title: Effect of non-catecholic 2-aminotetralin derivatives on dopamine metabolism in the rat striatum.
abstract: 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.
mesh_terms: D015081:2-Naphthylamine / Q000031:analogs & derivatives / Q000494:pharmacology*; D015102:3,4-Dihydroxyphenylacetic Acid / Q000378:metabolism; D000818:Animals; D001058:Apomorphine / Q000378:metabolism; D001522:Behavior, Animal / Q000187:drug effects; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism*; D005260:Female; D006719:Homovanillic Acid / Q000378:metabolism; D066298:In Vitro Techniques; D009281:Naphthalenes / Q000494:pharmacology*; D051381:Rats; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D009281:Naphthalenes; D013764:Tetrahydronaphthalenes; D015102:3,4-Dihydroxyphenylacetic Acid; C006561:2-aminotetralin; D015081:2-Naphthylamine; D001058:Apomorphine; D004298:Dopamine; D006719:Homovanillic Acid