| Autor: |
Veselkina OC, Petrishchev NN, Vasina LV, Borovitov ME, Seliutin AV, Chepanov SV, Sel'kov SA |
| Jazyk: |
ruština |
| Zdroj: |
Eksperimental'naia i klinicheskaia farmakologiia [Eksp Klin Farmakol] 2014; Vol. 77 (8), pp. 28-33. |
| Abstrakt: |
We have studied the influence of new N,N'-substituted piperazines with variable nature of the linker between piperazine and aromatic cycles (carbonyl group in VR-0411 versus sulfonyl group in VR-0511) on thrombin-induced platelet aggregation, cytoplasmic Ca2+ mobilization in platelets, and P-selectin exposure on the platelet plasma membrane. The inhibitory effect of VR-0511 on platelet aggregation exceeds the effects of the reference compound aspirin and VR-0411 by 35 and 42%, respectively (p < or = 0.01). The effects of test compounds on the mobilization of cytoplasmic Ca2+ in platelets and P-selectin exposure indicate that VR-0411 and VR-0511 inhibit platelet activation in these tests by 28 and 61%, (p < or = 0.01) and 34 and 58% (p < or = 0.01), respectively. The possible targets for VR-0411 and VR-0511 are thromboxane and inositol triphosphate-dependent (IP3 formation) pathways of activation signal transfer. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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