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Synthesis and Pharmacology of Ethylphenidate Enantiomers: The Human Transesterification Metabolite o

Synthesis and Pharmacology of Ethylphenidate Enantiomers: The Human Transesterification Metabolite o

  1. testodan
    Ethanol elevates methylphenidate (1) plasma concentrations and yields the metabolite
    ethylphenidate (2). The therapeutic implications are under investigation. The IC50 for dopamine
    reuptake inhibition by (+)-2 was 27 nM compared to 367 nM for cocaine and 1730 nM for
    (-)-2. Binding selectivity for dopamine versus norepinephrine transporters was greater for
    (+)-2 than for cocaine. Intraperitoneal (+)-2 was approximately half as active as (+)-1 in
    stimulating mouse motor activity at 5 mg/kg, but (+)-2 was as active as (+)-1 at 10 mg/kg.