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  • locomotor activity  (3)
  • (+)-UH 232 and (+)-AJ 76  (1)
  • 1
    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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  • 2
    ISSN: 1432-1106
    Keywords: Dopamine ; Autoreceptor antagonists ; (+)-UH 232 and (+)-AJ 76 ; Nigro-striatal system ; 6-OH-DA lesion ; Rotational behaviour ; In vivo DP-5,6-ADTN binding ; Receptor sensitivity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The in vivo dopamine (DA) receptor binding and behavioural properties of the recently characterised putative preferential DA autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 were studied in rats with a unilateral 6-OH-DA lesion of the substantia nigra. The main findings were a) that (+)-UH 232 and (+)-AJ 76 per se failed to produce significant turning behaviour, b) that both agents antagonised contralateral rotation caused by the DA agonist apomorphine, including a change of the characteristic two-peak apomorphine rotation pattern into a single peak, indicating that the DA antagonist properties of (+)-UH 232 and (+)-AJ 76 are retained also at denervation-sensitised postsynaptic DA receptors and — in support of this notion — c) that (+)-UH 232 and (+)-AJ 76 were able to displace the specific in vivo binding of the DA receptor agonist DP-5,6-ADTN in the denervated as well as in the intact striata of the 6-OH-DA-lesioned animals. Interestingly, in this regard (+)-UH 232 was significantly less efficient on the lesioned as compared to the intact side. The DP-5,6-ADTN-displacing effect of (+)-AJ 76 did not, however, differ between the intact and the denervated striatum. The implications of the present findings are discussed with particular reference to DA receptor sensitivity and adaptational phenomena.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 102 (1995), S. 209-220 
    ISSN: 1435-1463
    Keywords: Microinjections ; dopamine D3 receptors ; Leao's spreading depression ; locomotor activity ; rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Compounds showing an in vitro binding preference for the dopamine D3 vs. D2 receptors were tested for effects on locomotor activity after local application in the nucleus accumbens (N Acc) and the ventral tegmental area (VTA) of the rat brain. R-(+)-7-OH-DPAT, a dopamine D3 preferring agonist, inhibited spontaneous locomotor activity over a wide dose range after injection into the N Acc. A decrease in activity over a wide dose range was also seen after local application into the VTA of both R-(+)-7-OH-DPAT and the dopamine D2 preferring agonist (+)-3-PPP. Furthermore, (+)-3-PPP produced a dose dependent increase in activity after local application into the N Acc. The putative D3 antagonist, U99194A, with a 30 fold preference for the dopamine D3 vs. D2 receptor, produced an increase in activity when injected into the N Acc. A similar pattern were seen after infusion into the lateral ventricle. Local application into the VTA did, however, not produce any significant effects. The present results support the hypothesis that dopamine D3 receptors (in contrast to the D2 receptors) are mainly postsynaptically located where they display an inhibitory action on locomotor activity.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 95 (1994), S. 71-74 
    ISSN: 1435-1463
    Keywords: D3 receptor ; locomotor activity ; dopamine release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The dopamine D3 preferring ligand R-(+)-7-OH-DPAT induced strong hypolocomotion in rats. Doses producing reduction of locomotion failed to affect dopamine release or synthesis rate. These data support the hypothesis that the dopamine D3 receptor is a postsynaptic receptor with an inhibitory influence on rat locomotor activity.
    Type of Medium: Electronic Resource
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