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选定黄嘌呤类腺嘌呤 A 和 A 受体拮抗剂在大鼠血液中的抗血小板作用。

Antiplatelet Effects of Selected Xanthine-Based Adenosine A and A Receptor Antagonists Determined in Rat Blood.

机构信息

Department of Pharmacodynamics, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland.

Department of Pharmacological Screening, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland.

出版信息

Int J Mol Sci. 2023 Aug 29;24(17):13378. doi: 10.3390/ijms241713378.

DOI:10.3390/ijms241713378
PMID:37686188
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10487961/
Abstract

The platelet aggregation inhibitory activity of selected xanthine-based adenosine A and A receptor antagonists was investigated, and attempts were made to explain the observed effects. The selective A receptor antagonist PSB-603 and the A 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.

摘要

研究了几种黄嘌呤类腺嘌呤 A 和 A 受体拮抗剂对血小板聚集的抑制活性，并试图解释观察到的作用。选择性 A 受体拮抗剂 PSB-603 和 A 受体拮抗剂 TB-42 抑制胶原或 ADP 诱导的血小板聚集。除了阻断腺苷受体外，这些化合物还被发现具有中等强度的非选择性磷酸二酯酶（PDEs）抑制剂活性。TB-42 对 PDE3A 的抑制活性最高，对 PDE2A 和 PDE5A 也有中度活性。PSB-603 和 TB-42 的抗血小板活性可能是由于 PDE 抑制导致血小板中环磷酸腺苷（cAMP）和/或环磷酸鸟苷（cGMP）浓度增加所致。黄嘌呤类腺嘌呤受体拮抗剂对血小板无细胞毒性。一些化合物表现出抗氧化特性，可减少脂质过氧化。这些结果可能为未来开发用于治疗炎症和动脉粥样硬化以及预防心肌梗死和中风的多靶点黄嘌呤衍生物提供依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/79ee7405826b/ijms-24-13378-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/400c8a24f97a/ijms-24-13378-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/505e399d5aaf/ijms-24-13378-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/a8bcf0243035/ijms-24-13378-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/e10db555e961/ijms-24-13378-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/79ee7405826b/ijms-24-13378-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/400c8a24f97a/ijms-24-13378-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/48d15ea25e76/ijms-24-13378-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/fe87945213f8/ijms-24-13378-g003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/505e399d5aaf/ijms-24-13378-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/a8bcf0243035/ijms-24-13378-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/e10db555e961/ijms-24-13378-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfc/10487961/79ee7405826b/ijms-24-13378-g008.jpg

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