title: The vesicular monoamine transporter 2: an underexplored pharmacological target.
abstract: Active transport of neurotransmitters into synaptic vesicles is required for their subsequent exocytotic release. In the monoamine system, this process is carried out by the vesicular monoamine transporters (VMAT1 and VMAT2). These proteins are responsible for vesicular packaging of dopamine, norepinephrine, serotonin, and histamine. These proteins are essential for proper neuronal function; however, compared to their plasma membrane counterparts, there are few drugs available that target these vesicular proteins. This is partly due to the added complexity of crossing the plasma membrane, but also to the technical difficulty of assaying for vesicular uptake in high throughput. Until recently, reagents to enable high throughput screening for function of these vesicular neurotransmitter transporters have not been available. Fortunately, novel compounds and methods are now making such screening possible; thus, a renewed focus on these transporters as potential targets is timely and necessary.
authors.affiliation: Department of Environmental Health, Rollins School of Public Health, Emory University, Atlanta, GA 30322, USA.
authors.forename: Alison I
authors.initials: AI
authors.lastname: Bernstein
authors.affiliation: Department of Environmental Health, Rollins School of Public Health, Emory University, Atlanta, GA 30322, USA.
authors.forename: Kristen A
authors.initials: KA
authors.lastname: Stout
authors.affiliation: Department of Environmental Health, Rollins School of Public Health, Emory University, Atlanta, GA 30322, USA; Center for Neurodegenerative Diseases, Emory University, Atlanta, GA 30322, USA; Department of Pharmacology, Emory University, Atlanta, GA 30322, USA; Department of Neurology, Emory University, Atlanta, GA 30322, USA. Electronic address: gwmiller23@yahoo.com.
authors.forename: Gary W
authors.initials: GW
authors.lastname: Miller
mesh_terms: D000818:Animals; D006801:Humans; D001523:Mental Disorders / Q000188:drug therapy / Q000378:metabolism; D009422:Nervous System Diseases / Q000188:drug therapy / Q000378:metabolism; D050493:Vesicular Monoamine Transport Proteins / Q000187:drug effects* / Q000378:metabolism
chemical_list: C493452:SLC18A2 protein, human; D050493:Vesicular Monoamine Transport Proteins
keywords: SLC18A2; Transport; VMAT2; Vesicle