[In vivo testing of new ultrashort-acting ß-blockers with the effect on systolic blood pressure and heart rate]. / In vivo testovanie nových ultrakrátko pôsobiacich ß-blokátorov s efektom na systolický krvný tlak a tepovú frekvenciu.

In this experiment, newly synthesized ultrashort-acting blockers of ß-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.