The vesicular monoamine transporter 2: an underexplored pharmacological target

Neurochem Int. 2014 Jul;73:89-97. doi: 10.1016/j.neuint.2013.12.003. Epub 2014 Jan 4.

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.

Keywords: SLC18A2; Transport; VMAT2; Vesicle.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Humans
  • Mental Disorders / drug therapy
  • Mental Disorders / metabolism
  • Nervous System Diseases / drug therapy
  • Nervous System Diseases / metabolism
  • Vesicular Monoamine Transport Proteins / drug effects*
  • Vesicular Monoamine Transport Proteins / metabolism

Substances

  • SLC18A2 protein, human
  • Vesicular Monoamine Transport Proteins