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  • 1
    Electronic Resource
    Electronic Resource
    Further in vitro and in vivo studies with the putative presynaptic dopamine agonist N,N-dipropyl-7-hydroxy-2-aminotetralin (1987)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 336 (1987), S. 494-501 
    Details
    ISSN: 1432-1912
    Keywords: Aminotetralins ; Dopamine autoreceptors ; In vitro receptor binding ; Dopamine uptake sites ; Dopamine uptake inhibitors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The in vitro binding of the putative dopamine autoreceptor agonist [3H]DP-7-ATN to rat striatal membrane homogenates was investigated. The maximum number of binding sites B max was 497.5 ± 50.2 fmol/mg protein and the affinity constant K D was 8.3 ± 1.5 nM using 10 μM (+) butaclamol to define non-specific binding. Lesion of the left medium forebrain bundle by 6-hydroxydopamine resulted in an almost complete loss of dopamine in the striatum but did not affect the binding of [3H]DP-7-ATN. The binding of [3H]DP-7-ATN to the homogenates of the dopaminergic cell bodies in the substantia nigra revealed a B max of 542.4 ± 40.1 fmol/mg protein and a K D of 11.1 ± 1.3 nM. The pharmacological profile of the binding was characterized as being to D-2 receptors. No direct in vitro evidence could be found for a selective binding to DA autoreceptors. The dopamine uptake inhibitor GBR 12909 interacted in a noncompetitive manner with the in vitro binding of [3H]DP-7-ATN and the latter compounds uptake into isolated synaptosomes was not through the specific dopamine uptake system but rather through diffusion. GBR 12909 failed to reveal any agonistic or antagonistic activity in the GBL model but was able to antagonize the hypomotility in rats induced by 0.25 mg/kg DP-7-ATN. The inhibitory effect of DP-7-ATN on DA release was also demonstrated using in vivo brain dialysis in conscious rats. Based on the above results, the possibility is discussed that the release regulating DA autoreceptors, which might be coupled to the reuptake complex, and the DA biosynthesis regulating autoreceptors, are different entities.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00169305
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    Paper (German National Licenses)
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  • 2
    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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    Paper (German National Licenses)
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  • 3
    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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  • 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 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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