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Vesicular monoamine transporter 2

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Target not currently curated in GtoImmuPdb

Target id: 1012

Nomenclature: Vesicular monoamine transporter 2

Abbreviated Name: VMAT2

Systematic Nomenclature: SLC18A2

Family: SLC18 family of vesicular amine transporters

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 12 514 10q25.3 SLC18A2 solute carrier family 18 member A2
Mouse 12 517 19 54.64 cM Slc18a2 solute carrier family 18 (vesicular monoamine), member 2
Rat 12 515 1q55 Slc18a2 solute carrier family 18 member A2
Previous and Unofficial Names Click here for help
SVMT | VAT2 | SVAT | synaptic vesicular amine transporter | MNAT | vesicular amine transporter 2 | solute carrier family 18 (vesicular monoamine), member 2 | solute carrier family 18 (vesicular monoamine transporter), member 2 | solute carrier family 18 (vesicular monoamine)
Database Links Click here for help
Specialist databases
Bioparadigms SLC Tables SLC18A2 (Hs)
RESOLUTE SLC18A2 (Hs)
Other databases
Alphafold Q05940 (Hs), Q8BRU6 (Mm), Q01827 (Rn)
ChEMBL Target CHEMBL1893 (Hs), CHEMBL4295886 (Mm), CHEMBL4828 (Rn)
DrugBank Target Q05940 (Hs)
Ensembl Gene ENSG00000165646 (Hs), ENSMUSG00000025094 (Mm), ENSRNOG00000008890 (Rn)
Entrez Gene 6571 (Hs), 214084 (Mm), 25549 (Rn)
Human Protein Atlas ENSG00000165646 (Hs)
KEGG Gene hsa:6571 (Hs), mmu:214084 (Mm), rno:25549 (Rn)
OMIM 193001 (Hs)
Orphanet ORPHA356164 (Hs)
Pharos Q05940 (Hs)
UniProtKB Q05940 (Hs), Q8BRU6 (Mm), Q01827 (Rn)
Wikipedia SLC18A2 (Hs)
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
5-hydroxytryptamine Substrate is endogenous in the given species Hs Ki 9x10-7 M pKi 6.0 1
(-)-adrenaline Substrate is endogenous in the given species Hs Ki 1.9x10-6 M pKi 5.7 1
(-)-noradrenaline Substrate is endogenous in the given species Hs Ki 3.4x10-6 M pKi 5.5 1
dopamine Substrate is endogenous in the given species Hs Ki 1.4x10-6 M pKi 5.9 1
histamine Substrate is endogenous in the given species 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 Click here for help
1 amine (in): 2H+ (out)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]TBZOH Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inhibition 8.2 pKd 6
⤷ pKd 8.2 (Kd 6.6x10-9 M) [6]
[125I]iodovinyl-TBZ Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inhibition 8.1 pKd 3
⤷ pKd 8.1 (Kd 8.2x10-9 M) [3]
reserpine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pKi 1
⤷ pKi 7.9 (Ki 1.2x10-8 M) [1]
tetrabenazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.0 pKi 1
⤷ pKi 7.0 (Ki 9.7x10-8 M) [1]
valbenazine Small molecule or natural product Approved drug Primary target of this compound Rn Inhibition 6.7 pKi 2
⤷ pKi 6.7 (Ki 1.87x10-7 M) [2]
Description: Displacement binding assay using rat brain homogenate.
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pKi 1
⤷ pKi 6.3 (Ki 5.4x10-7 M) [1]
[11C]DTBZ Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inhibition - -
⤷
[125I]7-azido-8-iodoketanserine Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inhibition - - 5
⤷ [5]
deutetrabenazine Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition - -
⤷
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology Click here for help
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 USA, 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. Synapse, 18 (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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1012.