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Jacek Sapa - One of the best experts on this subject based on the ideXlab platform.

  • Antiarrhythmic Activity of new 2 methoxyphenylpiperazine xanthone derivatives after ischemia reperfusion in rats
    Pharmacological Reports, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic and α-Adrenoceptor Antagonistic Properties of Novel Arylpiperazine Derivatives of Pyrrolidin-2-one
    Archiv Der Pharmazie, 2015
    Co-Authors: Paula Zaręba, Magdalena Dudek, Klaudia Lustyk, Agata Siwek, Gabriela Starowicz, Leszek Nowiński, Małgorzata Zygmunt, Jacek Sapa, Marek Bednarski, Barbara Malawska
    Abstract:

    : In an effort to develop α-adrenoceptor antagonists with Antiarrhythmic Activity, we designed a series of pyrrolidin-2-one derivatives. The α1- and α2-adrenorecepor affinities of the new pyrrolidin-2-one derivatives were determined using a radioligand binding assay. The most active compound was then tested in vitro for intrinsic Activity toward α(1A)- and α(1B)-adrenoceptors and in vitro for Antiarrhythmic Activity in epinephrine-induced arrhythmia in rats. The highest affinity for the α1-adrenoceptor (pK(i) = 7.01) was displayed by 1-{4-[4-(2-methoxy-5-chlorophenyl)-piperazin-1-yl]-methyl}-pyrrolidin-2-one (9). 1-[4-(2-Fluorophenyl)-piperazin-1-yl]-methyl-pyrrolidin-2-one (7) showed the highest affinity toward the α2-adrenoceptor (pK(i) = 6.52). Intrinsic Activity studies of compound 9 showed that this compound is an antagonist of both α(1A)- (EC50 = 0.5 nM) and α(1B)- (EC50 = 51.0 nM) adrenoceptors. Compound 9 displayed Antiarrhythmic Activity in rats (ED50 = 5.0 mg/kg (3.13-7.99)). New derivatives of pyrrolidin-2-one with α1 -adrenoceptor affinity were identified. We propose that the Antiarrhythmic Activity of compound 9 is related to its antagonism of α(1A)- and α(1B)-adrenoceptors.

  • Antiarrhythmic Activity of new 2-methoxyphenylpiperazine xanthone derivatives after ischemia/reperfusion in rats
    Pharmacological reports : PR, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
    European journal of pharmacology, 2014
    Co-Authors: Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, Natalia Szkaradek, Henryk Marona
    Abstract:

    A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for Antiarrhythmic Activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological Activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant Activity, some biochemical studies were also performed. All tested compounds showed prominent Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed Antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking Activity. The results of this study suggest that new compounds with Antiarrhythmic Activity might be found in the group of xanthone derivatives.

  • Antiarrhythmic and antioxidant Activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
    Naunyn-Schmiedeberg's Archives of Pharmacology, 2011
    Co-Authors: Jacek Sapa, Alicja Nowaczyk, Katarzyna Kulig
    Abstract:

    A series of novel pyrrolidin-2-one derivatives (17 compounds) with adrenolytic properties was evaluated for Antiarrhythmic, electrocardiographic and antioxidant Activity. Some of them displayed Antiarrhythmic Activity in barium chloride-induced arrhythmia and in the rat coronary artery ligation-reperfusion model, and slightly decreased the heart rate, prolonged P–Q, Q–T intervals and QRS complex. Among them, compound EP-40 (1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one showed excellent Antiarrhythmic Activity. This compound had significantly antioxidant effect, too. The present results suggest that the Antiarrhythmic effect of compound EP-40 is related to their adrenolytic and antioxidant properties. A biological Activity prediction using the PASS software shows that compound EP-35 and EP-40 can be characterized by antiischemic Activity; whereas, compound EP-68, EP-70, EP-71 could be good tachycardia agents.

Henryk Marona - One of the best experts on this subject based on the ideXlab platform.

  • Antiarrhythmic Activity of new 2 methoxyphenylpiperazine xanthone derivatives after ischemia reperfusion in rats
    Pharmacological Reports, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of new 2-methoxyphenylpiperazine xanthone derivatives after ischemia/reperfusion in rats
    Pharmacological reports : PR, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
    European journal of pharmacology, 2014
    Co-Authors: Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, Natalia Szkaradek, Henryk Marona
    Abstract:

    A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for Antiarrhythmic Activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological Activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant Activity, some biochemical studies were also performed. All tested compounds showed prominent Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed Antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking Activity. The results of this study suggest that new compounds with Antiarrhythmic Activity might be found in the group of xanthone derivatives.

Barbara Filipek - One of the best experts on this subject based on the ideXlab platform.

