The tissue binding of cocaine (COG) and cocaethylene (CE) was investig
ated by equilibrium dialysis of homogenates of whole human tissue supp
lemented with either COC or CE at concentrations of 10 and 50 mu M for
each drug. Concentrations of COC and CE were measured by high-pressur
e liquid chromatography. Kidney bound COC predominantly whereas serum
bound it the least (about one tenth as much). In contrast, for CE, mos
t binding was noted to brain with the least to serum (about one twenti
eth as much). Heart, placenta, and liver showed intermediate binding o
verall. The binding of COC and CE to these tissues may be important in
understanding specific target-organ activity of both compounds.