RS-87337 

RS-87337 is an orally active piperazine-amidine hybrid class Ia (inhibiting V_max, IC₅₀ = 17 μM)/class III (prolonging ADP90, EC₁₅ = 2 μM) antiarrhythmic agent with selectivity for ventricular conduction. RS-87337 inhibits cardiac sodium channel, thereby reducing the maximum depolarization rate of action potential, with moderate onset and recovery kinetics. RS-87337 reduces cardiac outward potassium conductance (I_K), thus prolonging action potential duration. RS-87337 is applicable to research related to arrhythmia, ventricular arrhythmia, ventricular fibrillation, and myocardial ischemia-reperfusion injury^[1][2].

RS-87337 (0.1-30 μM; 30 min) produces class III (ADP90 prolongation, EC₁₅ = 2 μM) and class Ia (Vmax inhibition, IC₅₀ = 17 μM) antiarrhythmic effects in isolated guinea pig right ventricular papillary muscles, with intermediate sodium channel block kinetics^[2].
RS-87337 (10-1000 nM) does not impair baseline function of isolated working rat hearts, and at 1000 nM, it prevents reperfusion-induced ventricular fibrillation and maintains cardiac function following coronary ischemia^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RS-87337 (10 mg/kg; i.v.) shows no effects on intra-atrial or intra-ventricular conduction parameters, only one incidence of atrioventricular block at a pacing frequency of 261 beat/min, and no cardiodepressant effects on normal canine myocardium^[1].
RS-87337 (1-5 mg/kg; i.v.) significantly reduces the incidence of reperfusion-induced ventricular tachycardia, fibrillation, and mortality in anaesthetized Sprague-Dawley rats^[2].
RS-87337 (3-10 mg/kg; i.v.; 15-60 mg/kg; p.o.) reduces ectopic complex incidence in conscious dogs with post-coronary ligation arrhythmia, with rapid activity via i.v. (3, 10 mg/kg) and sustained activity via oral (30, 60 mg/kg) routes^[2].
RS-87337 (0.02-5.0 mg/kg; i.v.; cumulative doses) dose-dependently reduces S-T segment elevation during transient myocardial ischemia and speeds reperfusion recovery in anaesthetized beagle dogs without significant cardiodepression^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

395.28

C₁₈H₂₀Cl₂N₄O₂

107707-38-0

ClC1=CC(NC(N2CCN(CC2)C3=CC=C(C=C3OC)O)=N)=CC(Cl)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Allely MC, Alps BJ. Effects of the novel class Ia and class III antiarrhythmic agent RS-87337 on myocardial conduction in the anaesthetised dog. Arch Int Pharmacodyn Ther. 1988 Sep-Oct;295:138-46.
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  [2]. Dumez D, et al. Electrophysiologic, antiarrhythmic, and cardioprotective effects of N-[3,5 dichlorophenyl] 4-[4-hydroxy-2-methoxy-phenyl] piperazine carboxamidine dihydrochloride (RS-87337). J Cardiovasc Pharmacol. 1989 Aug;14(2):184-93.
   [Content Brief]