title: The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.
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.
authors.affiliation: Department of Physiology and Pharmacology, Wake Forest University Health Sciences, Winston-Salem, NC 27157, USA.
authors.forename: Gennady B
authors.initials: GB
authors.lastname: Lapa
authors.forename: Gary D
authors.initials: GD
authors.lastname: Byrd
authors.forename: Alla A
authors.initials: AA
authors.lastname: Lapa
authors.forename: Evgeny A
authors.initials: EA
authors.lastname: Budygin
authors.forename: Steven R
authors.initials: SR
authors.lastname: Childers
authors.forename: Sara R
authors.initials: SR
authors.lastname: Jones
authors.forename: Jill J
authors.initials: JJ
authors.lastname: Harp
mesh_terms: D050483:Dopamine Plasma Membrane Transport Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; D010880:Piperidines