PMID- 20135628
OWN - NLM
STAT- MEDLINE
DCOM- 20120202
LR  - 20231104
IS  - 1098-1128 (Electronic)
IS  - 0198-6325 (Print)
IS  - 0198-6325 (Linking)
VI  - 31
IP  - 4
DP  - 2011 Jul
TI  - Vesicular monoamine transporters: structure-function, pharmacology, and medicinal 
      chemistry.
PG  - 483-519
LID - 10.1002/med.20187 [doi]
AB  - Vesicular monoamine transporters (VMAT) are responsible for the uptake of 
      cytosolic monoamines into synaptic vesicles in monoaminergic neurons. Two closely 
      related VMATs with distinct pharmacological properties and tissue distributions 
      have been characterized. VMAT1 is preferentially expressed in neuroendocrine 
      cells and VMAT2 is primarily expressed in the CNS. The neurotoxicity and 
      addictive properties of various psychostimulants have been attributed, at least 
      partly, to their interference with VMAT2 functions. The quantitative assessment 
      of the VMAT2 density by PET scanning has been clinically useful for early 
      diagnosis and monitoring of the progression of Parkinson's and Alzheimer's 
      diseases and drug addiction. The classical VMAT2 inhibitor, tetrabenazine, has 
      long been used for the treatment of chorea associated with Huntington's disease 
      in the United Kingdom, Canada, and Australia, and recently approved in the United 
      States. The VMAT2 imaging may also be useful for exploiting the onset of diabetes 
      mellitus, as VMAT2 is also expressed in the beta-cells of the pancreas. VMAT1 gene 
      SLC18A1 is a locus with strong evidence of linkage with schizophrenia and, thus, 
      the polymorphic forms of the VMAT1 gene may confer susceptibility to 
      schizophrenia. This review summarizes the current understanding of the 
      structure-function relationships of VMAT2, and the role of VMAT2 on addiction and 
      psychostimulant-induced neurotoxicity, and the therapeutic and diagnostic 
      applications of specific VMAT2 ligands. The evidence for the linkage of VMAT1 
      gene with schizophrenia and bipolar disorder I is also discussed.
CI  - (c) 2010 Wiley Periodicals, Inc.
FAU - Wimalasena, Kandatege
AU  - Wimalasena K
AD  - Department of Chemistry, Wichita State University, Kansas 67260, USA. 
      kandatege.wimalasena@wichita.edu
LA  - eng
GR  - R01 NS039423/NS/NINDS NIH HHS/United States
GR  - R01 NS039423-04/NS/NINDS NIH HHS/United States
GR  - NS 39423/NS/NINDS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Review
DEP - 20100204
PL  - United States
TA  - Med Res Rev
JT  - Medicinal research reviews
JID - 8103150
RN  - 0 (Ligands)
RN  - 0 (Vesicular Monoamine Transport Proteins)
SB  - IM
MH  - Animals
MH  - Central Nervous System Diseases/therapy
MH  - Chemistry, Pharmaceutical
MH  - Humans
MH  - Kinetics
MH  - Ligands
MH  - Structure-Activity Relationship
MH  - Vesicular Monoamine Transport Proteins/antagonists & 
      inhibitors/*chemistry/*pharmacology
PMC - PMC3019297
MID - NIHMS229868
EDAT- 2010/02/06 06:00
MHDA- 2012/02/03 06:00
PMCR- 2012/07/01
CRDT- 2010/02/06 06:00
PHST- 2010/02/06 06:00 [entrez]
PHST- 2010/02/06 06:00 [pubmed]
PHST- 2012/02/03 06:00 [medline]
PHST- 2012/07/01 00:00 [pmc-release]
AID - 10.1002/med.20187 [doi]
PST - ppublish
SO  - Med Res Rev. 2011 Jul;31(4):483-519. doi: 10.1002/med.20187. Epub 2010 Feb 4.