Monoamine transporters (MATs) are a subfamily of the larger neurotransmitter:sodium symporters (NSSs), which includes transporters from prokaryotic to human, and are members of the solute carrier 6 (SLC6) family of human transporters. Dopamine (DA) transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) are the three main members of MATs. By reabsorbing dopamine, serotonin, and norepinephrine from extra-neuronal regions, MATs control neurotransmission and uphold neurotransmitter homeostasis.
In the plasma membranes of monoaminergic neurons, MATs are transmembrane proteins. In order to transport monoamines into or out of neurons, these proteins rely on ion (Na+, Cl) gradients as their energy source. The vesicular monoamine transporters 1 and 2 (VMAT1 and VMAT2) are found in the membrane of intracellular synaptic vesicles. They use a proton gradient as their energy source to sequester cytosolic monoamines into the vesicles and then release the monoamines into synaptic cleft by exocytosis. Depression, anxiety disorders, attention deficit hyperactivity disorder, obsessive-compulsive disorder, substance use disorders, epilepsy, Parkinson's disease, and autism spectrum disorder have all been linked to dysregulation of MATs. As a result, MATs are pharmacological targets for a number of neuropsychiatric and neurodegenerative diseases.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
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V34109 | (+)-Tetrabenazine | 1026016-83-0 | Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a potent and reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2) which inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1. |
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V3922 | Deutetrabenazine (SD-809) | 1392826-25-3 | Deutetrabenazine (formerly known as SD-809;GTPL8707; tetrabenazine-d6; trade name Austedo), the hexa-deuterated form of tetrabenazine, is anorally bioactive, small-molecule vesicular monoamine transporter 2 (VMAT2) inhibitor which has been approved by FDA in 2017 for the treatment of chorea associated with Huntingtons disease and tardive dyskinesia. |
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V4955 | Radafaxine HCl | 106083-71-0 | Radafaxine HCl (also known as GW-353162A) is a novel and potent DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, it is also an nAChR family modulator. |
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V1862 | Tetrabenazine (Xenazine) | 58-46-8 | Tetrabenazine (Ro 1-9569; trade name: Nitoman and Xenazin), a VMAT-inhibitor, is an FDA approved drug for the treatment of symptomatic treatment of hyperkinetic movement disorder. |
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V29528 | Tetrabenazine Racemate | 718635-93-9 | Tetrabenazine Racemate (Ro 1-9569 Racemate) is a selective and reversible VMAT-2 inhibitor. |
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V2960 | Valbenazine | 1025504-45-3 | Valbenazine (formerly NBI98854; MT5199;NBI-98854; MT-5199; trade name:Ingrezza)is a potent and selective inhibitor of VMAT2 (vesicular monoamine transporter 2) with potential usefulness in the treatment of TD/tardive dyskinesia(uncontrollable movement of the face, tongue, or other body parts). |
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