Effect of non-catecholic 2-aminotetralin derivatives on dopamine metabolism in the rat striatum

The concentrations of dopamine (DA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were measured in the striatum of rats after i.p. injection of dipropyl-2-aminotetralin and the four positional isomers of monohydroxy-dipropyl-2-aminotetralin. All compounds except 8-OH dipropylaminot...

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Published in:Naunyn-Schmiedeberg's archives of pharmacology 1980-09, Vol.313 (3), p.213-219
Main Authors: Feenstra, M G, Rollema, H, Dijkstra, D, Grol, C J, Horn, A S, Westerink, B H
Format: Article
Language:English
Subjects:
2-Naphthylamine - analogs & derivatives
2-Naphthylamine - pharmacology
3,4-Dihydroxyphenylacetic Acid - metabolism
Animals
Apomorphine - metabolism
Behavior, Animal - drug effects
Corpus Striatum - drug effects
Corpus Striatum - metabolism
Dopamine - metabolism
Female
Homovanillic Acid - metabolism
In Vitro Techniques
Naphthalenes - pharmacology
Rats
Tetrahydronaphthalenes - pharmacology
Time Factors
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Summary:The concentrations of dopamine (DA), dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were measured in the striatum of rats after i.p. injection of dipropyl-2-aminotetralin and the four positional isomers of monohydroxy-dipropyl-2-aminotetralin. All compounds except 8-OH dipropylaminotetralin caused a decrease in DOPAC- and HVA-concentrations. In addition, 5-OH-dipropylaminotetralin produced a small elevation in DA concentrations. In contrast, 7-OH dipropylaminotetralin, in doses of 100 mumol/kg and more, decreased DA to 50% and initially increased HVA and DOPAC to about 200%, after which the concentrations of the metabolites fell to 30% or less. The 5-OH isomer was found to be the most potent compound, decreasing HVA concentrations to 70% at a dose of 0.14 mumol/kg. The potencies are compared to those of catechol-group containing DA-agonists such as apomorphine and N,N-dipropyl-5,6-dihydroxy-2-aminotetralin. In addition, a comparison is made with reported behavioural data. It is suggested that the more active N-alkylated 2-aminotetralins have a conformation which corresponds to that of the alpha rotamer of dopamine.
ISSN:0028-1298
1432-1912
DOI:10.1007/BF00505736