Key result
Procainamide and its sulfonylcarbamide derivatives reversed carbachol-induced action potential duration shortening in guinea pig atrial muscles, with PA20 exhibiting the most potent anticholinergic effect.
Why the study?
Do procainamide and its sulfonylcarbamide derivatives reverse carbachol-induced action potential shortening and contraction force decrease in guinea pig atrial muscles?
Do procainamide and its sulfonylcarbamide derivatives reverse carbachol-induced action potential shortening and contraction force decrease in guinea pig atrial muscles?
The procainamide derivative PA20 demonstrates the most potent anticholinergic effect among the tested sulfonylcarbamide derivatives in reversing carbachol-induced electromechanical changes in guinea pig atria.
Answers are grounded in this paper and cite their sources.
Caution against clinical use of PA20; leaves open whether sulfonylcarbamide derivatives merit translation beyond guinea pig atria.
The aim of the study was to investigate the effect of class IA antiarrhythmic drug procainamide and its new derivatives PA20, PA23, PA28 and PA53 on carbachol-induced action potential duration and contraction force in guinea pig atrial muscles. Experiments were carried out using standard method of registration of myocardium electromechanical activity. Under control conditions (perfusion of atrial strips with Tyrode solution), mean action potential duration measured at 90% (AP90) and 50% (AP50) of repolarization were 92.5+/-4.5 ms and 44.4+/-2.9 ms (n=18), respectively, and contraction force was of 2.7+/-0.5 mN (n=12). Carbachol (10(-6) M), an agonist of muscarinic acetylcholine receptor and activator of K(Ach) channels, markedly decreased AP90 to 32.4+/-2.4%, AP50 - to 25.4+/-2.2% (n=18) (p<0.001) and contraction force - to 24.2+/-5.8% (n=16) (p<0.05), vs. control. Procainamide and its new sulfonylcarbamide derivatives PA20, PA23, PA28 (10(-5)-3x10(-3) M), and PA53 (10(-5)-10(-3) M) reversed the carbachol-induced action potential duration shortening at different extent: procainamide derivative PA20 (N-cyclohexylsulfonylcarbamide fragment is linked up to benzene ring) had the most potent anticholinergic effect on action potential duration and contraction force of guinea pig atrial muscles. N-ethylsulfonylcarbamide fragment in PA23 or permanent positive charge of aliphatic nitrogen in PA28 had a weaker anticholinergic effect (similar to procainamide action) on action potential duration and contraction force than PA20. The weakest anticholinergic effect was induced by procainamide derivative PA53 with isosteric form of sulfonylcarbamide.
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Gendvilienė et al. (2007) studied this question. Procainamide and its sulfonylcarbamide derivatives (PA20, PA23, PA28, PA53) vs. Carbachol alone / Tyrode solution control was evaluated on Carbachol-induced action potential duration and contraction force shortening. Procainamide and its sulfonylcarbamide derivatives reversed carbachol-induced action potential duration shortening in guinea pig atrial muscles, with PA20 exhibiting the most potent anticholinergic effect.
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