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  • 1
    Digitale Medien
    Digitale Medien
    Risperidone (R 64 766), a potent and complete LSD antagonist in drug discrimination by rats (1989)
    Springer
    Psychopharmacology 97 (1989), S. 206-212 
    Details
    ISSN: 1432-2072
    Schlagwort(e): LSD-cue ; Drug discrimination ; Risperidone ; Schizophrenia ; 5-HT2-catecholamine antagonism ; LSD antagonism ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Risperidone was studied in a 0.16 mg/kg LSD-saline drug discrimination test procedure. At doses varying from 0.0025 to 0.63 mg/kg, no LSD-like agonist effects were observed. Studies on the antagonism of the LSD-cue indicated that risperidone was able to completely block the discriminative stimulus properties of LSD with a minimum ED50-value of 0.028 mg/kg. Risperidone was also very active over time with reference to LSD antagonism, the ED50s after 2, 4 and 8 h pretreatment being 0.028, 0.064 and 0.44 mg/kg. Response rate reductions were only observed at doses ≧0.16 mg/kg after 1 h and at 0.63 mg/kg after 2 h pretreatment. Four and 8 h after treatment, no rate-reducing effects were apparent at doses up to 2.50 mg/kg. Thus at pretreatment intervals ranging between 2 and 8 h, complete antagonism of LSD without any rate effects was obtained. As compared to other LSD antagonists, risperidone was quantitatively better than setoperone and ritanserin and longer acting than pirenperone. Based on the pharmacological profile of risperidone and the other LSD antagonists, it was concluded that a potent central 5-HT2 and catecholamine antagonism is needed for a potent and complete antagonism of the 0.16 mg/kg LSD-cue. The potential clinical effect of risperidone in the positive and negative symptoms of schizophrenia is discussed.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00442251
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Behavioral and 5-HT antagonist effects of ritanserin: A pure and selective antagonist of LSD discrimination in rat (1985)
    Springer
    Psychopharmacology 86 (1985), S. 45-54 
    Details
    ISSN: 1432-2072
    Schlagwort(e): 5-HT antagonist ; LSD antagonist ; Drug discrimination ; Anxiety ; 5-HTP ; Head twitch ; Conflict behavior ; Hypothermia ; Ritanserin ; Pirenperone ; Chlordiazepoxide ; Diazepam ; Rat
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The newly synthesized compound and putative 5-HT2 antagonist ritanserin, but not the structurally related compound R 56413, resembles pirenperone in that it acts as a pure antagonist in an LSD-saline drug discrimination assay in the rat. Ritanserin exceeded pirenperone in terms of behavioral specificity; the lowest effective dose of ritanserin in antagonizing LSD was one order of magnitude higher than that of pirenperone, but the compound depressed rate of operant responding only at doses that were about 1000-fold higher than those at which pirenperone was effective. Ritanserin exerted effects in an open field test which were reminiscent of anxiolytic drug activity in the rat; its effects were greater than those of pirenperone, R 56413 and the benzodiazepines chlordiazepoxide and diazepam. The results of experiments on antagonism of 5-HT-induced hypothermia and of the 5-HTP-induced headtwitch response fail to support the possibility that the putative anxiolytic effects of ritanserin in the rat can be ascribed simply to a pharmacologically defined action at 5-HT receptors.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00431683
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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