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Arythmogenic effects of sigma agonist BD737

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NOVÁKOVÁ Marie BRAVENÝ Pavel

Rok publikování 1999
Druh Článek ve sborníku
Konference 1st Oslo Conference on Molecular Cardiology and Myocardial Function.
Fakulta / Pracoviště MU

Lékařská fakulta

Citace
Obor Fyziologie
Klíčová slova cardiac sigma receptor; arhythmogenesis; BD737
Popis Sigma receptor binding has been reported to alter contractility in isolated ventricular rat myocytes and to severely impair the regular rhythm in cell cultures. The aim of this study was to prove these effects of a highly selective sigma ligand BD737 in isolated perfused hearts. In contrast to isolated myocytes, the perfused whole hearts did not exhibit significant inotropic effects of 10nM BD737. However, the heart rate, steady at control conditions, revealed marked fluctuations, characteristic for IP3 production and [Ca2+]i oscillations measured in isolated myocytes. BD737 in 100nM concentration provoked bigeminy, multifocal ectopies and eventually, cardiac arrest. In conclusion, the perfused hearts are sensitive to sigma ligands in nanomolar concentrations, although the effects quantitavely differ from those on isolated myocytes.

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