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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.[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.
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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[8]
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Tayebati SK, El-Assouad D, Ricci A, Amenta F (Nov 2002). "Immunochemical and immunocytochemical characterization of cholinergic markers in human peripheral blood lymphocytes". Journal of Neuroimmunology. 132 (1–2): 147–55. doi:10.1016/s0165-5728(02)00325-9. PMID12417445. S2CID20921312.
Chireux MA, Le Van Thai A, Weber MJ (Mar 1995). "Human choline acetyltransferase gene: localization of alternative first exons". Journal of Neuroscience Research. 40 (4): 427–38. doi:10.1002/jnr.490400402. PMID7616604. S2CID42856768.
This page was last edited on 27 March 2024, at 10:03