The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines
Graphical abstract
The development of potent 4-(arylmethoxy)-1-alkylpiperidine inhibitors of the dopamine transporter is described. Symmetrical para substituents of the benzene rings are important for high potency in binding to the dopamine transporter. 3b has an IC50 = 22.1 ± 5.73 nM and elevates locomotor activity in mice, 3g has an IC50 = 12.1 ± 7.51 nM and is inactive in this test.
Section snippets
Acknowledgments
This work was supported by Wake Forest University School of Medicine Venture Funds, National Center for Minority Health and Health Disparities Grant MD00232 and National Institutes of Health Grant AA014091.
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