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  • 1
    ISSN: 1432-1912
    Keywords: Isamoltane ; 5-HT1B Receptors ; 5-HT Autoreceptors ; 5-HT Turnover ; 5-HT Syndrome
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The biochemical and behavioural effects of isamoltane, a \-adrenoceptor and 5-HT1B receptor antagonist that has higher affinity for 5-HT1B receptors than for 5-HTIA receptors, on 5-HT neurotransmission in the rat brain were examined. In binding experiments isamoltane was found to be about five times more potent as a ligand for the 5-HT1B receptor than for the 5-HT1A receptor (Ki values 21 and 112 nmol/l, respectively). Isamoltane increased the K+-evoked overflow of 3H from 3H-5-HT loaded slices of rat occipital cortex at 0.1 μmol/l, consistent with inhibition of the terminal 5HT autoreceptor. In vivo, isamoltane significantly increased the concentration of 5-hydroxyindoleacetic acid in hypothalamus and hippocampus indicating an increased 5-HT turnover with a maximal effect at 3 mg/kg s.c. A higher dose produced a less pronounced effect. This effect did not seem to be due to the β-adrenoceptor blocking action of isamoltane since the β-adrenoceptor antagonists, (−)-alprenolol, betaxolol or ICI 118,551 had no significant effects on 5-HT turnover at 5 mg/kg s.c. Isamoltane at 3 mg/kg s.c. induced the wet-dog shake response which was blocked by the tryptophan hydroxylase inhibitor p-chlorophenylalanine. In contrast, the same response induced by the 5-HT2 receptor agonist quipazine was not blocked by pretreatment with p-chlorophenylalanine. The wet-dog shakes evoked by isamoltane and quipazine were blocked by ritanserin, which indicates that 5-HT2 receptors are involved in their expression. These observations indicate that isamoltane, by inhibiting the terminal 5-HT autoreceptors, increased the synaptic concentration of 5-HT to a level that induced a behavioural response.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    International journal of legal medicine 83 (1979), S. 105-113 
    ISSN: 1437-1596
    Keywords: Tear gas, detection ; Chemical mace ; Chloracetophenone ; 1,1,2-Trichloro-1,2,2-trifluroethane ; 1,1,1-Trichloroethane ; Tränengas, Nachweis ; chemische Keule ; Chloracetophenon ; 1,1,2-Trichlor-1,2,2-trifluoräthan ; 1,1,1-Trichloräthan
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine , Law
    Description / Table of Contents: Zusammenfassung Zur Klärung der Frage, ob ein negativer Befund der gaschromatographischen Blutuntersuchung auf Bestandteile der „chemischen Keule“ beweist, daß keine oder allenfalls nur leichte Tränengasexposition vorgelegen hat, wurden Tierversuche durchgeführt. Im Blut von 10 Meerschweinchen, die den Komponenten der chemischen Keule 1–6 Std ausgesetzt worden waren, konnten die Trägergase 1,1,2-Trichlor-1,2,2-trifluoräthan (Frigen 113) und 1,1,1-Trichloräthan — auch noch 23 Std nach Expositionsende sowie nach 18wöchiger Lagerung der Blutproben — deutlich, der Wirkstoff Chloracetophenon (CN) dagegen überhaupt nicht nachgewiesen werden. In vitro-Versuche zeigten, daß das sehr reaktionsfähige CN relativ rasch mit Blutbestandteilen reagiert. Blutuntersuchungen auf CN müssen daher möglichst sofort nach der Entnahme durchgeführt werden. Bei Einatmung von Bestandteilen der chemischen Keule, d. h. bei der vergleichsweise leichtesten Einwirkungsart des Chloracetophenon, dürfte der Wirkstoff infolge schneller Reaktion mit Proteinen der respiratorischen Oberfläche der Lungen gar nicht erst in das Blut gelangen.
    Notes: Summary To answer the question whether a negative result of gas chromatographic blood analysis for components of chemical mace proves that no or at most only slight tear gas exposure can have occurred, animal experiments were carried out. In the blood of 10 guinea pigs, which were exposed to the contents of chemical mace for 1–6h, the solvants 1,1,2-trichloro-1,2,2-trifluorethane (freon 113) and 1,1,1-trichloroethane could easily be detected—even 23 h after the end of exposure or after a storage of the blood samples for 18 weeks—whereas the lacrimator chloracetophenone (CN) could not be found at al. In vitro experiments showed that CN relatively quickly reacts with components of blood. Therefore, blood samples should be analyzed for CN after withdrawal as soon as possible. In case of inhalation of the contents of chemical mace, i.e., after the comparatively mildest form of CN application, most probably no traces of the lacrimator at all can pass into the blood due to the quick reaction of CN with proteins of the respiratory surface of the lung.
    Type of Medium: Electronic Resource
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