Beneficial effects of amiodarone in heart failure: interaction with beta-adrenoceptors rather than G proteins.
The effect of the antiarrhythmic drug amiodarone on the human myocardial beta-adrenoceptor-G protein-adenylyl cyclase signalling cascade was investigated. Amiodarone had no effect on myocardial G proteins and maximal adenylyl cyclase activity, but acted as a beta-adrenoceptor antagonist. This mechanism might be at least partially responsible for the beneficial effects of the drug in patients with arrhythmia and heart failure.
Schnabel
P
P
Klinik III für Innere Medizin der Universität zu Köln, Cologne, Germany.
Mies
F
F
Maack
C
C
Rosenkranz
S
S
Zolk
O
O
Böhm
M
M
D000262:Adenylyl Cyclases / Q000378:metabolism; D000318:Adrenergic beta-Agonists / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists; D000638:Amiodarone / Q000627:therapeutic use*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000627:therapeutic use*; D019204:GTP-Binding Proteins / Q000187:drug effects* / Q000378:metabolism; D006321:Heart / Q000187:drug effects*; D006333:Heart Failure / Q000188:drug therapy*; D006801:Humans; D007545:Isoproterenol / Q000494:pharmacology; D009206:Myocardium / Q000201:enzymology / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D011943:Receptors, Adrenergic, beta / Q000187:drug effects* / Q000378:metabolism
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D000889:Anti-Arrhythmia Agents; D011943:Receptors, Adrenergic, beta; D019204:GTP-Binding Proteins; D000262:Adenylyl Cyclases; D007545:Isoproterenol; D000638:Amiodarone