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Cocaine and cocaethylene binding to human tissues: a preliminary study
1Department of Pathology, University of California, San Diego Medical Center 92103-8320, USA.
Therapeutic Drug Monitoring
|June 1, 1996
Summary
Cocaine and cocaethylene bind differently to human tissues. Kidney showed the highest cocaine binding, while brain showed the highest cocaethylene binding, influencing their organ-specific effects.
Area of Science:
- Pharmacology
- Toxicology
- Biochemistry
Background:
- Cocaine (COC) and its metabolite cocaethylene (CE) exhibit distinct pharmacological profiles.
- Understanding tissue distribution is crucial for elucidating target-organ toxicity and activity.
Purpose of the Study:
- To quantify and compare the tissue binding affinities of cocaine and cocaethylene in human tissues.
- To investigate the differential distribution of COC and CE across various human organs.
Main Methods:
- Equilibrium dialysis was employed using human tissue homogenates.
- Cocaine and cocaethylene concentrations were determined using high-pressure liquid chromatography (HPLC).
- Binding was assessed at 10 and 50 microM concentrations for both compounds.
Main Results:
- Kidney exhibited the highest binding for cocaine, while serum showed the least.
- Brain demonstrated the highest binding for cocaethylene, with serum showing minimal binding.
- Heart, placenta, and liver displayed intermediate binding levels for both substances.
Conclusions:
- Significant variations in tissue binding exist between cocaine and cocaethylene.
- Differential tissue distribution likely contributes to the specific target-organ effects observed for COC and CE.
- These findings aid in understanding the toxicological and pharmacological mechanisms of these compounds.