N-(2,6-Dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165): a new potent and long-acting antiarrhythmic agent. 1985

K Aisaka, and T Hidaka, and N Inomata, and S Hamasaki, and T Ishihara, and M Morita

N-(2,6-Dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165) at the doses of 2.5 mg/kg i.v. and 3-10 mg/kg i.d. or p.o. restored sinus rhythm from ventricular multifocal arrhythmias induced by two-stage ligation of the coronary artery in the conscious dogs, Harris model, without causing gastrointestinal and central nervous system side effects. The onset of antiarrhythmic action was 1-2 min after i.v. injection and 15-30 min after an oral administration, and this action lasted longer than 1 h after i.v. and 6 h after oral administration, respectively. SUN 1165 was also effective in suppressing ouabain-and halothane-epinephrine-induced ventricular arrhythmias at the doses of 1.7 and 1.2 mg/kg i.v. and 1-10 mg/kg i.d. It did not impair parasympathetic nerve activity. SUN 1165 showed a local anesthetic or membrane stabilizing activity comparable to lidocaine and disopyramide. In conscious dogs without arrhythmia, SUN 1165 had no deleterious cardiohemodynamic effect and no gross behavioral effect at the oral doses of 3 and 10 mg/kg. Thus, it is concluded that SUN 1165 is an orally effective, potent and long-acting class I type antiarrhythmic agent without serious side effects common to other antiarrhythmic drugs.

UI MeSH Term Description Entries
D008012 Lidocaine A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE. Lignocaine,2-(Diethylamino)-N-(2,6-Dimethylphenyl)Acetamide,2-2EtN-2MePhAcN,Dalcaine,Lidocaine Carbonate,Lidocaine Carbonate (2:1),Lidocaine Hydrocarbonate,Lidocaine Hydrochloride,Lidocaine Monoacetate,Lidocaine Monohydrochloride,Lidocaine Monohydrochloride, Monohydrate,Lidocaine Sulfate (1:1),Octocaine,Xylesthesin,Xylocaine,Xylocitin,Xyloneural
D008297 Male Males
D009200 Myocardial Contraction Contractile activity of the MYOCARDIUM. Heart Contractility,Inotropism, Cardiac,Cardiac Inotropism,Cardiac Inotropisms,Contractilities, Heart,Contractility, Heart,Contraction, Myocardial,Contractions, Myocardial,Heart Contractilities,Inotropisms, Cardiac,Myocardial Contractions
D010042 Ouabain A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE. Acocantherin,G-Strophanthin,Acolongifloroside K,G Strophanthin
D010210 Papillary Muscles Conical muscular projections from the walls of the cardiac ventricles, attached to the cusps of the atrioventricular valves by the chordae tendineae. Muscle, Papillary,Muscles, Papillary,Papillary Muscle
D002462 Cell Membrane The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells. Plasma Membrane,Cytoplasmic Membrane,Cell Membranes,Cytoplasmic Membranes,Membrane, Cell,Membrane, Cytoplasmic,Membrane, Plasma,Membranes, Cell,Membranes, Cytoplasmic,Membranes, Plasma,Plasma Membranes
D003326 Coronary Circulation The circulation of blood through the CORONARY VESSELS of the HEART. Circulation, Coronary
D003331 Coronary Vessels The veins and arteries of the HEART. Coronary Arteries,Sinus Node Artery,Coronary Veins,Arteries, Coronary,Arteries, Sinus Node,Artery, Coronary,Artery, Sinus Node,Coronary Artery,Coronary Vein,Coronary Vessel,Sinus Node Arteries,Vein, Coronary,Veins, Coronary,Vessel, Coronary,Vessels, Coronary
D004206 Disopyramide A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties. Diisopyramide,Disopyramide Monohydrochloride,Disopyramide Phosphate,Disopyramide Phosphate (1:1),Disopyramide Phosphate (1:1), (+-)-Isomer,Disopyramide Phosphate (1:1), (R)-Isomer,Disopyramide Phosphate (1:1), (S)-Isomer,Disopyramide, (+-)-Isomer,Disopyramide, (R)-Isomer,Disopyramide, (S)-Isomer,Disopyramide, D-Tartrate (1:1), (S)-Isomer,Disopyramide, L-Tartrate (1:1), (R)-Isomer,Disopyramide, L-Tartrate (1:1), (S)-Isomer,Disopyramide, L-Tartrate (1:2), (+-)-Isomer,Disopyramide, L-Tartrate, (S)-isomer,Norpace,Palpitin,Palpitine,Rhythmodan,Ritmilen,Rythmilen,SC-13957,SC 13957,SC13957
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog

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