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Related Experiment Videos

Certain beta-blockers can decrease beta-adrenergic receptor number: I. Acute reduction in receptor number by

A De Blasi1, M Fratelli, O Marasco

  • 1Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.

Circulation Research
|August 1, 1988
PubMed
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Certain beta-blockers, like tertatolol, rapidly decrease beta-adrenergic receptors by modifying them, not through sequestration or irreversible binding. This mechanism differs from other beta-blockers and agonists.

Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • Previous studies showed tertatolol reduces human mononuclear leukocyte beta-receptors in vivo.
  • The in vitro mechanism of beta-adrenergic receptor regulation by beta-antagonists requires further investigation.

Purpose of the Study:

  • To investigate the mechanism by which beta-antagonists, specifically tertatolol and bopindolol, reduce beta-adrenergic receptors in target cells in vitro.
  • To compare the effects of tertatolol and bopindolol with other beta-blockers (propranolol, pindolol) and agonists (isoproterenol).

Main Methods:

  • Used human mononuclear leukocytes and S49 murine lymphoma cells.
  • Measured beta-adrenergic receptors using hydrophilic (3H-CGP 12177) and lipophilic (125I-pindolol) ligands.
  • Assessed isoproterenol-stimulated cyclic AMP accumulation.

Related Experiment Videos

  • Compared effects with irreversible blocker bromo-acetyl-alprenolol-methane (BAAM).

    • Main Results:

    • Tertatolol and bopindolol, but not propranolol or pindolol, rapidly reduced beta-adrenergic receptors in 1 hour.
    • This reduction was observed for both surface and total receptors, excluding sequestration.
    • The effect was independent of partial agonist activity and not due to irreversible binding, as the reduction was slowly reversible.

    Conclusions:

    • Tertatolol and bopindolol exhibit a unique dual action on beta-adrenergic receptors: competitive binding followed by modification.
    • This modification renders receptors unavailable for ligand or catecholamine binding.
    • This mechanism explains the rapid reduction in beta-receptor number observed in vitro and potentially in vivo.