Stereospecific in vitro and in vivo effects of the new sinus node inhibitor (+)-S 16257

European Journal of Pharmacology

Volumn 339, Issue 1, 1997, Pages 43-51

  Thollon, Catherine ^a   Bidouard, Jean Pierre ^a   Cambarrat, Christine ^a   Lesage, Ludovic ^a   Reure, Hélène ^a   Delescluse, Isabelle ^a   Vian, Joël ^a   Peglion, Jean Louis ^a   Vilaine, Jean Paul ^a  

^a INSTITUT DE RECHERCHES SERVIER   (France)

Author keywords

Bradycardic agent; Heart rate; QT interval; S 16257; Stereospecificity; Transmembrane action potential

Indexed keywords

7,8 DIMETHOXY 3 [3 [[(4,5 DIMETHOXYBENZOCYCLOBUTAN 1 YL)METHYL]METHYLAMINO]PROPYL] 1,3,4,5 TETRAHYDRO 2H 3 BENZAZEPIN 2 ONE; BENZAZEPINE DERIVATIVE; IVABRADINE; S 15544; S 16260; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRADYCARDIA; CHRONOTROPISM; ENANTIOMER; GUINEA PIG; HEART DEPOLARIZATION; HEART MUSCLE POTENTIAL; HEART RATE; HEART REPOLARIZATION; INTRAVENOUS DRUG ADMINISTRATION; ISOMER; MALE; NONHUMAN; PRIORITY JOURNAL; PURKINJE FIBER; QT INTERVAL; RABBIT; SINUS NODE; STEREOSPECIFICITY; SWINE;

ACTION POTENTIALS; ANIMALS; BENZAZEPINES; BIOLOGICAL CLOCKS; CARDIOTONIC AGENTS; ELECTROCARDIOGRAPHY; GUINEA PIGS; HEART RATE; MALE; PAPILLARY MUSCLES; PURKINJE FIBERS; RABBITS; SINOATRIAL NODE; STEREOISOMERISM; SWINE;

EID: 0031578576     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)01364-2     Document Type: Article

References (32)

