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In vivo testing of new ultrashort-acting β-blockers with the effect on systolic blood pressure and heart rate


Authors: Ondrej Baďo;  Marek Frydrych;  Eliška Kolmanová;  Markéta Dlouhá
Authors‘ workplace: Ústav humánní farmakologie a toxikologie FaF, Veterinární a farmaceutická univerzita, Brno
Published in: Čes. slov. Farm., 2014; 63, 167-173
Category: Original Articles

Overview

In this experiment, newly synthesized ultrashort-acting blockers of β-adrenergic receptors were tested. Compounds were synthesized at the Department of Chemical Drugs of Pharmaceutical Faculty VFU Brno as esters of aryloxyaminopropanol, thereby gaining a very short half-life in blood plasma. Experiment was conducted in vivo in a rat model. Changes in systolic blood pressure and heart rate were monitored by invasive method in normotensive rats. The values ​​of blood pressure and heart rate were recorded for 20 minutes following the i.v. administration of tested substances or placebo into the jugular vein. In the experiment was tested a series of four substances (2MC2, 2MC2b, 2MC2c, 2MC2d) with different alkyl chain length at a dose of 3.0 mg·kg–1. After evaluation of results was carried out the second part of the experiment, i.e. testing of substances 2MC2c and 2MC2d at a lower dose of 1.0 mg·kg–1. The results show the best effect of 2MC2d, asubstance with longest alkyl chain and highest lipophilicity.

Keywords:
ultrashort-acting β-blockersratsystolic blood pressureheart rate


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