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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 276 (1973), S. 71-88 
    ISSN: 1432-1912
    Keywords: Noradrenaline Metabolites ; Guinea-Pig Atria ; Nictitating Membrane ; Normetanephrine ; Metanephrine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The effects of the five noradrenaline (NA) metabolites and of the O-methylated metabolite of adrenaline, metanephrine, were studied in a tissue with adrenergic beta-receptors (guinea-pig atria) and in a tissue with predominance of alpha-receptors (cat's nictitating membrane). In atria, normetanephrine and metanephrine elicited positive chronotrophic effects which were mediated through the beta-receptors. Both O-methylated metabolites had only 1/1000th of the potency of NA. In the normally innervated nictitating membrane normetanephrine and metanephrine elicited maximal responses of the same magnitude as NA. While normetanephrine had one half of the potency of NA, metanephrine was even more potent than NA. The effects of normetanephrine or metanephrine were mediated through the activation of the alpha-receptors and were not potentiated by either cocaine or denervation. Neither the deaminated nor the deaminated-O-methylated metabolites of NA had activity as agonists on alpha-or beta-receptors in concen-of up to 1×10−4M. These metabolites did not elicit alpha-or beta-receptor block in concentrations of up to 1×10−4M.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 287 (1975), S. 243-259 
    ISSN: 1432-1912
    Keywords: Scorpion Toxin ; Noradrenaline ; Noradrenaline Metabolites ; Guinea-Pig Atria ; Nerve Stimulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The effects of a purified fraction of the venom of the Brazilian scorpion, Tityus serrulatus, were studied in isolated guinea-pig atria previously labelled with 3H-noradrenaline. Exposure to 0.3 and 1.0 μ/ml of the scorpion toxin resulted in a long lasting positive chronotropic effect which was concentration-dependent. The increase in atrial rate coincided with an enhancement in spontaneous outflow of radioactivity. The increase in outflow of radioactive products elicited by exposure to 1.0 μg/ml of the scorpion toxin was approximately 3-fold. 3H-noradrenaline accounted for 60% of the total increase in outflow of radioactivity elicited by the scorpion toxin and the 3H-deaminated glycol (3,4-dihydroxyphenylglycol) represented the main metabolite formed, accounting for approximately 35% of the total release. 20 min after exposure to 1.0 μg/ml of the scorpion toxin the overflow of the labelled transmitter elicited by accelerans nerve stimulation (4 Hz, during 60 sec, supramaximal voltage) was increased 8-fold. This effect of the scorpion toxin appears to be unrelated to inhibition of neuronal uptake, block of α-adrenoceptors or stimulation of β-adrenoceptors. Consequently, in addition to releasing noradrenaline, the scorpion toxin enhances transmitter overflow elicited by nerve stimulation through a prejunctional effect which appears to reflect a nove mechanism of action.
    Type of Medium: Electronic Resource
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