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Title: Partial agonist activity of celiprolol.
Austin Authors: Tung, L H;Jackman, G;Campbell, B;Louis, Simon N S;Iakovidis, D;Louis, William J 
Affiliation: Department of Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Australia
Issue Date: 1-Mar-1993
Publication information: Journal of Cardiovascular Pharmacology; 21(3): 484-8
Abstract: Celiprolol given intravenously (i.v.) to pithed rats in the dose range of 0.1-10,000 micrograms/g produced a dose-dependent increase in heart rate (HR) which was greatest (123 beats/min) at 1,000-3,000 micrograms/kg. This partial agonist effect was blocked by the selective beta 1-adrenoceptor antagonist CGP 20712A. Celiprolol also produced a vasodepressor effect in this dose range which was abolished by the relatively selective beta 2-adrenoceptor antagonist ICI 118551 but not CGP 20712A. The magnitude of this intrinsic sympathomimetic activity (ISA) response was not significantly altered by reserpine pretreatment. Celiprolol also antagonised the effects of isoprenaline 0.05 microgram/kg on HR and blood pressure (BP). The beta 1 selectivity of celiprolol as an antagonist in pithed rats (beta 1/beta 2 = 340:1) was similar to that observed in studies with isolated guinea pig atria and trachea (beta 1/beta 2 = 63:1), both being considerably greater than that observed with atenolol. Celiprolol, however, like atenolol, potentiated the bronchoconstrictor responses to histamine (3 micrograms/kg). Metabolic studies of rats and human urine failed to show significant amounts of potentially vasoactive metabolites. These data are consistent with celiprolol acting as both a beta 1- and beta 2- adrenoceptor partial agonist.
Gov't Doc #: 7681512
Type: Journal Article
Subjects: Adrenergic beta-Antagonists.pharmacology
Airway Resistance.drug effects
Blood Pressure.drug effects
Decerebrate State
Guinea Pigs
Heart Rate.drug effects
In Vitro Techniques
Rats, Sprague-Dawley
Receptors, Adrenergic, beta.drug effects
Appears in Collections:Journal articles

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