Platelet GPIIb/IIIa receptor occupancy studies using a novel fluoresceinated cyclic Arg-Gly-Asp peptide.


:DMP 728 is a potent and specific platelet GPIIb/IIIa antagonist. Like all GPIIb/IIIa antagonists, DMP 728 has a steep dose-response relationship in inhibiting platelet aggregation. In this study the relationships between receptor occupancy, platelet aggregation and bleeding time was determined in anesthetized dogs after intravenous infusion of DMP 728 (0.01 and 0.1 mg/kg/2h). Receptor occupancy was determined by flow cytometry using XL086, a novel fluorescent cyclic RGD peptide that binds to GPIIb/IIIa with high specificity and affinity (kd approximately 55 nM). Mean number of GPIIb/IIIa as determined by flow cytometric assay was approximately 53,8000 and 79,000 on unactivated and ADP-activated platelets respectively. After DMP 728 intravenous infusion, there was a dose- and time-dependent increase in receptor occupancy, inhibition of platelet aggregation and bleeding time. The two methods of receptor occupancy determination correlate with each other with an r2 = 0.78. The present data suggest that blockade of only 40-60% (approximately 40,000 receptors) of the total platelet GPIIb/IIIa was required to achieve > 90% inhibition of platelet aggregation and > 15 min bleeding time. Our results showed the potential clinical utility of this approach in the study of GPIIb/IIIa dose-response relationship.


Thromb Res


Thrombosis research


Tsao PW,Bozarth JM,Jackson SA,Forsythe MS,Flint SK,Mousa SA




Has Abstract


1995-03-15 00:00:00














  • Diagnosis of pulmonary embolism.

    abstract::Pulmonary embolism (PE) is a common, lethal yet treatable disease. The clinical diagnosis of PE remains to be a problem due to the nonspecific presenting signs, symptoms, electrocardiographic findings, arterial blood gas abnormalities and chest X-ray changes. Despite these nonspecific clinical findings, clinicians are...

    journal_title:Thrombosis research

    pub_type: 杂志文章,评审


    authors: Rodger M,Wells PS

    更新日期:2001-09-15 00:00:00

  • Measuring functional limitations after venous thromboembolism: Optimization of the Post-VTE Functional Status (PVFS) Scale.

    abstract:INTRODUCTION:We recently proposed a scale for assessment of patient-relevant functional limitations following an episode of venous thromboembolism (VTE). Further development of this post-VTE functional status (PVFS) scale is still needed. METHODS:Guided by the input of VTE experts and patients, we refined the PVFS sca...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Boon GJAM,Barco S,Bertoletti L,Ghanima W,Huisman MV,Kahn SR,Noble S,Prandoni P,Rosovsky RP,Sista AK,Siegerink B,Klok FA

    更新日期:2020-06-01 00:00:00

  • Increased number of circulating endothelial cells and plasma markers of endothelial damage in chronic cocaine users.

    abstract:BACKGROUND:Cocaine use has been related with the development of accelerated atherosclerosis and with an increased risk of cardiac and cerebrovascular events, such as myocardial infarction, sudden cardiac death, and ischemic stroke. The underlying mechanisms leading to these complications are not fully understood, altho...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Sáez CG,Olivares P,Pallavicini J,Panes O,Moreno N,Massardo T,Mezzano D,Pereira J

    更新日期:2011-10-01 00:00:00

  • Variations of protein C in uremic hemodialysed patients.

    abstract::Protein C has been measured by three different assays (antigenic, amidolytic and chronometric) in 27 end-stage renal insufficient patients before and after hemodialysis. Protein C levels have been compared with other coagulation inhibitors (antithrombin III, protein S) and fibrinolytic parameters. Baseline anticoagula...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Nguyen P,Toupance O,Chanard J,Potron G

    更新日期:1993-03-15 00:00:00

  • Frequency of use and acceptability of clinical prediction rules for pulmonary embolism among Swiss general internal medicine residents.

    abstract:INTRODUCTION:Whether clinical prediction rules for pulmonary embolism are accepted and used among general internal medicine residents remains uncertain. We therefore evaluated the frequency of use and acceptability of the Revised Geneva Score (RGS) and the Pulmonary Embolism Severity Index (PESI), and explored which fa...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Faller N,Stalder O,Limacher A,Bassetti S,Beer JH,Genné D,Battegay E,Hayoz D,Leuppi J,Mueller B,Perrier A,Waeber G,Rodondi N,Aujesky D

    更新日期:2017-12-01 00:00:00

  • Immunohistochemical localization of plasminogen activators in human saphenous veins.

    abstract::Human saphenous veins were analyzed for presence of plasminogen activators (t-PA) in the endothelium of the vessel walls by immunohistochemical techniques. We used a polyclonal rabbit antihuman t-PA antibody, a monoclonal mouse-antihuman t-PA and a goat antibody to low molecular weight urokinase. To demonstrate presen...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Risberg B,Eriksson E,Björk S,Hansson GK

    更新日期:1986-02-01 00:00:00

  • Alloxan-induced hyperglycemia in rabbits and the response of platelets to aggregating agents in vitro and to exposed subendothelium in vivo.

