Vesicular monoamine transporter 2

Target id: 1012

Nomenclature: Vesicular monoamine transporter 2

Abbreviated Name: VMAT2

Systematic Nomenclature: SLC18A2

Family: SLC18 family of vesicular amine transporters

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Vesicular monoamine transporter 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 514 10q25 SLC18A2 solute carrier family 18 member A2
Mouse - 517 19 54.64 cM Slc18a2 solute carrier family 18 (vesicular monoamine)
Rat - 515 1q55 Slc18a2 solute carrier family 18 member A2
Previous and Unofficial Names
SVMT | VAT2 | SVAT | MNAT | synaptic vesicular amine transporter | vesicular amine transporter 2 | solute carrier family 18 (vesicular monoamine), member 2 | solute carrier family 18 (vesicular monoamine transporter), member 2
Database Links
Specialist databases
Bioparadigms SLC Tables SLC18A2 (Hs)
Other databases
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
Orphanet
UniProtKB
Wikipedia
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
5-hydroxytryptamine Hs Ki 9x10-7 M pKi 6.0 1
(-)-adrenaline Hs Ki 1.9x10-6 M pKi 5.7 1
(-)-noradrenaline Hs Ki 3.4x10-6 M pKi 5.5 1
dopamine Hs Ki 1.4x10-6 M pKi 5.9 1
histamine Hs Ki 1.43x10-4 M pKi 3.8 1
β-phenylethylamine Hs Ki 3.7x10-6 M pKi 5.4 1
dexamfetamine Hs Ki 2.1x10-6 M pKi 5.7 1
MPP+ Hs Ki 8.9x10-6 M pKi 5.1 1
MDMA Hs Ki 6.9x10-6 M pKi 5.2 1
fenfluramine Hs Ki 5.1x10-6 M pKi 5.3 1
Stoichiometry
1 amine (in): 2H+ (out)

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]TBZOH Hs Inhibition 8.2 pKd 6
pKd 8.2 (Kd 6.6x10-9 M) [6]
[125I]iodovinyl-TBZ Hs Inhibition 8.1 pKd 3
pKd 8.1 (Kd 8.2x10-9 M) [3]
reserpine Hs Inhibition 7.9 pKi 1
pKi 7.9 (Ki 1.2x10-8 M) [1]
tetrabenazine Hs Inhibition 7.0 pKi 1
pKi 7.0 (Ki 9.7x10-8 M) [1]
valbenazine Rn Inhibition 6.7 pKi 2
pKi 6.7 (Ki 1.87x10-7 M) [2]
Description: Displacement binding assay using rat brain homogenate.
ketanserin Hs Inhibition 6.3 pKi 1
pKi 6.3 (Ki 5.4x10-7 M) [1]
[11C]DTBZ Hs Inhibition - -
[125I]7-azido-8-iodoketanserine Hs Inhibition - - 5
[5]
deutetrabenazine Hs Inhibition - -
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Brain dopamine-serotonin vesicular transport disease
Orphanet: ORPHA352649
References:  4

References

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1. Erickson JD, Schafer MK, Bonner TI, Eiden LE, Weihe E. (1996) Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter. Proc. Natl. Acad. Sci. U.S.A.93 (10): 5166-71. [PMID:8643547]

2. Gano KW. (2013) Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-A]isoquinolin-2-ol compounds and methods relating thereto. Patent number: US8357697 B2. Assignee: Neurocrine Biosciences, Inc.. Priority date: 08/11/2006. Publication date: 22/01/2013.

3. Kung MP, Canney DJ, Frederick D, Zhuang Z, Billings JJ, Kung HF. (1994) Binding of 125I-iodovinyltetrabenazine to CNS vesicular monoamine transport sites. Synapse18 (3): 225-32. [PMID:7855735]

4. Rilstone JJ, Alkhater RA, Minassian BA. (2013) Brain dopamine-serotonin vesicular transport disease and its treatment. N. Engl. J. Med.368 (6): 543-50. [PMID:23363473]

5. Sievert MK, Ruoho AE. (1997) Peptide mapping of the [125I]Iodoazidoketanserin and [125I]2-N-[(3'-iodo-4'-azidophenyl)propionyl]tetrabenazine binding sites for the synaptic vesicle monoamine transporter. J. Biol. Chem.272 (41): 26049-55. [PMID:9325342]

6. Varoqui H, Erickson JD. (1996) Active transport of acetylcholine by the human vesicular acetylcholine transporter. J. Biol. Chem.271 (44): 27229-32. [PMID:8910293]

How to cite this page

SLC18 family of vesicular amine transporters: Vesicular monoamine transporter 2. Last modified on 19/08/2015. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1012.