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β-Adrenergic receptor coupled-adenylate cyclase of human fat cell ghosts

Das an adrenerge β-Rezeptoren gekoppelte Adenylat Cyclase System in menschlichen Fettzellen

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Zusammenfassung

Die Wirkungen beta-adrenerger Substanzen wie Isoproterenol, Adrenalin und Noradrenalin wurden entweder allein oder zusammen mit Propranolol, einem Beta-Blocker, auf das Adenylat-Cyclase System aus menschlichem Unterhautfettgewebe untersucht. Einen Katecholamin-Sensitivität des menschlichen Enzymsystems ließ sich ohne Zusatz von künstlichen Kofaktoren nachweisen. Maximal-Konzentrationen von Isoproterenol, Adrenalin und Nor-Adrenalin führten zu einer 2–6,5fachen Zunahme der Enzym-Aktivität. Isoproterenol stimulierte deutlich stärker als die beiden Hormome. Propranolol führte zu einer kompetitiven Hemmung des stimulierenden Effektes der beta-adrenergen Agonisten. Es wird gefolgert, daß die in-vitro Messung der Adenylat-Cyclase Aktivität im menschlichem Fettgewebe eine einfache Möglichkeit zur Testung von Substanzen mit adrenerger Wirkung darstellt.

Summary

The effects of beta-adrenergic agonists such as isoproterenol, norepinephrine and epinephrine upon the adenylate cyclase activity of human fat cell ghosts were tested, each alone and in combination with the beta-blocking agent propranolol. Saturating concentrations of these agents showed a 2–6.5-fold increase of enzyme activity without addition of any artificial cofactors. Isoproterenol was more potent in stimulating the enzyme system than epinephrine and nor-epinephrine. Propranolol caused a dose-dependent rightward shift of the log-dose response curve of these beta-adrenergic agonists. The assay of human fat cell adenylate cyclase in vitro may provide a simple and convenient assay system for the screening of beta-adrenergic drugs of potential therapeutic importance.

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Herrn Prof. Dr. Dr. h.c. G. Schettler zum 60. Geburtstag gewidmet

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Kather, H., Vogt, B. & Simon, B. β-Adrenergic receptor coupled-adenylate cyclase of human fat cell ghosts. Klin Wochenschr 55, 625–628 (1977). https://doi.org/10.1007/BF01482531

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  • DOI: https://doi.org/10.1007/BF01482531

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