Antagonism of cocaine's stimulant effects on local cerebral glucose utilization by the preferential autoreceptor antagonist (+)-AJ 76
by
Casey BL, Ray CA, Piercey MF
Upjohn Company, Kalamazoo, MI, USA.
J Neural Transm 1996; 103(3):277-85

ABSTRACT

(+)-AJ 76 is a stimulant dopamine (DA) antagonist, which has a putative preferential action at DA nerve terminal autoreceptors. Because it is both a mild stimulant and a DA antagonist, it has previously been suggested that (+)-AJ 76 might antagonize both the euphoria and craving associated with cocaine abuse and withdrawal, respectively. To evaluate this hypothesis further, (+)-AJ 76 was evaluated for its ability to affect cocaine-induced changes in regional brain energy metabolism. Using Sokoloff's 2-deoxyglucose autoradiographic technique, (+)-AJ 76 antagonized the stimulant effect of cocaine. Although classical DA antagonists are known to depress regional brain energy metabolism, (+)-AJ 76 by itself had no effect. It is concluded that the results are consistent with the previously stated hypothesis that (+)-AJ 76 might be useful as a pharmacotherapy for treatment of cocaine abuse.

AJ 76
GBR12909
Cocaine mules
Cocaine hotspots
AJ 76 and UH 232
Dopaminergic agents
"Cocaine antagonists"
AJ 76, UH 232 and dopamine
Monoamines, cocaine and rats
GBR12909: a dopaminergic antidepressant?

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