Platelet Inhibitors

Shifrin, Megan M.; Widmar, S. Brian

doi:10.1016/j.cnur.2015.10.004

Cited by 10 publications

(6 citation statements)

References 21 publications

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“…At least two separate receptors on platelet cell membranes, GpIb-V-IX complex and GpVI, function to tether the platelet and initiate cellular activation, simultaneously. Once the platelets have adhered to the damaged vascular endothelium, they recruit additional platelets from the circulation to augment the fragile platelet monolayer and eventually form a stable plug (23). Following platelet activation, a coordinated series of events is triggered, including a rapid conformational change and the secretion of α,δ-granules and other intracellular vesicles, including lysosomes, which provide a positive feedback signal during platelet activation (19).…”

Section: Discussionmentioning

confidence: 99%

Inhibitory effects of luteolin‑4'‑O‑β‑D‑glucopyranoside on P2Y12 and thromboxaneï¿½A2 receptor‑mediated amplification of platelet activation inï¿½vitro

Zhu

et al. 2018

Int J Mol Med

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Platelet activation and subsequent accumulation at sites of vascular injury are central to thrombus formation, which is considered to be a trigger of several cardiovascular diseases. Callicarpa nudiflora (C. nudiflora) Hook is a traditional Chinese medicinal herb for promoting blood circulation by removing blood stasis. In our previous study, several compounds extracted from this herb, including luteolin‑4'‑O‑β‑D‑glucopyranoside (LGP), were revealed to exert inhibitory effects on adenosine diphosphate (ADP)‑induced platelet aggregation. The aim of present study was to confirm these antiplatelet effects and elucidate the potential mechanisms. Using a platelet‑aggregation assay, it was revealed that LGP significantly inhibited platelet aggregation induced by ADP, U46619 and arachidonic acid. It was also found that LGP exhibited marked inhibitory effects on the activation of αIIbβ3 integrin, the secretion of serotonin from granules, and the synthesis of thromboxane A2. In addition, the results showed that LGP suppressed Ras homolog family member A and phosphoinositide 3‑kinase/Akt/glycogen synthase kinase 3β signal transduction. Data from a radiolabeled ligand‑binding assay indicated that LGP exhibited apparent competing effects on thromboxane receptor (TP) and P2Y12 receptors. In conclusion, the data presented here demonstrated that LGP, a natural compound from C. nudiflora Hook, inhibited the development of platelet aggregation and amplification of platelet activation. These inhibitory effects may be associated with its dual‑receptor inhibition on P2Y12 and TP receptors.

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Section: Discussionmentioning

confidence: 99%

Inhibitory effects of luteolin‑4'‑O‑β‑D‑glucopyranoside on P2Y12 and thromboxaneï¿½A2 receptor‑mediated amplification of platelet activation inï¿½vitro

Zhu

et al. 2018

Int J Mol Med

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“…Acute coronary syndrome (ACS) is a common disease prevalent worldwide, and although its lethality has declined in the last 30 years, it remains the leading cause of human death with high morbidity and mortality ( Chan et al, 2016 ; Bergmark et al, 2022 ). The main treatment for ACS is antiplatelet coagulation ( Shifrin and Widmar, 2016 ; Tsoumani et al, 2016 ; Szarpak et al, 2022 ). Ticagrelor, currently the most commonly used antiplatelet coagulation inhibitor, is widely employed in ACS treatment ( Kabil et al, 2022 ; Tao et al, 2022 ).…”

Section: Introductionmentioning

confidence: 99%

Fluorescence quenching-based immunological probe for ticagrelor monitoring

Zhang,

Cheng,

Gao

et al. 2023

Front. Bioeng. Biotechnol.

