Increased Cardiac Alpha-1-Adrenoceptor Density In Rats Following Treatment With Amiodarone

Claudia Evelina Budu, Nisim Balas, Asher Shainberg, Hermann Nawrath, Jorg W. Wegener

Research output: Contribution to journalArticlepeer-review

2 Scopus citations


This study was undertaken to investigate the interaction between amiodarone and alpha-1-adrenoceptors in rat cardiac cells. The level (Bmax) and affinity (Kd) of alpha-1-adrenoceptors in heart cells were determined by [3H]prazosin radioligand binding following amiodarone treatment. In cultured intact cardiocytes treated for 48 h with 10 μM amiodarone, [3H]prazosin binding increased by 31% compared with the control cells (p<0.05). The increase was both dose and time dependent and was found to be specific because no significant change occurred in creatine kinase activity. Additionally, under the same conditions, an increase in [3H]prazosin binding to cultured cardiocyte cell membranes was also obtained. Oral gavage of amiodarone to rats for 8 d resulted in a 25% increase in [3H]prazosin binding to isolated ventricle membranes compared with control rats (p<0.05). We conclude that amiodarone treatment can increase the response to alpha-1-adrenoceptors agonist in the heart due to an increase in the density of alpha-1-adrenoceptors.

Original languageEnglish
Pages (from-to)33-48
Number of pages16
JournalJournal of Basic and Clinical Physiology and Pharmacology
Issue number1
StatePublished - 2001


  • [H]prazosin binding
  • alpha-1-adrenoceptors
  • amiodarone
  • heart


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