Summary
Concentrations of dopamine (DA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were measured in the striatum of rats after i.p. injection of apomorphine, N,N-dipropyldopamine and a series of alkylated and/or esterified dopamine analogues of the dihydroxyaminotetralin type.
All compounds tested caused a decrease in DOPAC- and HVA-concentrations. The N-alkylated derivatives had a rapid onset of action, showing a maximal HVA decrease after 15–45 min, after which time the metabolite concentrations slowly returned to control values. In addition, the dihydroxyaminotetralins, especially N,N-dipropylamino-5,6-dihydroxytetrahydronaphthalene (DiPr-5,6-ADTN), produced a rapid, short lasting elevation of DA concentrations. The esterified primary amines, dibenzoyl-5,6-and dibenzoyl-6,7-dihydroxyaminotetralin, had a delayed effect, causing a maximal HVA decrease after 4–6 h.
DiPr-5,6-ADTN was found to be the most potent compound, with a maximal effect at a dose of 0.33 μmol/kg, it being 30 times more potent than apomorphine and DiPr-6,7-ADTN. The results corroborate reported behavioural data, and the relative potencies of the alkylated derivatives in this test system for dopaminergic activity are in agreement with those based on stereotyped behaviour.
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Feenstra, M.G.P., Rollema, H., Horn, A.S. et al. Effect of dihydroxy-2-aminotetralin derivatives on dopamine metabolism in the rat striatum. Naunyn-Schmiedeberg's Arch. Pharmacol. 310, 219–225 (1980). https://doi.org/10.1007/BF00499913
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DOI: https://doi.org/10.1007/BF00499913