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Introduction: Ticagrelor is extensively utilized for the treatment of acute coronary syndromes (ACS), but its platelet aggregation inhibitory effects can potentially result in tissue bleeding, posing a serious risk to patients’ lives.Methods: In this study, we developed highly sensitive full length anti-ticagrelor Quenchbodies (Q-bodies) for fast monitoring of ticagrelor both in solution and serum for the first time. Ticagrelor coupled with N- hydroxysuccinimide (Ticagrelor-NHS) ester was also designed and synthesized for interaction and biological activity detection.Results: Both ATTO-labeled MEDI2452 (2452A) Q-body and TAMRA-labeled IgG 152 (152T) Q-body demonstrated efficient detection of ticagrelor and its active metabolite (TAM). The 2452A Q-body exhibited a broader detection range, while the 152T Q-body displayed a lower limit of detection (LOD). Under physiological conditions (Ticagrelor:TAM, 3:1), the concentration of ticagrelor was further measured, yielding LOD values of 4.65 pg/mL and 2.75 pg/mL for the two Q-bodies, with half-maximal effect concentrations of 8.15 ng/mL and 3.0 ng/mL, respectively.Discussion: Compared with traditional liquid chromatography-mass spectrometry (LC-MS) methods, anti-ticagrelor Q-bodies have higher sensitivity and detection speed. It enabled the completion of analysis within 3 min, facilitating rapid preoperative detection of blood drug concentration in ACS to determine the feasibility of surgery and mitigate the risk of intraoperative and postoperative hemorrhage. The swift detection of ticagrelor holds promise for enhancing individualized drug administration, preventing adverse reactions, and providing preoperative guidance.

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“…Clopidogrel is a potent antiplatelet agent widely used to prevent coronary artery diseases and treat vascular thrombosis [13,14]. Its antiplatelet activity results from selective inhibition of ADP binding to the platelet receptor preventing ADP-mediated platelet responses [15,16]. Therefore, Clopidogrel should be used with caution in patients receiving other drugs that increase bleeding risk include anticoagulants, other antiplatelet, and NSAIDs [17].…”

Section: Introductionmentioning

confidence: 99%

Bioanalytical Rp-HPLC Method Development and Validation of Clopidogrel Bisulfate in Wistar Rat Plasma and Its Application to Pharmacokinetic Study

2022

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Objective: A novel, simple, precise, accurate, sensitive, and reproducible HPLC method for determining clopidogrel bisulfate in Wistar rat plasma was developed and validated. Methods: The chromatographic separation was performed using Xterra C18 (250 x 4.6 mm, 5μ) column. Mobile phase composed of Acetonitrile ACN: 0.05M potassium dihydrogen orthophosphate buffer pH 4.2 and in the ratio of 75:25% v/v at a flow rate of 1.2 ml/min. Detection was carried out using a PDA detector at 220 nm. The bioanalytical clopidogrel method was validated as per ICH guidelines. Results: The selected chromatographic condition was found to efficiently separate clopidogrel bisulfate (RT-2.838 min). The calibration curve was linear over the concentration range 40-200 ng/ml in Wistar rat plasma with a correlation coefficient of 0.999, respectively. The precision study revealed that the cumulative percentage variation was within the acceptable limit, and accuracy research showed the value of mean percent recovery between 99.72-99.83 %. Conclusion: A simple, rapid, specific, accurate, and precise analytical method was developed and validated using Wistar rat plasma. The technique was strictly validated according to the ICH guidelines. Acquired results demonstrate that the proposed strategy can be effortlessly and advantageously applied for routine analysis of clopidogrel in the Wistar rat plasma.

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Platelet Inhibitors

Cited by 10 publications

References 21 publications

Inhibitory effects of luteolin‑4'‑O‑β‑D‑glucopyranoside on P2Y12 and thromboxaneï¿½A2 receptor‑mediated amplification of platelet activation inï¿½vitro

Inhibitory effects of luteolin‑4'‑O‑β‑D‑glucopyranoside on P2Y12 and thromboxaneï¿½A2 receptor‑mediated amplification of platelet activation inï¿½vitro

Fluorescence quenching-based immunological probe for ticagrelor monitoring

Bioanalytical Rp-HPLC Method Development and Validation of Clopidogrel Bisulfate in Wistar Rat Plasma and Its Application to Pharmacokinetic Study

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