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 Inhibitors
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Monoamine Transporter Related Products (82)
Related Products (82)
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4-Methyl-α-ethyltryptamine
0 ImagesCat. No.: HY-W743021CAS No.: 28289-30-74-Methyl-α-ethyltryptamine is a homolog of α-Ethyltryptamine. α-Ethyltryptamine alters monoamine release and re-uptake in the brain.
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VMAT2-IN-4
0 ImagesCat. No.: HY-120788CAS No.: 1436695-49-6VMAT2-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.
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FFN511 hydrochloride
0 ImagesCat. No.: HY-103465BCAS No.: 2596358-28-8FFN511 (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.
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6-APDB
0 ImagesCat. No.: HY-W680886CAS No.: 152623-93-36-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.
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Pseudoisocyanine iodide (Standard)
0 ImagesSynonyms: 1,1'-Diethyl-2,2'-cyanine iodide (Standard); Decynium 22 (Standard); Diethylcyanine iodide (Standard); Eastman 7851 (Standard)Pseudoisocyanine iodide (Standard) is the analytical standard of Pseudoisocyanine (iodide) (HY-107740). This product is intended for research and analytical applications. Pseudoisocyanine iodide (1,1'-Diethyl-2,2'-cyanine iodide) is an inhibitor of organic cation transporters (OCT1, OCT2, OCT3) and plasma membrane monoamine transporter (PMAT). Pseudoisocyanine iodide has antidepressant activity.
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FFN511 (Standard)
0 ImagesCat. No.: HY-103465RCAS No.: 1004548-96-2FFN511 (Standard) is the analytical standard of FFN511 (HY-103465). This product is intended for research and analytical applications. FFN511 is a potent fluorescent false neurotransmitters (FFNs) that targets neuronal vesicular monoamine transporter 2 (VMA T2). FFN511 inhibits serotonin binding to VMA T2-containing membranes with an IC50 of 1 μM. FFN511 directly images the dynamics of release during exocytosis, can be used to label dopamine terminals in live cortical-striatalacute slices.
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Tetrabenazine (Standard)
0 ImagesTetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. 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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Bevantolol-d7 hydrochloride
0 ImagesCat. No.: HY-121186SSynonyms: SOM3355-d7Bevantolol-d7 hydrochloride (SOM3355-d7) is the d7-labeled Bevantolol hydrochloride (HY-121186). Bevantolol hydrochloride (SOM3355) 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 hydrochloride 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 hydrochloride 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 hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease.
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WY-46824
0 ImagesCat. No.: HY-187589CAS No.: 960521-38-4WY-46824 is a selective norepinephrine transporter (NET) inhibitor. WY-46824 does not alter the total expression level or cell surface expression level of hNET. WY-46824 can be used in related research on attention deficit hyperactivity disorder (ADHD).
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GZ-11608
0 ImagesCat. No.: HY-152171CAS No.: 2141974-01-6GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder.
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Nisoxetine (Standard)
0 ImagesNisoxetine (Standard) is the analytical standard of Nisoxetine. This product is intended for research and analytical applications. Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
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3-Bromoamphetamine hydrochloride
0 ImagesCat. No.: HY-135022CAS No.: 1210708-61-43-Bromoamphetamine hydrochloride is a para-substituted amphetamine that acts as a monoamine releasing agent.
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Reserpine hydrochloride (Standard)
0 ImagesReserpine (hydrochloride) (Standard) is the analytical standard of Reserpine (hydrochloride). This product is intended for research and analytical applications. Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
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Bevantolol hydrochloride (Standard)
0 ImagesCat. No.: HY-121186RCAS No.: 42864-78-8Synonyms: SOM3355 (Standard)Bevantolol hydrochloride (Standard) (SOM3355 (Standard)) is the analytical standard of Bevantolol hydrochloride (HY-121186). This product is intended for research and analytical applications. Bevantolol hydrochloride (SOM3355) 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 hydrochloride 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 hydrochloride 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 hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease.
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Cilobamine methanesulfonate
0 ImagesCat. No.: HY-183457ACAS No.: 69429-85-2Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.
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Valbenazine (Standard)
0 ImagesSynonyms: NBI-98854 (Standard)Valbenazine (Standard) is the analytical standard of Valbenazine. This product is intended for research and analytical applications. Valbenazine (NBI-98854) is a vesicular monoamine transporter 2 (VMAT2) inhibitor with the Ki of 110-190 nM.
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N-Methyl-2-phenylpropan-1-amine hydrochloride
0 ImagesCat. No.: HY-W354635CAS No.: 5969-39-1N-Methyl-2-phenylpropan-1-amine hydrochloride is a β-Methylphenethylamine (BMPEA) analog, and has transmitter releasing action at NET and DAT assay.
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Cilobamine
0 ImagesCat. No.: HY-183457CAS No.: 69429-84-1Cilobamine is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine can be used in the research of depression.
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EXP631
0 ImagesCat. No.: HY-183420CAS No.: 151656-58-5EXP631 is a centrally acting non-opioid analgesic that targets serotonin and norepinephrine transporters. EXP631 exhibits activity against acute pain induced by chemical stimuli, stress, and electrical stimulation. EXP631 blocks the reuptake of serotonin and norepinephrine. EXP631 can be used in research related to moderate to moderately severe acute and chronic pain.
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Esreboxetine succinate
0 ImagesCat. No.: HY-14790ACAS No.: 635724-55-9Synonyms: PNU-165442G; (S,S)-Reboxetine succinateEsreboxetine succinate (PNU-165442G; (S,S)-Reboxetine succinate) is a selective norepinephrine transporter (NET) inhibitor, with a pIC50 of 9.6 and a pKi of 9.2 in rats, and it can cross the blood-brain barrier. Esreboxetine succinate increases urethral closure pressure and urethral resistance in rats. Esreboxetine succinate is applicable to research related to inflammatory pain and stress urinary incontinence.