  • Antiarrhythmic Activity of new 2 methoxyphenylpiperazine xanthone derivatives after ischemia reperfusion in rats
    Pharmacological Reports, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of new 2-methoxyphenylpiperazine xanthone derivatives after ischemia/reperfusion in rats
    Pharmacological reports : PR, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
    European journal of pharmacology, 2014
    Co-Authors: Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, Natalia Szkaradek, Henryk Marona
    Abstract:

    A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for Antiarrhythmic Activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological Activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant Activity, some biochemical studies were also performed. All tested compounds showed prominent Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed Antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking Activity. The results of this study suggest that new compounds with Antiarrhythmic Activity might be found in the group of xanthone derivatives.

  • Synthesis and Antiarrhythmic properties of basic amide derivatives of imidazolidine-2,4-dione and pyrrolidine-2,5-dione. II
    Farmaco (Societa chimica italiana : 1989), 1995
    Co-Authors: Katarzyna Kieć-kononowicz, Barbara Filipek, Hanna Byrtus, A. Zejc, Pierre Chevallet
    Abstract:

    Basic amide derivatives of imidazolidine-2,4-dione and pyrrolidine-2,5-dione were synthesized as potential Antiarrhythmic agents. Some of them have shown Antiarrhythmic Activity in the chloroform, barium chloride or adrenaline induced arrhythmia.

  • Influence of ethanol on the Antiarrhythmic Activity of verapamil.
    Polish journal of pharmacology and pharmacy, 1992
    Co-Authors: Barbara Filipek, Krupińska J, K. Zebala, Ilona Szymańska, Tadeusz Librowski, Wojciech Piekoszewski
    Abstract:

    The aim of this work was to determine the influence of ethanol on the Antiarrhythmic Activity of verapamil in the model of calcium arrhythmia in rats non-dependent and dependent on ethanol. The results of the experiment show that a combined, single administration of ethanol and verapamil attenuates in a statistically significant manner the Antiarrhythmic effect of verapamil. Ethanol administered repeatedly together with verapamil does not diminish the Antiarrhythmic Activity of verapamil.

Anna Rapacz - One of the best experts on this subject based on the ideXlab platform.

  • Antiarrhythmic Activity of new 2 methoxyphenylpiperazine xanthone derivatives after ischemia reperfusion in rats
    Pharmacological Reports, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of new 2-methoxyphenylpiperazine xanthone derivatives after ischemia/reperfusion in rats
    Pharmacological reports : PR, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
    European journal of pharmacology, 2014
    Co-Authors: Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, Natalia Szkaradek, Henryk Marona
    Abstract:

    A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for Antiarrhythmic Activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological Activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant Activity, some biochemical studies were also performed. All tested compounds showed prominent Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed Antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking Activity. The results of this study suggest that new compounds with Antiarrhythmic Activity might be found in the group of xanthone derivatives.

Natalia Szkaradek - One of the best experts on this subject based on the ideXlab platform.

  • Antiarrhythmic Activity of new 2 methoxyphenylpiperazine xanthone derivatives after ischemia reperfusion in rats
    Pharmacological Reports, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of new 2-methoxyphenylpiperazine xanthone derivatives after ischemia/reperfusion in rats
    Pharmacological reports : PR, 2015
    Co-Authors: Anna Rapacz, Magdalena Dudek, Jacek Sapa, Barbara Filipek, Karolina Pytka, Natalia Szkaradek, Henryk Marona
    Abstract:

    Abstract Background We have previously shown significant prophylactic and therapeutic Antiarrhythmic Activity in adrenaline-induced arrhythmia, as well as α 1 -adrenolytic properties of new derivatives of xanthone. Herein, we investigated their Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated hearts. Furthermore, we assessed antioxidant Activity in biochemical studies. Methods Antiarrhythmic Activity in the model of ischemia/reperfusion in isolated perfused hearts was performed according to the Langendorff technique. Antioxidant Activity was measured by lipid peroxidation level in tissue homogenate and in the FRAP assay. Results All studied compounds ( MH-94 , MH-99 and MH-105 ) showed significant Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. However, they did not demonstrate antioxidant effect, probably, because of the lack of free hydroxyl group(s) at a key position in the xanthone scaffold. Conclusions The present study provides evidences for Antiarrhythmic Activity of some 2-methoxyphenylpiperazine derivatives of xanthone.

  • Antiarrhythmic Activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
    European journal of pharmacology, 2014
    Co-Authors: Anna Rapacz, Jacek Sapa, Marek Bednarski, Barbara Filipek, Natalia Szkaradek, Henryk Marona
    Abstract:

    A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for Antiarrhythmic Activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological Activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant Activity, some biochemical studies were also performed. All tested compounds showed prominent Antiarrhythmic Activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed Antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking Activity. The results of this study suggest that new compounds with Antiarrhythmic Activity might be found in the group of xanthone derivatives.