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.
Reference:
[1]. Ennis, E.A., Wright, J., Retzlaff, C.L., et al. Identification and characterization of ML352: A novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem. Neurosci. 6(3), 417-427 (2015).