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  • 1
    Electronic Resource
    Electronic Resource
    Neurochemical and behavioural profiles of five dopamine analogues (1981)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 316 (1981), S. 304-310 
    Details
    ISSN: 1432-1912
    Keywords: Stereotypy ; Dopamine metabolism ; Gammabutyrolactone ; Dopamine agonist ; Ester ; Aminotetralin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The dopaminergic actions of five hydroxylated dopamine analogues have been examined for: i) Ability to induce stereotypy, ii) Effects upon dopamine metabolism, iii) Ability to antagonise the rise in striatal dopamine caused by gammabutyrolactone. With the exception of the resorcinol derivative 2-(3,5-dihydroxyphenyl)-N,N-dipropylethylamine, all of the compounds tested exhibited dopamine-like actions, and similarities were found in the induction of stereotypy and in the reduction of dopamine metabolism. For example, 2-(3-hydroxyphenyl)-N,N-dipropylethylamine had a short duration of action as far as reducing dopamine metabolism and inducing stereotypy were concerned. On the other hand, 2-(3-hydroxyphenyl)-N-n-propyl-N-phenylethyl-cthylamine (e) and also 5-hydroxy-2-(N-n-propyl-N-phenylethyl)-aminotetralin had a long duration of agonist-like effects upon both parameters, the aminotetralin derivative being the more potent of the two. Thus, in going from the simple dopamine-like structure to the aminotetralin compound there has been an increase in dopamine agonist-like activity. The differences in dopamine agonist potency of the drugs used are discussed in relation to the structure of these compounds, and are compared with the potencies of related compounds. Also, the potencies of the compounds under investigation upon presynaptic dopamine receptors (using the gammabutyrolactone model as a test system) were investigated, and the ester, 2-(3-benzoyloxyphenyl)-N-n-propyl-N-phenylethyl-ethylamine was the most potent. This ester, which is probably converted to (e) in the brain, also had a long duration of action in the stereotypy and dopamine metabolism tests. The results suggest that certain of the compounds might be useful leads for the design of dopamine agonists of possible clinical use.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00501362
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  • 2
    Electronic Resource
    Electronic Resource
    Effect of dihydroxy-2-aminotetralin derivatives on dopamine metabolism in the rat striatum (1980)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 310 (1980), S. 219-225 
    Details
    ISSN: 1432-1912
    Keywords: Dihydroxyaminotetralins ; Apomorphine ; Prodrugs ; Striatum ; Dopamine metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: 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.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00499913
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Effect of non-catecholic 2-aminotetralin derivatives on dopamine metabolism in the rat striatum (1980)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 313 (1980), S. 213-219 
    Details
    ISSN: 1432-1912
    Keywords: 2-Aminotetralins ; Dopamine agonists ; Dopamine metabolism ; Striatum ; Structure activity relations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: 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 μmol/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 μmol/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 α rotamer of dopamine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00505736
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    Paper (German National Licenses)
    Fulltext
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