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  1. Article: Menarini Academy Cardiovascular Research Awards in Basic Science 2001: ligands of the orphan receptor peroxisome-proliferator activator-gamma reduce myocardial infarct size.

    Thiemermann, C / Wayman, N S

    Medical science monitor : international medical journal of experimental and clinical research

    2001  Volume 7, Issue 4, Page(s) 787–789

    MeSH term(s) Awards and Prizes ; Humans ; Ligands ; Myocardial Infarction/pathology ; Receptors, Cytoplasmic and Nuclear/metabolism ; Thiazoles/metabolism ; Transcription Factors/metabolism
    Chemical Substances Ligands ; Receptors, Cytoplasmic and Nuclear ; Thiazoles ; Transcription Factors
    Language English
    Publishing date 2001-07
    Publishing country United States
    Document type Letter
    ZDB-ID 1439041-3
    ISSN 1643-3750 ; 1234-1010
    ISSN (online) 1643-3750
    ISSN 1234-1010
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4924: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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  2. Article: 5-aminoisoquinolinone, a potent inhibitor of poly (adenosine 5'-diphosphate ribose) polymerase, reduces myocardial infarct size.

    Wayman, N / McDonald, M C / Thompson, A S / Threadgill, M D / Thiemermann, C

    European journal of pharmacology

    2001  Volume 430, Issue 1, Page(s) 93–100

    Abstract: This study investigates the effects of a novel, water-soluble inhibitor of the activity of poly (adenosine 5'-diphosphate ribose) polymerase, 5-aminoisoquinolinone [5-aminoisoquinolin-1(2H)-one], on (i) poly (adenosine 5'-diphosphate ribose) polymerase ... ...

    Abstract This study investigates the effects of a novel, water-soluble inhibitor of the activity of poly (adenosine 5'-diphosphate ribose) polymerase, 5-aminoisoquinolinone [5-aminoisoquinolin-1(2H)-one], on (i) poly (adenosine 5'-diphosphate ribose) polymerase activity in rat cardiac myoblasts and (ii) the infarct size caused by regional myocardial ischaemia and reperfusion in the rat. Exposure of H9c2 cells to hydrogen peroxide (H2O2, 1 mM) caused a significant increase in poly (adenosine 5'-diphosphate ribose) polymerase activity and an 80-90% reduction in mitochondrial respiration (cellular injury). Pretreatment of these cells with 5-aminoisoquinolinone (0.003-1 mM) caused a concentration-dependent inhibition of poly (adenosine 5'-diphosphate ribose) polymerase activity (IC50: approximately 4.5 microM, n=6-9) and cell injury (EC50: approximately 4.45 microM, n=9). In a rat model of myocardial infarction, left anterior descending coronary artery occlusion (25 min) and reperfusion (2 h) resulted in an infarct size of 50+/-3%. Administration (1 min before reperfusion) of 5-aminoisoquinolinone reduced myocardial infarct size in a dose-related fashion. Thus, 5-aminoisoquinolinone is a potent inhibitor of poly (adenosine 5'-diphosphate ribose) polymerase activity in cardiac myoblasts and reduces myocardial infarct size in vivo.
    MeSH term(s) Animals ; Cells, Cultured ; Enzyme Inhibitors/pharmacology ; Heart/drug effects ; Hydrogen Peroxide ; Isoquinolines/chemical synthesis ; Isoquinolines/pharmacology ; Isoquinolines/therapeutic use ; Myocardial Ischemia/drug therapy ; Myocardial Ischemia/pathology ; Myocardial Reperfusion ; Myocardium/metabolism ; Myocardium/pathology ; Nitroblue Tetrazolium ; Poly(ADP-ribose) Polymerase Inhibitors ; Rats ; Staining and Labeling
    Chemical Substances 5-aminoisoquinolinone ; Enzyme Inhibitors ; Isoquinolines ; Poly(ADP-ribose) Polymerase Inhibitors ; Nitroblue Tetrazolium (298-83-9) ; Hydrogen Peroxide (BBX060AN9V)
    Language English
    Publishing date 2001-10-26
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 80121-5
    ISSN 1879-0712 ; 0014-2999
    ISSN (online) 1879-0712
    ISSN 0014-2999
    DOI 10.1016/s0014-2999(01)01359-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 522: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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