title: Cocaine and cocaethylene binding to human liver.
abstract: The binding of cocaine (COC) and cocaethylene (CE) to whole human liver homogenates in vitro was studied by equilibrium dialysis. Drugs were measured by high-pressure liquid chromatography. Up to 32% of COC and up to 43% of CE were bound. Scatchard analysis suggested a high-affinity, low-capacity binder for both COC (Ka, 4.69 x 10(4) L/mol; Bo, 1.08 x 10(-5) mol/L) and CE (Ka, 4.38 x 10(4) L/mol; Bo, 1.54 x 10(-5) mol/L). In addition, low-affinity, high-capacity binders for COC (Ka, 2.93 x 10(3) L/mol; Bo, 1.32 x 10(-4) mol/L) and CE (Ka, 6.50 x 10(3) L/mol; Bo, 1.11 x 10(-4) mol/L) were noted. Finally, for both compounds, very low-affinity, high-capacity binding, which was likely nonspecific in nature, was defined as follows: COC, Ka, 8.00 x 10(2) L/mol; Bo, 5.45 x 10(-4) mol/L and CE, Ka, 2.10 x 10(3) L/mol; Bo, 3.71 x 10(-4) mol/L. The binding profiles of COC and CE in liver were compared with those in human serum and placenta studied previously by this laboratory.
authors.affiliation: Department of Pathology, University of California Medical Center, San Diego 92103-8320, USA.
authors.forename: D N
authors.initials: DN
authors.lastname: Bailey
mesh_terms: D000328:Adult; D000368:Aged; D000779:Anesthetics, Local / Q000097:blood / Q000378:metabolism*; D003042:Cocaine / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism*; D018765:Dopamine Uptake Inhibitors / Q000097:blood / Q000378:metabolism*; D005260:Female; D006801:Humans; D008099:Liver / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D010920:Placenta / Q000378:metabolism
chemical_list: D000779:Anesthetics, Local; D018765:Dopamine Uptake Inhibitors; C066444:cocaethylene; D003042:Cocaine