- 期刊
Effect of DC-015, a Novel Potent and Selective α1-Adrenoceptor Antagonist, Comparison with Prazosin on Noradrenaline-Induced Platelet Aggregation
並列摘要
The antiplatelet activity of DC-015, a newly synthesized quinazoline derivative was determined in human platelet-rich plasma. From the binding studies, the Ki values of DC-015 for α1-, α2- adrenoceptors and 5-HT1, 5-HT2 receptors were about 0.21(nM), 0.59(μM), 0.16(μM) and 0.38(μM), respectivity. On the otherhand, the Ki values of prazosin for α1- and α2-adrenoceptors were about 0.19(nM) and 4.8(μM), respectivity. Experimental results indicated that DC-015 dose-dependently inhibited noradrenaline (10μM)-induced platelet aggregation in human platelet-rich plasma. At 20μM, DC-015 would completely inhibit platelet aggregation induced by noradrenaline. A high concentration of prazosin (＞30mM) caused sligh inhibition of aggregation. Furthermore, DC-015 (2μM) significantly increased the cyclic AMP level in human platelet-rich plasma, whereas, prazosin significantly increased cyclic AMP level only at higher concentrations (100μM). We can conclude that DC-015 inhibited noradrenaline-induced platelet aggregation mainly through binding to cc2-receptor on platelets, resulting in inhibiting platelet aggregation.
被引用紀錄
延伸閱讀
- Barbero, A. R., Bosque, E., Cabanero, L. R., Arevalo, M., & Novoa, J. L. (1992). Effect of platelet activating factor antagonist treatment on gentamicin nephrotoxicity. Mediators of Inflammation, 1992(), 23-26. https://doi.org/10.1155/S096293519200005X
- Yuwen, H. (2014). Effect of LXR Agonist on Migration, Invasion, and Progression of Androgen-Independent PC3 and DU-145 Human Prostate Cancer Cells [master's thesis, National Tsing Hua University]. Airiti Library. https://www.airitilibrary.com/Article/Detail?DocID=U0016-2912201413495866
- Wu, C. H., Cheng, S. M., Chu, K. M., Yang, S. P., Lai, J. H., & Cheng, C. C. (2009). Pioglitazone, a PPAR-γ Agonist, Downregulates Cytokine Production and AP-1 DNA-Binding Protein in Human Peripheral Blood T Cells-Potential Implication in the Treatment of Atherosclerotic Disease. Acta Cardiologica Sinica, 25(3), 127-133. https://www.airitilibrary.com/Article/Detail?DocID=10116842-200909-25-3-127-133-a
- 劉滿海（2010）。The Protective Effects of Phytoestrogen (Coumestrol and Daidzein) against Amyloid-??-peptide and LPS-induced Toxicity on Mice Astrocyte Cells〔博士論文，臺北醫學大學〕。華藝線上圖書館。https://doi.org/10.6831/TMU.2010.00114
- 賴瑩純（2011）。To Determine the Effect of Rosiglitazone on Acid Labile Subunit Expression in Adipocyte and Type 2 Diabetes Patients after Activation of Peroxisome Proliferator-Activated Receptor-γ〔碩士論文，國立臺灣大學〕。華藝線上圖書館。https://doi.org/10.6342/NTU.2011.10296