| Autor: |
J, Neumann, T, Eschenhagen, I L, Grupp, A, Haverich, J W, Herzig, S, Hirt, P, Kalmár, W, Schmitz, H, Scholz, B, Stein, H, Wenzlaff, N, Zimmermann |
| Rok vydání: |
1996 |
| Předmět: |
|
| Zdroj: |
The Journal of pharmacology and experimental therapeutics. 277(3) |
| ISSN: |
0022-3565 |
| Popis: |
In trabeculae carneae from failing human myocardium, CGP 48506 increased the force of contraction, which reached 310 +/- 41% of predrug values at 100 mumol/l. Its stereoisomer CGP 48508 did not affect the force of contraction (100 mumol/l). The positive inotropic effect of CGP 48506 was not sensitive to 10 mumol/l carbachol. The positive inotropic effect of CGP 48506 was accompanied by increases in time to peak tension and time of relaxation amounting to 175 +/- 4% and 205 +/- 15% of control, respectively, at 100 mumol/l. CGP 48506 but not CGP 48508 sensitized skinned trabeculae from failing human myocardium to calcium with an EC50 value of 10 mumol/l. However, CGP 48506 and CGP 48508 (up to 300 mumol/l) did not affect the activity of PDE isoenzymes I to IV from failing human myocardium. CGP 48506 is the first inotropic agent with calcium-sensitizing properties in the human heart that has been found to be devoid of inhibitory activity on human cardiac PDE isoenzymes. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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