Abstract:
:beta-Antiadrenergic properties are part of the pharmacological characteristics of amiodarone. In the present study, the action of amiodarone on rat-heart beta-adrenoceptors was investigated. [125I]Cyanopindolol (CYP) was used to label beta-adrenoceptors in crude rat-heart microsomes. In competition binding experiments, amiodarone up to 10(-6) M did not displace [125I]CYP from cardiac beta-adrenergic receptors. The effects of amiodarone on the number and affinity for [125I]CYP of beta-adrenoceptors were evaluated in saturation experiments. In vitro exposure of cardiac microsomes to 10(-5) M amiodarone did not modify these parameters. At higher concentrations the beta-receptor number decreased while the affinity for [125I]CYP was not affected. In vivo experiments showed a significant decrease in beta-adrenoceptor density after a single oral dose of 50 mg/kg amiodarone. In chronically treated animals, the same decrease in beta-receptor number was observed 24 hr after the last administration of the drug. 5'-Nucleotidase activity, another specific marker of the plasma membrane, was unaffected by the treatment. These results suggest that part of the beta-adrenergic antagonism of amiodarone is due to a decrease in the beta-adrenoceptor density at the surface of the myocardial cell.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Nokin P,Clinet M,Schoenfeld Pdoi
10.1016/0006-2952(83)90004-7subject
Has Abstractpub_date
1983-09-01 00:00:00pages
2473-7issue
17eissn
0006-2952issn
1873-2968pii
0006-2952(83)90004-7journal_volume
32pub_type
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
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pub_type: 杂志文章
doi:10.1016/0006-2952(83)90365-9
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journal_title:Biochemical pharmacology
pub_type: 杂志文章,评审
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pub_type: 杂志文章
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pub_type: 杂志文章,评审
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更新日期:1985-01-01 00:00:00
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/j.bcp.2007.02.005
更新日期:2007-06-01 00:00:00
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journal_title:Biochemical pharmacology
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journal_title:Biochemical pharmacology
pub_type: 杂志文章
doi:10.1016/0006-2952(83)90426-4
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pub_type: 杂志文章
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更新日期:2008-09-01 00:00:00
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pub_type: 杂志文章
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