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Related Experiment Videos

Partial agonist activity of celiprolol

L H Tung1, G Jackman, B Campbell

  • 1Department of Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Australia.

Journal of Cardiovascular Pharmacology
|March 1, 1993
PubMed
Summary

Celiprolol exhibits partial agonist activity at beta-1 and beta-2 adrenoceptors, influencing heart rate and blood pressure. Its antagonist properties show significant beta-1 selectivity, similar to atenolol, but potentiate histamine-induced bronchoconstriction.

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Area of Science:

  • Pharmacology
  • Cardiovascular Physiology
  • Adrenoceptor Research

Background:

  • Celiprolol is a beta-blocker with a unique pharmacological profile.
  • Understanding its adrenoceptor interactions is crucial for clinical application.

Purpose of the Study:

  • To investigate the adrenoceptor agonist and antagonist properties of celiprolol in vivo.
  • To determine the beta-1 vs. beta-2 selectivity of celiprolol as both an agonist and antagonist.

Main Methods:

  • Intravenous administration of celiprolol to pithed rats.
  • Utilized selective beta-1 (CGP 20712A) and beta-2 (ICI 118551) adrenoceptor antagonists.
  • Assessed effects on heart rate (HR) and blood pressure (BP).
  • Compared antagonist selectivity with isolated guinea pig atria and trachea preparations.

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Main Results:

  • Celiprolol demonstrated a dose-dependent increase in HR (partial agonist effect), blocked by a beta-1 antagonist.
  • A vasodepressor effect was observed, abolished by a beta-2 antagonist.
  • Celiprolol exhibited significant beta-1 selectivity as an antagonist (340:1 in rats).
  • Potentiated histamine-induced bronchoconstriction, similar to atenolol.

Conclusions:

  • Celiprolol acts as a partial agonist at both beta-1 and beta-2 adrenoceptors.
  • It possesses significant beta-1 selectivity as an antagonist.
  • Its effects on bronchoconstriction warrant consideration in clinical use.