Key result
The newly synthesized compounds 44Bu and 444 produced significant bradycardic effects in rats with isoprenaline-induced tachycardia, though their maximum effects were less than that of esmolol.
Why the study?
Do newly synthesized ultrashort-action beta-blockers reduce heart rate in an isoprenaline-induced tachycardia rat model?
Do newly synthesized ultrashort-action beta-blockers reduce heart rate in an isoprenaline-induced tachycardia rat model?
Two newly synthesized ultrashort-acting beta-blockers demonstrated significant bradycardic effects and blockade of sodium and potassium currents in a rat model.
Answers are grounded in this paper and cite their sources.
These rat data merit further preclinical optimization; leaves open clinical translation of ultrashort-acting beta-blockade.
Changes in the heart rate induced by four different doses of two newly synthesized potential ultrashort-action antagonists of beta adrenergic receptors were tested in 90 male laboratory Wistar rats. The isoprenaline-induced tachycardia model was used. Their effects were compared with those of esmolol. In the second part of the study, approximate electro-physiological measurements were made in vitro to assess the influence of the compounds tested on ion membrane currents in isolated ventricular cardiomyocytes. Both compounds demonstrated significant bradycardic effects in all concentrations tested compared with the control group, but they differed in the time of the onset of their action. Both newly synthesized compounds induced blockade of the fast sodium current (I Na ) and potassium currents (I to , I K1 , I K,end ).
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Bartošová et al. (2006) studied Isoprenaline-induced tachycardia (n=90). Compounds 44Bu and 444 vs. Esmolol and placebo was evaluated on Maximum heart rate reduction from baseline (p=<0.001). The newly synthesized compounds 44Bu and 444 produced significant bradycardic effects in rats with isoprenaline-induced tachycardia, though their maximum effects were less than that of esmolol.
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