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  • 1
    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
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  • 2
    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
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