Vesicular acetylcholine transporter

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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.[1][2] 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.[3] Acetylcholine transport utilizes a proton gradient established by a vacuolar ATPase.

VAChT uptake inhibitors

Radiolabeled compounds

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[4]

References

  1. 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.
  2. 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. doi:10.1073/pnas.93.8.3547. PMC 39647. PMID 8622973.
  3. Waymire, Jack. "Storage of ACh". University of Texas Medical Center.
  4. 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

External links



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