    abstract::Many patients with diabetes mellitus show increased platelet aggregation and prostaglandin synthesis in response to physiological agents such as ADP and collagen when their platelets are tested in platelet-rich plasma or washed platelet suspensions. However, the relationship between increased platelet aggregation in v...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Ingerman-Wojenski CM,Smith M,Silver MJ

    更新日期:1987-06-01 00:00:00

  • PO-01 - Congestive heart failure is an independent risk factor for venous thromboembolism and mortality in cancer patients.

    abstract:INTRODUCTION:Prediction of venous thromboembolism (VTE) occurrence in cancer patients using individual risk factors may contribute to preventing the burden of disease associated with VTE. Congestive heart failure in patients with cancer may increase the risk of VTE and worsen the prognosis. AIM:We sought to investigat...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Königsbrügge O,Riedl J,Grilz E,Wiltschke C,Zielinski C,Pabinger I,Ay C

    更新日期:2016-04-01 00:00:00

  • Clinical factors associated with inappropriate prophylaxis of venous thromboembolic disease in critically ill patients. A single day cross-sectional study.

    abstract:PURPOSE:A poor implementation of VTE prophylactic measures recommended for critically ill patients has been observed in several epidemiological studies. The clinical factors associated with this have not been clearly established. The objective of our study was to identify which factors could be related to the inappropr...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: García-Olivares P,Guerrero JE,Keough E,Galdos P,Carriedo D,Murillo F,Rivera A,PROF-ETEV study investigators.

    更新日期:2016-07-01 00:00:00

  • Clinical relevance of pulmonary infarction in patients with pulmonary embolism.

    abstract:INTRODUCTION:Data regarding the clinical relevance of pulmonary infarction (PI) in patients with pulmonary embolism (PE) are lacking. The aim of this study was to investigate the clinical features of PE patients with PI and the prognostic role of PI for PE patients. MATERIALS AND METHODS:Based on computed tomography s...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Cha SI,Shin KM,Lee J,Hwangbo Y,Yoo SS,Lee J,Lee SY,Kim CH,Park JY,Jung TH

    更新日期:2012-09-01 00:00:00

  • Increased fibrinolytic activity after surgery induced by low dose heparin.

    abstract::Forty women undergoing surgery under general anaesthesia for hyperplasia mammae were randomized to treatment with low dose heparin (5000 IU twice daily) or not. Preoperatively, and repeated on the 3. postoperative day, assays of euglobulin clot lysis time (ELT) after venous stasis, tissue plasminogen activator (t-PA) ...

    journal_title:Thrombosis research

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Arnesen H,Engebretsen LF,Ugland OM,Seljeflot I,Kierulf P

    更新日期:1987-03-01 00:00:00

  • Antithrombin III in renal transplant recipients.

    abstract::Antithrombin III (AT III) is increased in situations where there is increased platelet turnover. Plasma AT III levels measured in 39 renal transplant recipients were significantly higher than in 20 healthy subjects (p less than 0.001) and 20 patient controls (p less than 0.025). AT III levels were significantly correl...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Woo KT,Lee EJ,Lau YK,Lim CH

    更新日期:1985-05-01 00:00:00

  • Inhibition of platelet aggregation and endogenous lectin activity by oligoamines.

    abstract::Amino sugars and basic amino acids inhibit platelet aggregation and the activity of the endogenous platelet lectin, yet, relatively high concentrations (approximately 30 mM) are required for the inhibition. If cooperative interactions are involved in these platelet surface activities, oligomers of primary amines shoul...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Agam G,Gartner TK,Livne A

    更新日期:1984-02-01 00:00:00

  • Protective activity of defibrotide against lethal acute myocardial ischemia in the cat.

    abstract::Defibrotide (D) is a natural polydeoxyribonucleotide from mammalian lungs with profibrinolytic and antithrombotic activities. D also has PGI2-stimulating and tissue plasminogen activator (TPA)-releasing activities, but has no anticoagulant properties. The protective effects of D were demonstrated very recently in a mo...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Niada R,Porta R,Pescador R,Mantovani M,Prino G

    更新日期:1986-05-01 00:00:00

  • Immunopurification of an S-antigen-like protein from human platelets.

    abstract::S-antigen (also named arrestin or 48K protein) is a protein abundant in photoreceptor cells of vertebrates and invertebrates. The presently known function of this protein in retina is to arrest the enzymatic cascade of phototransduction in retinal rods, through its binding to photoactivated and phosphorylated rhodopsi...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Mirshahi M,Razaghi A,Mirshahi SS,Van Tuyen V,Faure JP

    更新日期:1991-12-01 00:00:00

  • Development of an ELISA for the quantification of fibrin in canine tumours.

    abstract::Fibrin is found in most solid tumours, and there is speculation regarding its role in tumour invasion and metastasis. An assay to quantitate fibrin levels in tissues would be a useful preliminary tool in assessing the above. Such an assay to quantitatively detect levels of fibrin in various types of canine tumour was ...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Raut S,McEvoy F,Gaffney PJ

