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Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on Threo-methylphenidate and its analogs

1997; Elsevier BV; Volume: 7; Issue: 9 Linguagem: Inglês

10.1016/s0960-894x(97)00193-5

1464-3405

Mark Froimowitz, Howard M. Deutsh, Quing Shi, Kuo-Ming Wu, Robert Glaser, Itay Adin, Clifford George, Margaret M. Schweri,

Neuroscience and Neuropharmacology Research

N-methyl derivatives of methylphenidate and four analogs were synthesized and assayed for affinity at the dopamine transporter. The binding affinities of the N-methyl compounds were consistently lower by a factor ranging from 4 to 30 as compared with the corresponding secondary amine. This is consistent with the predictions of a pharmacophore model of compounds that bind to the dopamine transporter.