title: [In vivo testing of new ultrashort-acting β-blockers with the effect on systolic blood pressure and heart rate].
abstract: 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.
authors.forename: Ondrej
authors.initials: O
authors.lastname: Baďo
authors.forename: Marek
authors.initials: M
authors.lastname: Frydrych
authors.forename: Eliška
authors.initials: E
authors.lastname: Kolmanová
authors.forename: Markéta
authors.initials: M
authors.lastname: Dlouhá
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects*; D051381:Rats; D011943:Receptors, Adrenergic, beta / Q000187:drug effects
chemical_list: D000319:Adrenergic beta-Antagonists; D011943:Receptors, Adrenergic, beta