1. Argentieri T.M., Troy H.H., Carroll M.S., Doroshuk C.M., Sullivan M.E. Electrophysiologic activity and antiarrhythmic efficacy of CK-3579, a new class III antiarrhythmic agent with β-adrenergic blocking properties. J. Cardiovasc. Pharmacol. 21:1993;647-655.
2. Bazett H.C. An analysis of the time-relations of electrocardiograms. Heart. 7:1920;353-370.
3. Bois P., Bescond J., Renaudon B., Lenfant J. Mode of action of bradycardic agent, S 16257, on ionic currents of rabbit sinoatrial node cells. Br. J. Pharmacol. 118:1996;1051-1057.
4. f) in guinea-pig dissociated sinoatrial node cells. Br. J. Pharmacol. 110:1993;343-349.
5. Carlsson L., Almgren O., Duker G. QTU-prolongation and torsades de pointes induced by putative class III antiarrhythmic agents in the rabbit: Etiology and interventions. J. Cardiovasc. Pharmacol. 16:1990;276-285.
6. Carmeliet E. Electrophysiologic and voltage clamp analysis of the effects of Sotalol on isolated cardiac muscle and Purkinje fibers. J. Pharmacol. Exp. Ther. 232:1985;817-825.
7. Carre F., Denolle T., Lecoz F., Violet I., Lerebours G., Gandon J.M. First intravenous phase I of S 16257, a new bradycardic agent: Effects on the maximal exercise parameters. Thérapie. 50:1995;377.
8. Di Francesco D. The onset and autonomic regulation of cardiac pacemaker activity: Relevance of the f current. Cardiovasc. Res. 29:1995;449-456.
9. Di Francesco, D., 1995. Cardiac pacemaker: 15 years of 'new' interpretation. Acta Cardiol. L, 413-427.
10. f) plays an important role in regulating SA node pacemaker activity. Cardiovasc. Res. 30:1995;307-308.
11. f) by cAMP in the rabbit sino-atrial node. J. Physiol. 474:1994;473-482.
12. Doerr T., Trautwein W. On the mechanism of the 'specific bradycardic action' of the verapamil derivative UL-FS49. Naunyn-Schmiedeberg's Arch. Pharmacol. 341:1990;331-340.
13. Dolphin A.C., Scott R.H. Interaction between calcium channel ligands and guanine nucleotides in cultured rat sensory and sympathetic neurones. J. Physiol. 413:1989;271-288.
14. + current acting as pure class III antiarrhythmic agents. J. Cardiovasc. Pharmacol. 20:1992;S106-S113.
15. F in rabbit sinoatrial node cells by Zatebradine (UL-FS 49). Circ. Res. 88:1993;2389-2401.
16. Guth B.D., Heusch G., Seitelberger R., Matsuzaki M., Ross J. Role of heart rate reduction in the treatment of exercise-induced myocardial ischaemia. Eur. Heart J. 8:1987;61-68.
17. Guth B.D., Heusch G., Seitelberger R., Ross J. Mechanism of beneficial effect of β-adrenergic blockade on exercise-induced myocardial ischemia in conscious dogs. Circ. Res. 60:1987;738-746.
18. Harron D.W.G., Jady K., Riddell J.G., Shanks R.G. Effects of alinidine, a novel bradycardic agent, on heart rate and blood pressure in man. J. Cardiovasc. Pharmacol. 4:1982;213-220.
19. Indolfi C., Guth B.D., Miura T., Miyazaki S., Schulz R., Ross J. Mechanisms of improved ischemic regional dysfunction by bradycardia. Studies on UL-FS 49 in swine. Circulation. 80:1989;983-993.
20. Irisawa H., Brown H.F., Giles W. Cardiac pacemaking in the sinoatrial node. Physiol. Rev. 73:1993;197-227.
21. Kobinger W., Lillie C. Cardiovascular characterization of UL-FS 49, 1,3,4,5-tetrahydro-7,8-dimethoxy-3-(3-)[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-2H-3-benzazepin-2-on hydrochloride, a new 'specific bradycardic agent'. Eur. J. Pharmacol. 104:1984;9-18.
22. Kobinger W., Lillie C. Specific bradycardic agents - a novel pharmacological class? Eur. Heart J. 8:1987;7-15.
23. Perez O., Gay P., Franqueza L., Carron R., Valenzuela C., Delpon E., Tamargo J. Effects of the two enantiomers, S-16257-2 and S-16260-2, of a new bradycardic agent on guinea-pig isolated cardiac preparations. Br. J. Pharmacol. 115:1995;787-794.
24. Rasmussen H.S., Allen M.J., Blackburn K.J., Butrous G.S., Dalrymple H.W. Dofetilide, a novel class III antiarrhythmic agent. J. Cardiovasc. Pharmacol. 20:1992;S96-S105.
25. Singh B.N. Antiarrhythmic actions of DL-sotalol in ventricular and supraventricular arrhythmias. J. Cardiovasc. Pharmacol. 20:1992;S75-S90.
26. Simon L., Ghaleh B., Puybasset L., Giudicelli J.F., Berdeaux A. Coronary and hemodynamic effects of S 16257, a new bradycardic agent, in resting and exercising conscious dogs. J. Pharmacol. Exp. Ther. 275:1995;659-666.
27. Surawicz B. Role of potassium channels in cycle length dependent regulation of action potential duration in mammalian cardiac Purkinje and ventricular muscles fibers. Cardiovasc. Res. 26:1992;1021-1029.
28. Thollon C., Cambarrat C., Vian J., Prost J.F., Peglion J.L., Vilaine J.P. Electrophysiological effects of S 16257, a novel sino-atrial node modulator, on rabbit and guinea-pig cardiac preparations: Comparison with UL-FS 49. Br. J. Pharmacol. 112:1994;37-42.
29. f) does not play an important role in regulating SA node pacemaker activity. Cardiovasc. Res. 30:1995;309-310.
30. Verheijck E.E., Van Ginneken A.C.G., Bourier J., Bouman L.N. Effects of delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ. Res. 76:1995;607-615.
31. 2+ channels in chick neural retina cells characterized by 1,4-dihydropyridine antagonists and activators. Can. J. Physiol. Pharmacol. 67:1989;506-514.
32. Zaza A., Robinson R.B., Di Francesco D. Basal responses of the L-type Ca2+ and hyperpolarization-activated currents to autonomic agonists in the rabbit sino-atrial node. J. Physiol. 491(2):1996;347-355.