Abstract
The aminotetralins (+)-AJ76 and (+)-UH232 are stimulant dopaminergic antagonists, which may preferentially antagonize autoreceptors of dopamine nerve terminals. Both agents antagonized cocaine's depressant effects on firing rates of ventral tegmental dopaminergic neurons, but (+)-UH232 was much more potent. When injected simultaneously with cocaine, (+)-UH232 inhibited and (+)-AJ76 enhanced the locomotor stimulation observed during the first 30 min following s.c. cocaine administration. However, (+)-AJ76 antagonized cocaine-induced stereotypies as well as the later more intense cocaine locomotor stimulation. It is suggested that preferential dopamine autoreceptor antagonists may provide a novel approach to a pharmacotherapy for treating cocaine abuse.
MeSH terms
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3,4-Dihydroxyphenylacetic Acid / metabolism
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8-Hydroxy-2-(di-n-propylamino)tetralin / analogs & derivatives*
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8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
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Animals
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Behavior, Animal / drug effects*
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Brain Chemistry / drug effects
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Cocaine / antagonists & inhibitors*
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Dihydroxyphenylalanine / metabolism
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Dopamine / metabolism
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Dopamine Antagonists*
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Electrophysiology
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Homovanillic Acid / metabolism
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Male
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Microelectrodes
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Motor Activity / drug effects
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Rats
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Rats, Sprague-Dawley
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Tetrahydronaphthalenes / pharmacology*
Substances
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Dopamine Antagonists
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Tetrahydronaphthalenes
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3,4-Dihydroxyphenylacetic Acid
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Dihydroxyphenylalanine
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8-Hydroxy-2-(di-n-propylamino)tetralin
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5-methoxy-1-methyl-2-(n-propylamino)tetralin
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UH 232
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Cocaine
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Dopamine
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Homovanillic Acid