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Effects of chronic pindolol treatment on human myocardial ß1- and ß2-adrenoceptor function

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Summary

To evaluate the effects of chronic pindolol treatment on human myocardial ß-adrenoceptor, membrane preparations from right atrial auricles from patients on chronic pindolol treatment and from patients not treated with ß-blocker were compared with respect to specific binding of [125I]-iodocyanopindolol ([125I]-ICYP) and adenylate cyclase (AC) activity. Pindolol treatment was associated with a 25% increase in total ß-adrenoceptor density (72.3 vs. 58.3 fmol/mg protein). This increase was due a 40% increase of the ß1-adrenoceptor subtype (62.2 vs. 44.3 fmol/mg protein), while ß2-adrenoceptor density was decreased by about 25% (10.0 vs. 14.0 fmol/mg). Isoprenaline 5 μmol/l (9.7 vs. 14.2 pmol/min/mg) and terbutaline 50 gmol/l (4.9 vs. 8.3 pmol/min/mg protein) stimulated adenylate cyclase activity was reduced, whereas fluoride (10 mmol/l) stimulated cAMP production to the same extent in both groups (9.4 vs. 9.4 pmol/min/mg protein). Thus, chronic treatment with pindolol was associated with upregulation of the ß1-adrenoceptors and a down-regulation of the ß2-adrenoceptors. The total level of ß-adrenoceptors was slightly increased. In spite of this, adenylate cyclase activity and response was reduced.

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Authors and Affiliations

  1. Medical Department B and Institute of Pathology, Rikshospitalet University Hospital, N-0027, Oslo 1, Norway

    Reidar Bjornerheim & Svein Golf

  2. Institute of Medical Biochemistry, University of Oslo, Oslo, Norway

    Vidar Hansson

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  1. Reidar Bjornerheim
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  2. Svein Golf
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  3. Vidar Hansson
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Bjornerheim, R., Golf, S. & Hansson, V. Effects of chronic pindolol treatment on human myocardial ß1- and ß2-adrenoceptor function. Naunyn-Schmiedeberg's Arch Pharmacol 342, 429–435 (1990). https://doi.org/10.1007/BF00169460

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  • DOI: https://doi.org/10.1007/BF00169460

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