descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 1976 English Publisher:Elsevier BVJournal:Biochemical Pharmacology, volume 25, pages 131-134 (issn: 0006-2952,

Authors: P. Polster; J. Broekhuysen;

doi: 10.1016/0006-2952(76)90279-3

pmid: 1259774

The adrenergic antagonism of amiodarone

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Abstract

Abstract Inhibition by amiodarone and propranolol of the chronotropic effect of isoproterenol on spontaneously beating rabbit right atria has been studied in vitro. Propranolol behaved like a typical competitive β1-adrenoceptor antagonist with a pA2 value of 8.33. Amiodarone acted as a non-competitive inhibitor with a pD'2 value of about 4.17. Inhibition by amiodarone and phentolamine of the norepinephrine-induced contractions of isolated rat aortic strips has been studied likewise. Phentolamine was shown to inhibit the adrenergic α receptor competitively with a pA2 value of 8.69. Amiodarone, though devoid of any appreciable effect on calcium permeability, acted again as a non-competitive inhibitor, with a pD'2 value of about 4.06. The mechanism of action of amiodarone is discussed.

Keywords

Male, Dose-Response Relationship, Drug, Isoproterenol, Amiodarone, Aorta, Thoracic, Atrial Function, Propranolol, Stimulation, Chemical, Receptors, Adrenergic, Norepinephrine, Heart Rate, Animals, Female, Heart Atria, Rabbits, Benzofurans

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