ORM-10962

ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC 50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effect In Vitro ORM-10962 (10 nM, 100 nM and 1 μM) decreased the NCX current in dog ventricular myocytes in a concentration-dependent manner with estimated IC 50 values of 55 and 67 nM at -80 and at 20 mV, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ORM-10962 (0.3 mg/kg, IV, once) pre-treatment significantly delays the development and recurrence of ventricular extrasystoles (by about 50%) or ventricular tachycardia (by about 30%) in anesthetized guinea pigs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male guinea-pigs (250-300 g) Dosage: 0.3 mg/kg Administration: IV, 10 min before starting ouabain infusion Result: Significantly delayed the development of ventricular extrasystoles (from 24±1.7 min in controls to 36.6±2.7 min in the presence of the drug) or ventricular tachycardia (from 31.8±1.8 min in controls to 40.8±2.1 min in the presence of the drug). Form:Solid IC50& Target:NCX

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