) inhibitor with a rat Ki of 4.61 nM. (+)-Tetrabenazine inhibits monoamine uptake into granular vesicles of presynaptic neurons. (+)-Tetrabenazine is 3 times more active than (-)-Tetrabenazine. (+)-Tetrabenazine can be used for the research of Huntington's disease and hyperkinetic movement disorders (including chorea).
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Liafensine
0 ImagesCat. No.: HY-19907CAS No.: 1198790-53-2Synonyms: BMS-820836Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC50 of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression.
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m-Iodobenzylguanidine
0 ImagesCat. No.: HY-129040CAS No.: 80663-95-2Synonyms: MIBG; Iobenguanem-Iodobenzylguanidine (Iobenguane) is a ligand with high affinity against norepinephrine transporter (NET). m-Iodobenzylguanidine is used as an imaging agent in the diagnostic imaging and radionuclide studies of neuroendocrine tumors, such as neuroblastoma, pheochromocytoma and carcinoid tumor.
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FFN200 dihydrochloride
0 ImagesFFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively.
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GZ-793A
0 ImagesGZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction.
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(R,S,S)-Dihydrotetrabenazine
0 ImagesSynonyms: R,S,S-DHTBZ(R,S,S)-Dihydrotetrabenazine (R,S,S-DHTBZ) is a kind of discrete isomeric secondary alcohol metabolites of Tetrabenazine (TBZ, HY-B0590), is a poor VMAT2 inhibitor (Ki = 690 nM).
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4-Methylamphetamine hydrochloride
0 ImagesSynonyms: 4-MA hydrochloride4-Methylamphetamine hydrochloride is a 5-HT1A receptor agonist that induces hypothermia in rats by binding to the 5-HT1A receptor. Additionally, 4-Methylamphetamine hydrochloride acts on norepinephrine (NE), dopamine (DA), and serotonin (5-HT) transporters to increase the extracellular levels of these neurotransmitters. 4-Methylamphetamine hydrochloride can be used in the study of neurological disorders.
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Dihydrotetrabenazine
0 ImagesDihydrotetrabenazine (DHTBZ) is the active metabolite of Tetrabenazine (HY-B0590). Dihydrotetrabenazine is the inhibitor for human vesicular monoamine transporter 2 (VMAT2), that reduces monoamine content in presynaptic neurons, and can be used in movement disorder research.
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F3288-0031
0 ImagesCat. No.: HY-179568CAS No.: 926493-93-8F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC50 = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions.
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4-Ethyl-N,N-Dmc hydrochloride
0 Images4-Ethyl-N,N-Dmc hydrochloride is an analog of Methedrone. Methedrone acts as a non-selective substrate for monoamine transporters, facilitating a neurotransmitter release.
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(-)-Tetrabenazine
0 ImagesSynonyms: (-)-TBZ; (3S,11bS)-TBZ; (3S,11bS)-Tetrabenazine(-)-Tetrabenazine ((-)-TBZ; compound 13) is an enantiomer of Tetrabenazine (HY-B0590). (+)-Tetrabenazine proves 3-fold more active than (-)-Tetrabenazine in inhibiting vesicular monoamine transporter 2 (VMAT2).
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(+)-Tetrabenazine-d6
0 ImagesCat. No.: HY-B0590S1CAS No.: 1977511-05-9(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
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Tetrabenazine mesylate
0 ImagesTetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
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Radafaxine
0 ImagesCat. No.: HY-137107CAS No.: 192374-14-4Synonyms: (S,S)-Hydroxybupropion; GW-353162A free base; BW-306U free baseRadafaxine ((S,S)-Hydroxybupropion) is an antidepressant. Radafaxine blocks dopamine transporters (DAT). Radafaxine is an active metabolite of Bupropion.
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Lafadofensine (D-(-)-Mandelic acid)
0 ImagesCat. No.: HY-145577APurity: 99.95%Lafadofensine D-(-)-Mandelic acid is the monoamines reuptake inhibitor. Lafadofensine D-(-)-Mandelic acid has sufficient effects after short-term administration.
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Thionisoxetine
0 ImagesCat. No.: HY-U00069CAS No.: 155273-01-1Thionisoxetine is a norepinephrine transporter inhibitor with a Ki value of 0.2 nM in rats, and exhibits anti-hyperalgesic and analgesic activities. Thionisoxetine reverses thermal hyperalgesia and mechanical allodynia in rats. Thionisoxetine can be used in studies related to persistent inflammatory pain.
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Cavα2δ1&NET-IN-2
0 ImagesCat. No.: HY-148863CAS No.: 2143586-17-6Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain.
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Cavα2δ1&NET-IN-1
0 ImagesCat. No.: HY-148862CAS No.: 2314361-39-0Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain.
