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ML-352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively.1 It is selective for CHT over dopamine, norepinephrine, and serotonin transporters in HEK293 cells expressing human transporters when used at a concentration of 5 μM as well as a panel of 68 G protein-coupled receptors, ion channels, and transporters when used at a concentration of 10 μM. ML-352 (5 μM) increases cell surface expression of CHT without affecting total protein levels.
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1. Identification and characterization of ML352: A novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem. Neurosci. 6(3), 417-427 (2015).