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  • Dopamine agonist  (2)
  • carbon taxes  (2)
  • Dopamine agonists  (1)
  • 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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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    A comparison of the potencies of various dopamine receptor agonists in models for pre- and postsynaptic receptor activity (1983)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 324 (1983), S. 108-115 
    Details
    ISSN: 1432-1912
    Keywords: Dopamine agonists ; 2-Aminotetralins ; γ-Butyrolactone ; Presynaptic dopamine receptors ; Homovanillic acid
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Several dopamine (DA) receptor agonists, notably N,N-dipropyl-2-aminotetralin analogues differing in the number and position of phenolic hydroxyl groups, were evaluated in model systems for pre- and postsynaptic dopaminergic activity. Apomorphine, piribedil and pergolide were included for comparison. All compounds inhibited the γ-butyrolactone (GBL)-induced increase in DA concentrations in the rat striatum and olfactory tubercle, although a dosedependency could not be demonstrated for one of the compounds, i.e. N,N-dipropyl-2-amino-5,6-dihydroxytetralin. In addition to the reversal of the DA-increase all compounds decreased the HVA and DOPAC levels in a dose-dependent manner, in much the same way as in normal, non GBL-pretreated rats. The potencies of the drugs to decrease HVA in normal rats and to inhibit the DA-increase and to decrease HVA in GBL-pretreated rats, both in the striatum and the olfactory tubercle were compared with each other and with the potencies to induce stereotyped behaviour. It may be concluded that (1) N,N-dipropyl-2-amino-7-hydroxytetralin shows the largest difference in activity in the biochemical and the behavioural models, suggesting a selective presynaptic activity. This was corroborated by the appearance of a marked hypomotility after low doses of this compound; (2) The potencies to decrease striatal HVA concentrations are generally somewhat different from the potencies to inhibit GBL-induced DA-increases, but appear to be comparable to the potencies to inhibit GBL-induced dihydroxyphenylalanine (DOPA)-increases; (3) There is no indication that the DA agonists in general are more potent at presynaptic receptors in the tubercle than in the striatum.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00497015
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacological profile of non-hydroxylated and ether derivatives of the potent D2-selective agonist N-0437 (1991)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 343 (1991), S. 134-142 
    Details
    ISSN: 1432-1912
    Keywords: Aminotetralins ; Dopamine agonist ; Microdialysis ; 6-Hydroxydopamine ; Prodrugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Derivatives of the potent dopamine D2-selective agonist 2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetralin (N-0437) were designed, aimed at producing drugs with less sensitivity towards metabolic inactivation (in particular glucuronidation at the 5-OH position). Since aminotetralins with a 5-methoxy substituent or lacking the 5-hydroxy group have been reported to retain dopaminergic activity, the non-5-hydroxylated N-0437 (N-0918) and two ethers of N-0437 [5-methoxyN-0437 (N-0724) and 5-cyclopentoxy-N-0437 (N-0953)] have been prepared and tested. Three indices for activity at central dopamine receptors are considered: (1) the displacement of (3 H)-SCH-23390 and (3H)-spiperone from calf caudate membranes, (2) the effects on dopamine release and metabolism in the striatum of freely moving rats after systemic and intrastriatal administration as assessed by brain microdialysis, and (3) the ability to elicit contralateral turning in rats with a unilateral 6-OH-dopamine lesion of the nigrostriatal pathway. In order to differentiate between direct dopaminergic activity and metabolic activation, brain and plasma levels of N-0437 after administration of N-0724 and N-0953 were measured. The results show the necessity of the 5-OH group for direct dopaminergic activity: N-0918, N-0724 and N-0953 are all inactive after intrastriatal administration in the microdialysis model and all three drugs show a weak in vitro affinity for both D1 and D2 receptors. Although N-0918 is also inactive after systemic administration in the microdialysis and turning model, N-0724 and N-0953 do exhibit dopaminergic activity after systemic administration in these models. Because of the in vivo formation of N-0437 after N-0724 and N-0953 administration, it is hypothesized that this dopaminergic activity is the result of metabolic activation. The cyclopentoxy group (present in N-0953) then appears to be an interesting prodrug moiety because it seems to give rise to small (but sufficient) and constant N-0437 levels in the brain. Deceased January 2, 1990 Send offprint requests to J. M. Jansen at the above address
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00168600
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  • 4
    Electronic Resource
    Electronic Resource
    Hybrid carbon incentive mechanisms and political acceptability (1997)
    Springer
    Environmental and resource economics 9 (1997), S. 43-63 
    Details
    ISSN: 1573-1502
    Keywords: carbon pollution credits ; carbon taxes ; environmental policy ; externalities ; hybrid instruments ; tradeable carbon permits
    Source: Springer Online Journal Archives 1860-2000
    Topics: Energy, Environment Protection, Nuclear Power Engineering , Economics
    Notes: Abstract This paper analyses how hybrid systems of carbon taxes and tradeable permits optimize some conflicting dimensions of political acceptability related to the design of these instruments. Pure systems like taxes without exemptions or auctioned tradeable permits cause problems for political acceptability in open economies due to high overall costs (abatement cost plus payments on the tax or auctions) for current polluters. Unfortunately, pure systems based on grandfathering of emission rights across the board do not provide a feasible alternative because of monitoring and enforcement problems. In contrast, consciously designed hybrid systems employ grandfathering of emission rights together with either carbon taxes or auctioned carbon permits in order to overcome acceptability problems of pure systems, while leaving incentives to reduce emissions at the margin untouched. Moreover, monitoring and enforcement costs of the hybrid systems are less due to the lower number of participating agents compared with the pure systems, while opportunities for costor burden-sharing exist as well.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02441369
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    Paper (German National Licenses)
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  • 5
    Electronic Resource
    Electronic Resource
    Hybrid Carbon Incentive Mechanisms and Political Acceptability (1997)
    Springer
    Environmental and resource economics 9 (1997), S. 43-63 
    Details
    ISSN: 1573-1502
    Keywords: carbon pollution credits ; carbon taxes ; environmental policy ; externalities ; hybrid instruments ; tradeable carbon permits
    Source: Springer Online Journal Archives 1860-2000
    Topics: Energy, Environment Protection, Nuclear Power Engineering , Economics
    Notes: Abstract This paper analyses how hybrid systems of carbon taxes and tradeable permits optimize some conflicting dimensions of political acceptability related to the design of these instruments. Pure systems like taxes without exemptions or auctioned tradeable permits cause problems for political acceptability in open economies due to high overall costs (abatement cost plus payments on the tax or auctions) for current polluters. Unfortunately, pure systems based on grandfathering of emission rights across the board do not provide a feasible alternative because of monitoring and enforcement problems. In contrast, consciously designed hybrid systems employ grandfathering of emission rights together with either carbon taxes or auctioned carbon permits in order to overcome acceptability problems of pure systems, while leaving incentives to reduce emissions at the margin untouched. Moreover, monitoring and enforcement costs of the hybrid systems are less due to the lower number of participating agents compared with the pure systems, while opportunities for cost- or burden-sharing exist as well.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1026451607522
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    Paper (German National Licenses)
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