[Effect of cordarone on the cellular adrenergic systems].
Cordarone was examined for its effects on alpha- and beta-adrenergic receptors and adenylate cyclase (AC) of some tissues. Cordarone was shown to suppress the binding of [3H]-clonidine with alpha 2-receptors of the rabbit brain (Ki = 4 microM) and that of [3H]-prazosin with alpha 1-receptors of the rat liver (Ki = 22 microK), but not to displace [3H]-dihydroalprenolol from rabbit cardiac and pulmonary beta 1-receptors and from beta 2-receptors of rat reticulocytes and human lungs. Cordarone failed to affect the activity of rabbit heart and lung AC, as well as that of thrombocytes and human lungs, but showed a 80% inhibition of the activating effect of isoproterenol on reticulocyte AC. It was suggested that the effect of cordarone on reticulocytes was not mediated by beta-receptors and was tissue specific and dependent on the characteristics of AC regulation in these cells. Cordarone's antiadrenergic effect found in vitro may be one of the causes of its coronary dilating and antiarrhythmic effects.
Kurennaia
G S
GS
Baldenkov
G N
GN
Tkachuk
V A
VA
Mazur
N A
NA
D000067956:Adenylyl Cyclase Inhibitors; D000262:Adenylyl Cyclases / Q000378:metabolism; D000638:Amiodarone / Q000494:pharmacology*; D000818:Animals; D001773:Blood Cells / Q000187:drug effects / Q000502:physiology; D001921:Brain / Q000166:cytology / Q000187:drug effects / Q000201:enzymology; D003864:Depression, Chemical; D006321:Heart / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008168:Lung / Q000166:cytology / Q000187:drug effects / Q000201:enzymology; D009206:Myocardium / Q000166:cytology / Q000201:enzymology; D011817:Rabbits; D051381:Rats; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects* / Q000502:physiology; D011943:Receptors, Adrenergic, beta / Q000187:drug effects* / Q000502:physiology; D014781:Viscera / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology
D000067956:Adenylyl Cyclase Inhibitors; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; D000262:Adenylyl Cyclases; D000638:Amiodarone
Deĭstvie kordarona na adrenergicheskie sistemy kletki.