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Antiplatelet Effects of Selected Xanthine-Based Adenosine A 2A and A 2B Receptor Antagonists Determined in Rat Blood.
- Source :
-
International journal of molecular sciences [Int J Mol Sci] 2023 Aug 29; Vol. 24 (17). Date of Electronic Publication: 2023 Aug 29. - Publication Year :
- 2023
-
Abstract
- The platelet aggregation inhibitory activity of selected xanthine-based adenosine A <subscript>2A</subscript> and A <subscript>2B</subscript> receptor antagonists was investigated, and attempts were made to explain the observed effects. The selective A <subscript>2B</subscript> receptor antagonist PSB-603 and the A <subscript>2A</subscript> 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.
- Subjects :
- Animals
Rats
Xanthine pharmacology
Adenosine
Blood Platelets
Atherosclerosis
Subjects
Details
- Language :
- English
- ISSN :
- 1422-0067
- Volume :
- 24
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- International journal of molecular sciences
- Publication Type :
- Academic Journal
- Accession number :
- 37686188
- Full Text :
- https://doi.org/10.3390/ijms241713378