GE 70 (rac-1-[3-(phenylethyl)-2-benzofuryl]-2-(isopropyl-amino)-ethanol hydrochloride) is a newly synthesized antiarrhythmic compound in a series of substances structurally related to propafenone (Figure 1). Racemic propafenone is classified as a Ic antiarrhythmic agent. Besides these properties propafenone posesses a weak calcium antagonistic effect and nonselective beta-adrenoceptor blocking activity, which may be clinically relevant in humans. The (+)-(S)-enantiomer is the beta-adreno-ceptor blocking moiety of propafenone, whereas both (R)-and (S)-propafenone exert equal class I antiarrhythmic activity. Propafenone blocks sodium channels during the activated and the inactivated states. The drug provoked a flickering block in DPI-modified sodium channels.
GE 70 was shown to possess negative inotropic and negative chronotropic effects in papillary muscles and spontaneously beating right atria, whereas beta-adrenoceptor blocking activity was insignificant. Thus, we studied in more detail the effects of GE 70 with respect to its sodium channel blocking activity in papillary muscles and ventricular myocytes of guinea pigs.
Figure 1 Structural formulas of propafenone (left) and GE 70 fright)
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