The adrenergic antagonism of amiodarone

The adrenergic antagonism of amiodarone

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 β 1-adrenoceptor antagonist with a p A 2 value of 8.33. Amiodarone acted as a non-competitive inh...

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Veröffentlicht in:Biochemical pharmacology 1976-01, Vol.25 (2), p.131-134
Hauptverfasser: Polster, P., Broekhuysen, J.
Format: Artikel
Sprache:eng
Schlagworte:
Amiodarone - pharmacology
Animals
Aorta, Thoracic - drug effects
Aorta, Thoracic - physiology
Atrial Function
Benzofurans - pharmacology
Dose-Response Relationship, Drug
Female
Heart Atria - drug effects
Heart Rate - drug effects
Isoproterenol - pharmacology
Male
Norepinephrine - pharmacology
Propranolol - pharmacology
Rabbits
Receptors, Adrenergic
Stimulation, Chemical
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Zusammenfassung: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 β 1-adrenoceptor antagonist with a p A 2 value of 8.33. Amiodarone acted as a non-competitive inhibitor with a p D' 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 p A 2 value of 8.69. Amiodarone, though devoid of any appreciable effect on calcium permeability, acted again as a non-competitive inhibitor, with a p D' 2 value of about 4.06. The mechanism of action of amiodarone is discussed.
ISSN:0006-2952
1873-2968
DOI:10.1016/0006-2952(76)90279-3