Comparison of the properties of central and peripheral binding sites for cocaine.

Cocaine and its analogs bound saturably to membranes of brain and liver of mice. The binding sites on membranes of liver had a lower affinity for cocaine than those of brain. In addition, there were striking differences between the two tissues in regard to the relative potencies of cocaine analogs in competing with [3H]cocaine for binding. In comparison with the binding sites in brain, those in liver had only moderate stereospecificity, and they discriminated less between the centrally active compounds and the centrally inert analogs.