The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines

…, AA Lapa, EA Budygin, SR Childers, SR Jones…

Index: Lapa, Gennady B.; Byrd, Gary D.; Lapa, Alla A.; Budygin, Evgeny A.; Childers, Steven R.; Jones, Sara R.; Harp, Jill J. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4915 - 4918

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Citation Number: 10

Abstract

The synthesis of potent 4-aryl methoxypiperidinol 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. 4-[Bis (4-fluorophenyl) methoxy]-1- methylpiperidine has an IC50 of 22.1±5.73 nM and increases locomotor activity in mice.