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  • 1
    Electronic Resource
    Electronic Resource
    The dopamine D3-receptor: A postsynaptic receptor inhibitory on rat locomotor activity (1993)
    Springer
    Journal of neural transmission 94 (1993), S. 11-19 
    Details
    ISSN: 1435-1463
    Keywords: Dopamine ; release ; D 3 receptor ; locomotor activity ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary We report on the pharmacological effects of the 20 fold D 3 vs. D 2 dopamine receptor preferring compound U 99194 A. It is shown that U 99194 A increases rat locomotor activity at doses that do not increase release or utilisation of dopamine in the striatum or the nucleus accumbens significantly. The data do not support any direct agonist action of U 99194 A at dopamine receptors. It is suggested that U 99194 A can antagonise a population of postsynaptic dopamine receptors involved in the suppression of some aspects of psychomotor activity. These postsynaptic receptors presumably belong to the D 3 receptor subtype.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01244979
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Selective blockade of brainα 2-autoreceptors by yohimbine: Effects on motor activity and on turnover of noradrenaline and dopamine (1982)
    Springer
    Journal of neural transmission 55 (1982), S. 111-120 
    Details
    ISSN: 1435-1463
    Keywords: Motor activity ; turnover ; noradrenaline ; dopamine ; α-autoreceptors ; postsynapticα-receptors ; yohimbine ; prazosin ; mouse
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The motor activity of groups of three mice was increased by yohimbine at doses up to 3 mg/kg intraperitoneally. The turnover of dopamine and noradrenaline in the mouse brain, as assessed by the disappearance of catecholamines following treatment with the tyrosine hydroxylase inhibitorα-methyltyrosine, was accelerated by yohimbine with a peak effect after 10 mg/kg intraperitoneally. Prazosin (3 mg/kg i.p.) completely antagonized the stimulatory effect of yohimbine on motor activity and on dopamine turnover but it somewhat potentiated the stimulatory effect on the turnover of noradrenaline. Amphetamine reversed the prazosin-induced hypomotility, indicating that prazosin can selectively block postsynapticα 1-receptors. Yohimbine did not stimulate motor activity following 10 mg/kg and it retarded the turnover of dopamine following 30 mg/kg. These actions might be due to blockade of postsynapticα-receptors by yohimbine. The data indicate that yohimbine at low doses stimulates motor activity and dopamine turnover by selectively blockingα 2-autoreceptors leading to increased release of noradrenaline and subsequent activation of postsynapticα 1-receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01243754
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    A homologous series of N-alkylated cis-(+)-(1 S, 2 R)-5-methoxy-1-methyl-2-aminotetralins: Central dopamine receptor antagonists showing profiles ranging from classical antagonism to selectivity for autoreceptors (1986)
    Springer
    Journal of neural transmission 65 (1986), S. 29-38 
    Details
    ISSN: 1435-1463
    Keywords: 2-Aminotetralins ; dopamine ; antagonists ; autoreceptor ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary N-alkylated and N, N-dialkylated cis-(+)-(1 S, 2 R)-5-methoxy-1-methyl-2-aminotetralins were tested for central dopamine receptor antagonism usingin vivo biochemical and behavioral models in rats. The di-methyl analogue showed a profile similar to classical dopamine receptor antagonists. It produced a marked hypomotility including catalepsy and a pronounced increase in dopamine synthesis rate. This compound also displaced DiPr-5, 6-ADTN from striatal binding sites and antagonized the hyperactivity induced by the ligand. In contrast, the mono-propyl analogue increased locomotor activity and dopamine synthesis rate over a wide dose range. This compound failed to antagonize the hyperactivity induced by DiPr-5, 6-ADTN and to displace thisin-vivo binding ligand. Thus, the mono-propyl analogue appears to lack postsynaptic dopamine receptor antagonistic properties; it seems to produce its effects via a selective dopamine autoreceptor antagonism. The di-ethyl and di-propyl, but not the dibutyl, analogues were also active in the models used. Whereas the di-ethyl compound shows a profile similar to classical dopamine receptor blockers, the di-propyl compound appears to act preferentially on autoreceptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01249609
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Effects of dopamine D3 preferring compounds on conditioned place preference and intracranial self-stimulation in the rat (1995)
    Springer
    Journal of neural transmission 101 (1995), S. 27-39 
    Details
    ISSN: 1435-1463
    Keywords: D3 receptor ; conditioned place preference ; intracranial self-stimulation ; 7-OH-DPAT ; (+)-3PPP ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Compounds showing an in vitro binding preference for the dopamine D3 receptor were tested in two models designed to assess positive reinforcement in the rat: intracranial self-stimulation (ICSS) and conditioned place preference (CPP). R-(+)-7-OH-DPAT, a D3 preferring agonist, inhibited ICSS behaviour over a wide dose range. At higher doses, a facilitation of ICSS was seen. In the CPP model, 7-OH-DPAT was inactive except at the highest dose where a significant change in preference was seen. A dose of R-(+)-7-OH-DPAT, that significantly inhibited ICSS behaviour, was combined with a dose of d-amphetamine, that significantly facilitated ICSS behaviour. Surprisingly, this resulted in a significant synergistic facilitation of the amphetamine response. The putative D3 antagonist, U99194A was inactive in the ICSS model but induced significant place preference. The present results suggest that the dopamine D3 receptor, in contrast to the D2 receptor, has an inhibitory influence on reward mechanisms.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01271543
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    Paper (German National Licenses)
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  • 5
    Electronic Resource
    Electronic Resource
    Differential effects of dopamine D2 and D3 receptor antagonists in regard to dopamine release, in vivo receptor displacement and behaviour (1994)
    Springer
    Journal of neural transmission 98 (1994), S. 39-55 
    Details
    ISSN: 1435-1463
    Keywords: Dopamine ; D2 ; D3 ; receptors ; antagonists ; displacement ; release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary To establish possible functional differences between the dopamine D2 and D3 receptor we investigated the relation between the ability, for a set of nine mixed dopamine D2 and D3 receptor antagonists, to displace N, N-dipropyl-2-amino-5,6-dihydroxy tetralin (DP-5,6-ADTN) from striatal binding sites and the subsequent behavioural consequences in vivo. Dopamine D2 receptor preferring antagonists are powerful displacers of DP-5,6-ADTN from the striatum. Maximal displacement is followed by strong hypomotility. Displacement of the agonist by the D3 preferring antagonist U99194A is only partial and results in synergistic increases in locomotor activity. Superimposing haloperidol upon GBR12909 leads to a synergistic increase in striatal dialysate dopamine concentrations. This effect is absent when combining GBR12909 with the putative D3 antagonist U99194A. These data give support for the hypothesis that the dopamine D3 receptor is functionally relevant at the postsynaptic level. Here, in contrast to the D2 receptor, it is proposed to exert an inhibitory influence on psychomotor functions.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01277593
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    Paper (German National Licenses)
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