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Burimamide

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Manfred Göthert – 1st expert on this subject based on the ideXlab platform

  • Involvement of presynaptic H_3 receptors in the inhibitory effect of histamine on serotonin release in the rat brain cortex
    Naunyn-Schmiedeberg's Archives of Pharmacology, 1990
    Co-Authors: Klaus Fink, Eberhard Schlicker, A. Neise, Manfred Göthert

    Abstract:

    Rat brain cortex slices or synaptosomes preincubated with ^3H-serotonin were superfused with physiological salt solution (which, in the case of slices, contained citalopram, an inhibitor of serotonin uptake), and the effects of histamine and related drugs on the evoked tritium overflow were studied. The electrically (3 Hz) evoked tritium overflow from slices was inhibited by histamine and the H_3 receptor agonists R-(−)-α-methylhistamine and Nα-methylhistamine (pIC_12.5 values: 6.41, 7.28 and 6.12, respectively), but not affected by the H_1 receptor agonist 2-(2-thiazolyl)ethylamine and the H_2 receptor agonist dimaprit (each at 10 μmol/l). The concentration-response curve for histamine was shifted to the right by the H_3 receptor antagonists impromidine, Burimamide and thioperamide (apparent pA_2 values: 7.45, 5.97 and 7.88, respectively); the concentration-response curve of serotonin for its inhibitory effect on the electrically evoked overflow was not affected by the three drugs (apparent pA_2 values: < 5.5, < 5.5 and < 6.5). Given alone, impromidine, thioperamide and a low concentration of Burimamide facilitated the electrically evoked overflow. In slices superfused with K^+-rich, Ca^2+-free solution containing tetrodotoxin throughout and in synaptosomes superfused with Ca^2+-free solution, histamine inhibited the overflow evoked by introduction of Ca^2+ (in synaptosomes, simultaneously with an increased amount of K^+). In either tissue, the effect of histamine was counteracted by thioperamide. The results provide evidence that exogenous and probably also endogenous histamine inhibits serotonin release in the rat brain cortex via presynaptic histamine H_3 receptors.

Klaus Fink – 2nd expert on this subject based on the ideXlab platform

  • Involvement of presynaptic H_3 receptors in the inhibitory effect of histamine on serotonin release in the rat brain cortex
    Naunyn-Schmiedeberg's Archives of Pharmacology, 1990
    Co-Authors: Klaus Fink, Eberhard Schlicker, A. Neise, Manfred Göthert

    Abstract:

    Rat brain cortex slices or synaptosomes preincubated with ^3H-serotonin were superfused with physiological salt solution (which, in the case of slices, contained citalopram, an inhibitor of serotonin uptake), and the effects of histamine and related drugs on the evoked tritium overflow were studied. The electrically (3 Hz) evoked tritium overflow from slices was inhibited by histamine and the H_3 receptor agonists R-(−)-α-methylhistamine and Nα-methylhistamine (pIC_12.5 values: 6.41, 7.28 and 6.12, respectively), but not affected by the H_1 receptor agonist 2-(2-thiazolyl)ethylamine and the H_2 receptor agonist dimaprit (each at 10 μmol/l). The concentration-response curve for histamine was shifted to the right by the H_3 receptor antagonists impromidine, Burimamide and thioperamide (apparent pA_2 values: 7.45, 5.97 and 7.88, respectively); the concentration-response curve of serotonin for its inhibitory effect on the electrically evoked overflow was not affected by the three drugs (apparent pA_2 values: < 5.5, < 5.5 and < 6.5). Given alone, impromidine, thioperamide and a low concentration of Burimamide facilitated the electrically evoked overflow. In slices superfused with K^+-rich, Ca^2+-free solution containing tetrodotoxin throughout and in synaptosomes superfused with Ca^2+-free solution, histamine inhibited the overflow evoked by introduction of Ca^2+ (in synaptosomes, simultaneously with an increased amount of K^+). In either tissue, the effect of histamine was counteracted by thioperamide. The results provide evidence that exogenous and probably also endogenous histamine inhibits serotonin release in the rat brain cortex via presynaptic histamine H_3 receptors.

A. Neise – 3rd expert on this subject based on the ideXlab platform

  • Involvement of presynaptic H_3 receptors in the inhibitory effect of histamine on serotonin release in the rat brain cortex
    Naunyn-Schmiedeberg's Archives of Pharmacology, 1990
    Co-Authors: Klaus Fink, Eberhard Schlicker, A. Neise, Manfred Göthert

    Abstract:

    Rat brain cortex slices or synaptosomes preincubated with ^3H-serotonin were superfused with physiological salt solution (which, in the case of slices, contained citalopram, an inhibitor of serotonin uptake), and the effects of histamine and related drugs on the evoked tritium overflow were studied. The electrically (3 Hz) evoked tritium overflow from slices was inhibited by histamine and the H_3 receptor agonists R-(−)-α-methylhistamine and Nα-methylhistamine (pIC_12.5 values: 6.41, 7.28 and 6.12, respectively), but not affected by the H_1 receptor agonist 2-(2-thiazolyl)ethylamine and the H_2 receptor agonist dimaprit (each at 10 μmol/l). The concentration-response curve for histamine was shifted to the right by the H_3 receptor antagonists impromidine, Burimamide and thioperamide (apparent pA_2 values: 7.45, 5.97 and 7.88, respectively); the concentration-response curve of serotonin for its inhibitory effect on the electrically evoked overflow was not affected by the three drugs (apparent pA_2 values: < 5.5, < 5.5 and < 6.5). Given alone, impromidine, thioperamide and a low concentration of Burimamide facilitated the electrically evoked overflow. In slices superfused with K^+-rich, Ca^2+-free solution containing tetrodotoxin throughout and in synaptosomes superfused with Ca^2+-free solution, histamine inhibited the overflow evoked by introduction of Ca^2+ (in synaptosomes, simultaneously with an increased amount of K^+). In either tissue, the effect of histamine was counteracted by thioperamide. The results provide evidence that exogenous and probably also endogenous histamine inhibits serotonin release in the rat brain cortex via presynaptic histamine H_3 receptors.