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  • 1985-1989  (1)
  • 1980-1984  (1)
  • Cardiac glycosides  (1)
  • Cat papillary muscles  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of molecular medicine 62 (1984), S. 390-393 
    ISSN: 1432-1440
    Keywords: Amrinone ; Ouabain ; Positive inotropy ; Cat papillary muscles
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Amrinone has been shown to produce haemodynamic benefits in digitalis-treated patients. Since amrinone is a positive inotropic agent on isolated heart muscle, these benefits may mean that amrinone increases the maximal ouabain-induced increase in force of contraction, without causing toxicity. We have therefore measured, in cat right ventricular papillary muscles, the inotropic effects of ouabain, amrinone alone and amrinone with a maximally effective, non-toxic ouabain concentration (2×10−7 M). Ouabain is much more potent than amrinone (EC50-values: ouabain, 8×10−8 M, amrinone, 1–2.8×10−3 M). The highest amrinone concentration used (6×10−3 M) produced a significantly lower increase in force of contraction than ouabain (2×10−7 M) in the same muscles. After ouabain (2×10−7 M) produced a stable effect, no further increase in force of contraction was observed with any amrinone concentration. Sustained arrhythmias were observed in five of six muscles at 3×10−3 M amrinone with ouabain (2×10−7 M), but in only one of these muscles with amrinone 3×10−3 M alone. Since the positive inotropic effects of amrinone are not additive with those from a maximally effective ouabain concentration, the haemodynamic benefits seen in patients are probably due to non-cardiac effects of amrinone such as vasodilatation.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 332 (1986), S. 98-102 
    ISSN: 1432-1912
    Keywords: Cardiac glycosides ; Gomphoside ; Inotropic agents ; SAR
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The 5αH-cardenolide, gomphoside, is one of a small group of naturally occurring cardiac glycosides in which the sugar residue is bilinked to the steroid ring system. This arrangement prevents the sugar moiety from rotating and this makes gomphoside and related compounds potentially useful for structure-activity relationship (SAR) studies. When gomphoside was tested for inotropic activity using guinea pig left atria, the compound was found to have very high potency comparable to the most active 5βH-cardenolides. Removal of the sugar moiety reduced inotropic activity almost 500-fold indicating that it was the presence of the sugar moiety that was mainly responsible for the drug's high potency. Modification of the steroid or sugar residue of gomphoside reduced activity in all cases. It would thus appear that gomphoside with its high potency and non-rotatable glycosidic linkage is an excellent tool for SAR studies.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
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