The effects of pincainide, a new beta-amino anilide, on contractile responses and 45Ca fluxes were studied in rat aorta and on spontaneous mechanical activity in rat portal veins. Pincainide (10(-5) to 10(-2) M) produced a dose-dependent inhibition of noradrenaline (NA) and high K+ -induced contractions. These inhibitory effects were observed with pincainide added either before or after the induced contractions. The Ca2+ -induced contractions of K+ -depolarized aorta as well as the spontaneous mechanical activity of portal veins were also inhibited by pincainide. Pincainide (5 X 10(-3) M) inhibited the 45Ca influx stimulated by 10(-6) M NA and increased 45Ca efflux. It was concluded that in isolated rat aorta, pincainide not only inhibited the influx of Ca2+ reducing the contractile responses to NA and high K+ but it also inhibited other effects related to NA-induced release of intracellular Ca2+ stores.

01 Nov 1983·European Journal of PharmacologyQ3 · MEDICINE

Comparison of three β-amino anilides: IQB-M-81, lidocaine and tocainide, on isolated rat atria

Q3 · MEDICINE

Article

Author: Teresa Tejerina ; Santos Barrigón ; Juan Tamargo

The effects of a new beta-amino anilide, IQB-M-81, on electrical and mechanical activity of isolated rat atria were studied and compared with those of lidocaine and tocainide. In spontaneously beating right atria IQB-M-81 produced a dose-dependent decrease in rate, contractile force and maximum following frequency and prolonged the sinus node recovery time and the effective refractory period of atrial fibers. The negative inotropic effect was not modified by pretreating the atria with atropine or practolol. In isolated right atria IQB-M-81 did not block the positive chronotropic and inotropic responses to isoprenaline but shifted the dose-response curve to the right. IQB-M-81 and lidocaine, but not tocainide, reduced in a dose-dependent manner the slow contractions induced by isoprenaline in K-depolarized right atria. These results suggest that in contrast to other beta-amino anilides, IQB-M-81 exerted a negative chronotropic effect and that it presented a class I antiarrhythmic effect on isolated rat atria. A possible class IV antiarrhythmic effect is also discussed.

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Indication	Highest Phase	Country/Location	Organization	Date
Arrhythmias, Cardiac	Phase 1	-	Iqb	-

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