In this experiment, newly synthesized ultrashort-acting blockers of β-adrenergic receptors were t... more 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.
High rates of cardiovascular mortality have long been a serious problem in all European countries... more High rates of cardiovascular mortality have long been a serious problem in all European countries. Despite advancements in health care the situation is not improving fast enough. In the last decades, no new ultra-short-acting β-blockers have been registered in the European Union except for esmolol and landionol. In this study, eight newly-synthesised ultra-short-acting β-blockers were tested. These β-blockers contain an ester functional group which can be easily cleaved by plasma or cytoplasmic esterases. The substances were prepared in the
Composites of yeast glucan particles and curcumin lead to improvement of dextran sulfate sodium-i... more Composites of yeast glucan particles and curcumin lead to improvement of dextran sulfate sodium-induced acute bowel inflammation in rats
Ceská a Slovenská farmacie : casopis Ceské farmaceutické spolecnosti a Slovenské farmaceutické spolecnosti, 2014
In this experiment, newly synthesized ultrashort-acting blockers of β-adrenergic receptors were t... more 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 hig...
In this experiment, newly synthesized ultrashort-acting blockers of β-adrenergic receptors were t... more 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.
High rates of cardiovascular mortality have long been a serious problem in all European countries... more High rates of cardiovascular mortality have long been a serious problem in all European countries. Despite advancements in health care the situation is not improving fast enough. In the last decades, no new ultra-short-acting β-blockers have been registered in the European Union except for esmolol and landionol. In this study, eight newly-synthesised ultra-short-acting β-blockers were tested. These β-blockers contain an ester functional group which can be easily cleaved by plasma or cytoplasmic esterases. The substances were prepared in the
Composites of yeast glucan particles and curcumin lead to improvement of dextran sulfate sodium-i... more Composites of yeast glucan particles and curcumin lead to improvement of dextran sulfate sodium-induced acute bowel inflammation in rats
Ceská a Slovenská farmacie : casopis Ceské farmaceutické spolecnosti a Slovenské farmaceutické spolecnosti, 2014
In this experiment, newly synthesized ultrashort-acting blockers of β-adrenergic receptors were t... more 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 hig...
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