Vesicular acetylcholine transporter

The Vesicular acetylcholine transporter (VAChT) is a neurotransmitter transporter which is responsible for loading acetylcholine (ACh) into secretory organelles in neurons making acetylcholine available for secretion.[5][6] It is encoded by Solute carrier family 18, member 3 (SLC18A3) gene, located within the first intron of the choline acetyltransferase gene. VAChT is able to transport ACh into vesicles by relying on an exchange between protons (H+) that were previously pumped into the vesicle diffusing out, thus acting as an antiporter. ACh molecules are then carried into the vesicle by the action of exiting protons.[7] Acetylcholine transport utilizes a proton gradient established by a vacuolar ATPase.

SLC18A3
Identifiers
AliasesSLC18A3, VACHT, solute carrier family 18 member A3, CMS21
External IDsOMIM: 600336; MGI: 1101061; HomoloGene: 11022; GeneCards: SLC18A3; OMA:SLC18A3 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_003055

NM_021712

RefSeq (protein)

NP_003046

NP_068358

Location (UCSC)Chr 10: 49.61 – 49.61 MbChr 14: 32.18 – 32.19 Mb
PubMed search[3][4]
Wikidata
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VAChT uptake inhibitors

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Radiolabeled compounds

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PET imaging of the VAChT may provide insights into early diagnosis of Alzheimer's disease.

  • (−)-trans-2-Hydroxy-3-(4-(4-[18F]fluorobenzoyl)piperidino)tetralin; racemate: Ki = 2.70 nM for VAChT, 191 nM for σ1, and 251 nM for σ2[8]

References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000187714Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000100241Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ Erickson JD, Varoqui H (Dec 2000). "Molecular analysis of vesicular amine transporter function and targeting to secretory organelles". FASEB Journal. 14 (15): 2450–8. doi:10.1096/fj.00-0206rev. PMID 11099462. S2CID 15305436.
  6. ^ Weihe E, Tao-Cheng JH, Schäfer MK, Erickson JD, Eiden LE (Apr 1996). "Visualization of the vesicular acetylcholine transporter in cholinergic nerve terminals and its targeting to a specific population of small synaptic vesicles". Proceedings of the National Academy of Sciences of the United States of America. 93 (8): 3547–52. Bibcode:1996PNAS...93.3547W. doi:10.1073/pnas.93.8.3547. PMC 39647. PMID 8622973.
  7. ^ Waymire J. "Storage of ACh". University of Texas Medical Center.
  8. ^ Tu Z, Efange SM, Xu J, Li S, Jones LA, Parsons SM, Mach RH (Mar 2009). "Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter". Journal of Medicinal Chemistry. 52 (5): 1358–69. doi:10.1021/jm8012344. PMC 2765529. PMID 19203271.

Further reading

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