Stimulus generalization from cocaine to analogs with high in vitro affinity for dopamine uptake sites

Results indicate that phenyltropane derivatives of cocaine are from 6–13 times more potent than cocaine in producing cocaine-appropriate responding, providing further evidence in support of the importance of dopamine uptake inhibition for the behavioral effects of cocaine, and suggests utility of these compounds in understanding cocaine abuse.

Abstract

Previous research has shown that phenyltropane derivatives of cocaine are very potent ligands for dopamine transporters in in vitro binding and uptake, and in in vivo binding assays. In the present study, these analogs were tested for their ability to substitute for cocaine in rats trained to discriminate cocaine from saline. Results indicate that these compounds are from 6-13 times more potent than cocaine in producing cocaine-appropriate responding. This provides further evidence in support of the importance of dopamine uptake inhibition for the behavioral effects of cocaine, and suggests utility of these compounds in understanding cocaine abuse.