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Abstract
The effects of amiodarone [2-butyl-3-(3,5-diiodo-4-β-diethylaminoethoxy-benzoyl)-benzofuran hydrochloride], a potent antianginal and antiarrhythmic drug, have been studied in vitro on the ATP splitting activities of several rabbit muscle preparations. The “actomyosin” and myofibrillar heart and crural muscle preparations contained a calcium-dependent ATPase, which was considered as representative of the contractile system, together with other ATPases which could be kept inactive by omitting magnesium ions and by adding sodium azide (mitochondrial ATPase). Amiodarone inhibits the magnesium-dependent enzyme of all preparations in the same way as it acts on guinea pig heart sodium and potassium activated magnesium-dependent ATPase; 6 inhibition was shown, in the case of heart “actomyosin”, to be competitive with respect to ATP, not to magnesium. On the “contractile” calcium-dependent ATPase of all preparations, however, amiodarone failed to exert any effect at concentrations up to 0.6 mM. It is concluded that amiodarone is not likely to impair muscular and cardiac contractility.
Published Version
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