JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2014, 63(4):167-173 | DOI: 10.36290/csf.2014.033

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

Ondrej Baďo*, Marek Frydrych, Eliška Kolmanová, Markéta Dlouhá
Ústav humánní farmakologie a toxikologie FaF, Veterinární a farmaceutická univerzita, Brno

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-blockers; rat; systolic blood pressure; heart rate

Received: July 3, 2014; Accepted: July 21, 2014; Published: April 1, 2014  Show citation

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Baďo O, Frydrych M, Kolmanová E, Dlouhá M. In vivo testing of new ultrashort-acting β-blockers with the effect on systolic blood pressure and heart rate. Čes. slov. farm. 2014;63(4):167-173. doi: 10.36290/csf.2014.033.
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