19130-92-8Relevant articles and documents
Synthesis and pharmacology of ethylphenidate enantiomers: The human transesterification metabolite of methylphenidate and ethanol
Patrick, Kennerly S.,Williard, Robin L.,VanWert, Adam L.,Dowd, Justin J.,Oatis Jr., John E.,Middaugh, Lawrence D.
, p. 2876 - 2881 (2007/10/03)
Ethanol elevates methylphenidate (1) plasma concentrations and yields the metabolite ethylphenidate (2). The therapeutic implications are tinder 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.
