التفاصيل البيبلوغرافية
| العنوان: |
Antiplatelet Effects of Selected Xanthine-Based Adenosine A2A and A2B Receptor Antagonists Determined in Rat Blood |
| المؤلفون: |
Monika Kubacka, Szczepan Mogilski, Marek Bednarski, Krzysztof Pociecha, Artur Świerczek, Noemi Nicosia, Jakub Schabikowski, Michał Załuski, Grażyna Chłoń-Rzepa, Jörg Hockemeyer, Christa E. Müller, Katarzyna Kieć-Kononowicz, Magdalena Kotańska |
| المصدر: |
International Journal of Molecular Sciences ; Volume 24 ; Issue 17 ; Pages: 13378 |
| بيانات النشر: |
Multidisciplinary Digital Publishing Institute |
| سنة النشر: |
2023 |
| المجموعة: |
MDPI Open Access Publishing |
| مصطلحات موضوعية: |
adenosine A 2A, A 2B receptors, A 2B receptor antagonists, anti-aggregation effect, antiplatelet activity, phosphodiesterase activity, lipid peroxidation |
| جغرافية الموضوع: |
agris |
| الوصف: |
The platelet aggregation inhibitory activity of selected xanthine-based adenosine A2A and A2B receptor antagonists was investigated, and attempts were made to explain the observed effects. The selective A2B receptor antagonist PSB-603 and the A2A receptor antagonist TB-42 inhibited platelet aggregation induced by collagen or ADP. In addition to adenosine receptor blockade, the compounds were found to act as moderately potent non-selective inhibitors of phosphodiesterases (PDEs). TB-42 showed the highest inhibitory activity against PDE3A along with moderate activity against PDE2A and PDE5A. The antiplatelet activity of PSB-603 and TB-42 may be due to inhibition of PDEs, which induces an increase in cAMP and/or cGMP concentrations in platelets. The xanthine-based adenosine receptor antagonists were found to be non-cytotoxic for platelets. Some of the compounds showed anti-oxidative properties reducing lipid peroxidation. These results may provide a basis for the future development of multi-target xanthine derivatives for the treatment of inflammation and atherosclerosis and the prevention of heart infarction and stroke. |
| نوع الوثيقة: |
text |
| وصف الملف: |
application/pdf |
| اللغة: |
English |
| Relation: |
Molecular Pathology, Diagnostics, and Therapeutics; https://dx.doi.org/10.3390/ijms241713378 |
| DOI: |
10.3390/ijms241713378 |
| الاتاحة: |
https://doi.org/10.3390/ijms241713378 |
| Rights: |
https://creativecommons.org/licenses/by/4.0/ |
| رقم الانضمام: |
edsbas.4020E15C |
| قاعدة البيانات: |
BASE |