Haustein K O, Nowak G
Arch Int Pharmacodyn Ther. 1979 Jun;239(2):270-82.
The cardiac and extracardiac effects of a new glycoside, helveticosol-3',4'-di-nitrate (HdN), were compared with those of helveticosol (H) and helveticosol-3',4'-di-propionate (HdP) in isolated guinea-pig heart preparations, in volunteers and dogs. In the atrium and heart, HdN produces positive inotropic effects at the same concentrations as H and at 10 times lower concentrations than HdP. In the heart, the difference between equieffective concentrations of HdN and HdP is smaller, but this is true only for the concentration required to produce the maximum inotropic effect. In the anaesthetized dog equieffective cardiac effects are obtained after oral admiinistration of the glycosides in the ratio 1 : 2 : 0.5 (HdN : HdP : H). After administration of HdN and HdP at equal ratios, no significant differences were observed between the toxic effects in conscious dogs or in the extent of shortening of STI in volunteers. Replacement of the hydrophobic subsituent propionate for the more hydrophilic nitrate residue causes slight changes in cardiac efficiency.
在离体豚鼠心脏制剂、志愿者和犬身上,比较了一种新糖苷helveticosol - 3',4'-二硝酸酯(HdN)与helveticosol(H)和helveticosol - 3',4'-二丙酸酯(HdP)的心脏和心脏外效应。在心房和心脏中,HdN在与H相同的浓度下产生正性肌力作用,且浓度比HdP低10倍。在心脏中,HdN和HdP等效浓度之间的差异较小,但这仅适用于产生最大正性肌力作用所需的浓度。在麻醉犬中,口服糖苷的比例为1 : 2 : 0.5(HdN : HdP : H)时可获得等效的心脏效应。以相等比例给予HdN和HdP后,在清醒犬的毒性作用或志愿者的STI缩短程度方面未观察到显著差异。用亲水性更强的硝酸酯残基取代疏水性的丙酸酯取代基会使心脏效率略有变化。