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The information on the inhibitory effect of propafenone in vascular smooth  muscle is sparse. Propafenone acts through blockage of voltage-dependent  cardiac Na+ channels, L-type Ca2+ channels, voltage-sensitive K+ (Kv)  channels, as well as β-adrenergic receptors in the heart. The introduction  of different chemical groups in the benzyl moiety of propafenone influences  pharmacological properties of newly developed derivate of propafenone. Here  we investigated the effect of new ortho-chloro derivate of propafenone  (5OCl) on the vascular tone of precontracted rat aorta. 5OCl produced  endothelium-independent relaxation of rat aorta. In order to test the  involvement of different ion channels in 5OCl mechanism of action,  antagonist of Na+, lidocaine, KV channels, 4-aminopyiridine (4-AP) and  L-type Ca2+ channels, nifedipine were used. All tested antagonists of ion  channels did not influence the relaxation of rat aorta induced by high a  concentration of 5OCl (≥10 μM), but antagonized the relaxation induced by  low concentrations of this propafenone derivate. Thus, 5OCl derivate has  comparable potency and efficacy as propafenone. According to its interaction  with lidocaine, 4-AP and nifedipine it seems that 5OCl partly shares the  mechanism of action with propafenone. The mechanism of vasodilatation  induced by high micromolar concentration of 5OCl is not defined and further  investigations are necessary

The novel ortho-chloro derivate propafenone induced relaxation in isolated rat aorta