Abstract
Ethanol elevates methylphenidate (1) plasma concentrations and yields the metabolite ethylphenidate (2). The therapeutic implications are under investigation. The IC(50) 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.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Animals
-
Cell Line
-
Cocaine / metabolism
-
Dopamine Plasma Membrane Transport Proteins
-
Esterification
-
Ethanol / metabolism*
-
Humans
-
Male
-
Membrane Glycoproteins / metabolism
-
Membrane Transport Proteins / metabolism
-
Methylphenidate / analogs & derivatives*
-
Methylphenidate / chemistry*
-
Methylphenidate / metabolism*
-
Methylphenidate / pharmacology
-
Mice
-
Mice, Inbred C57BL
-
Motor Activity / drug effects
-
Nerve Tissue Proteins / metabolism
-
Norepinephrine Plasma Membrane Transport Proteins
-
Protein Binding
-
Radioligand Assay
-
Receptors, Dopamine / metabolism
-
Receptors, Serotonin / metabolism
-
Stereoisomerism
-
Structure-Activity Relationship
-
Symporters / metabolism
Substances
-
Dopamine Plasma Membrane Transport Proteins
-
Membrane Glycoproteins
-
Membrane Transport Proteins
-
Nerve Tissue Proteins
-
Norepinephrine Plasma Membrane Transport Proteins
-
Receptors, Dopamine
-
Receptors, Serotonin
-
SLC6A2 protein, human
-
Slc6a2 protein, mouse
-
Symporters
-
Methylphenidate
-
Ethanol
-
ethylphenidate
-
Cocaine