Cocaine self-administration appears to be mediated by dopamine uptake inhibition (1988)

FRANÇAIS :
Les auteurs veulent mettre en évidence le site de fixation associé aux propriétés de potentialisation ou de dépendance de la cocaïne. Chez le rat, l'efficacité des drogues apparentées à la cocaïne pour susciter l'autoadministration est corrélée avec leur efficacité à inhiber la fixation du mazindol tritié aux transporteurs de dopamine dans les noyaux striés. Le récepteur cocaïnique lié à l'abus doit être le site de fixation associé à l'inhibition du recaptage de la dopamine au niveau des terminaisons nerveuses dopaminergiques.
ENGLISH:
1. While cocaine binds to several known sites in the brain, the binding site or receptor associated with its reinforcing or addictive properties has not been identified as such. 2. The identification of the pharmacologically relevant receptor(s) requires that an association exist between the potency of a variety of cocaine of cocaine-related drugs in animal models of substance and their potency at a binding site in the brain. 3. Our experiments indicate that the potencies of cocaine-like drugs in animal studies of drug self-administration are correlated with their potencies in inhibiting 3H-mazindol binding to dopamine transporters in the rat striatum. Cocaine binding to several other presynaptic and postsynaptic binding sites does not appear to be associated with the reinforcing effects of the drug. 4. Thus, the cocaine receptor related to substance abuse appears to be the binding site associated with inhibition of dopamine uptake on the dopaminergic nerve terminals.