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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 275 (1972), S. 95-104 
    ISSN: 1432-1912
    Keywords: Temperature ; β-Receptors ; Guinea-Pig Atrium ; Affinity ; Adrenergic Drugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Using electrically stimulated guinea-pig atria the influence of temperature on the contractility and on the efficacy of some β-sympathomimetic and-lytic drugs, was studied. The following results were obtained. 1. Raising the temperature of the bath fluid from 25–42°C decreased significantly the developed amplitude of contraction under control conditions, whereas dT/dt max values were not altered. The maximal developed tension induced by the sympathomimetic drugs decreased at 42°C. The corresponding dT/dt max values, on the other hand, were increased by elevation of the temperature. 2. The dose-response curves of the sympathomimetic drugs isoprenaline (IPN), Th 1165a and orciprenaline (OPN) were shifted to the right when the temperature was increased from 25–42°C. The affinity of IPN at 33°C was found about 30- and 100-times higher than that of Th 1165a and OPN, respectively. 3. The β-adrenolytic drug pindolol (LB 46), as well as the cardioselective β-blocker, practolol, antagonized the β-sympathomimetic effects evoked by IPN and Th 1165a in a competitive manner. As indicated by the pA2 values, pindolol had a 100-times higher affinity than practolol. The present results lead to the conclusion that, on the guinea-pig atrium, the agonist β-receptor reaction depends on the metabolic rate of this organ.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 275 (1972), S. 105-113 
    ISSN: 1432-1912
    Keywords: Sympathomimetic Affinity ; β-Receptors ; Temperature ; Metabolic State ; Isolated Organs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Experiments on isolated organs-rabbit ileum, guinea-pig trachea and atrium — with different “β-receptor subtypes” were carried out in order to determine whether changes of the metabolic state or of the extracellular pH were able to alter the responsiveness of these receptors to sympathomimetic amines. 1. Guinea-Pig Atrium. Lowering of the pH of the bath fluid from 7.48 to 6.79 resulted in a significant decrease of the affinity of isoprenaline (IPN) calculated as the pD2-value. Metabolic inhibition induced by iodoacetic acid (IAA) (5×10−5 M) increased the affinity of Th 1165a. 2. Rabbit Ileum. The affinity of IPN was not changed by lowering the pH, even to values of 6.11. At this pH the spontaneous motility was already markedly impaired. IAA (2.4×10−5 M) caused a moderate increase in the affinity of IPN whereas those of Th 1165a and orciprenaline (OPN) were elevated 10-fold. 3. Guinea-Pig Trachea. Lowering of the pH caused a decrease of the pD2-values of IPN and in particular of Th 1165a. The metabolic inhibitor IAA had no influence upon the pD2 value of IPN. 4. The present results favour the existence of only one type of β-receptor which changes its sensitivity depending on the metabolic state. It seems therefore very likely that the affinity of sympathomimetic drugs depends not only on the structure of the β-receptor but also on the metabolic state of the tissue.
    Type of Medium: Electronic Resource
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