    更新日期:1999-10-01 00:00:00

  • Effect of aspirin and clopidogrel on platelet-dependent tissue factor expression in endothelial cells.

    abstract::Tissue factor is an ubiquitous membrane-anchored glycoprotein that initiates blood coagulation by forming a complex with circulating factors VII and VIIa. Under normal circumstances, endothelial cells do not express tissue factor but, in some pathological situations, when the endothelium or the monocytes are exposed t...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Savi P,Bernat A,Dumas A,Aït-Chek L,Herbert JM

    更新日期:1994-01-15 00:00:00

  • Compression inhibits aggregation of human platelets under high hydraulic pressure.

    abstract::It has been found in our laboratory that compression induces disaggregation and decompression induces aggregation of human platelets. The experimental design was based on the premise that oppositely charged amino acid residues of fibrinogen are juxtaposed in the specific adhesive site(s). This can be explained by the ...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Murayama M

    更新日期:1987-03-15 00:00:00

  • The action of thrombin on peptide p-nitroanilide substrates: hydrolysis of Tos-Gly-Pro-Arg-pNA and D-Phe-Pip-Arg-pNA by human alpha and gamma and bovine alpha and beta-thrombins.

    abstract::Human and bovine alpha-thrombins (greater than 90% alpha form) with high fibrinogen clotting activities (approximately 3,000 U.S. units/mg protein) exhibit similar Michaelis menten kinetics with the p-nitroanilide tripeptide substrates Tos-Gly-Pro-arg-pNA (Chromozym-TH) and D-Phe-Pip-Arg-pNA (S-2238). The kinetic para...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Lottenberg R,Hall JA,Fenton JW 2nd,Jackson CM

    更新日期:1982-11-01 00:00:00

  • Long-term erythropoietin therapy does not affect endothelial markers, coagulation activation and oxidative stress in haemodialyzed patients.

    abstract:INTRODUCTION:Although the general improvement caused by recombinant human erythropoietin (rHuEPO) in the correction of uraemic anaemia cannot be questioned, some data suggest that the changes in the haemostasis, endothelial function and oxidative stress (SOX) are induced. The aim of the present study was to investigate...

    journal_title:Thrombosis research

    pub_type: 临床试验,杂志文章


    authors: Pawlak K,Pawlak D,Mysliwiec M

    更新日期:2007-01-01 00:00:00

  • Reductions in tissue plasminogen activator and thrombomodulin in blood draining veins damaged by venous access devices.

    abstract::A frequent complication of venous access devices (VADs) is axillary-subclavian venous thrombosis. To study this problem we have compared blood drawn through VADs with peripheral blood samples in a group of oncology patients with venographically demonstrated venous damage (N = 14) and a group with normal venograms (N =...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Horne MK 3rd,Merryman PK,Mayo DJ,Gralnick HR,Chang RC,Alexander HR

    更新日期:1995-08-15 00:00:00

  • Incidence and risk factors of subclinical umbilical catheter-related thrombosis in neonates.

    abstract:INTRODUCTION:This study aimed to determine the risk factors for subclinical umbilical catheter-related thrombosis (UCRT) and its association with clinical morbidities. MATERIALS AND METHODS:In infants without any symptoms associated with umbilical catheterization, the presence of thrombosis was monitored using abdomin...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Hwang JH,Chung ML,Lim YJ

    更新日期:2020-10-01 00:00:00

  • Noninvasive transcutaneous ultrasound augments thrombolysis in the left circumflex coronary artery--an in vivo canine study.

    abstract:BACKGROUND:Ultrasound has the potential to augment chemical thrombolysis. METHODS AND RESULTS:Thrombotic occlusions in the left circumflex artery (LCx) were induced in 27 dogs. Sixty minutes later, tissue-type plasminogen activator (t-PA) was given intravenously over 90 min. Thrombotic occlusions (n = 20) were treated...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Jeon DS,Luo H,Fishbein MC,Miyamoto T,Horzewski M,Iwami T,Mirocha JM,Ikeno F,Honda Y,Siegel RJ

    更新日期:2003-05-01 00:00:00

  • Study on pharmacokinetics of radioactive labelled defibrotide after oral or intravenous administration in rats.

    abstract::Defibrotide (D) was labelled with 125I or with 32P. The radiolabelled compounds ([125I]-Defibrotide ([125I]-D), [32P]-Defibrotide ([32P]-D) retained the same profibrinolytic activity, in vitro, as the parent drug, suggesting that the labelling procedures had not modified the pharmacological properties of D and hence t...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Fisher J,Holland TK,Pescador R,Porta R,Ferro L

    更新日期:1996-01-01 00:00:00

  • Role of red cells in preventing the growth of platelet aggregation.

    abstract::Using high-resolution real-time two-dimensional ultrasound, we have investigated the role of red cells in the growth of already established platelet aggregates under controlled flow conditions. Platelet rich plasma (PRP) was circulated in vitro in horizontally and vertically arranged tubing at mean shear rate ranging ...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Machi J,Sigel B,Ramos JR,Justin JR,Feinberg H,LeBreton GC,Robertson AL Jr

    更新日期:1984-10-01 00:00:00

  • Next-generation DNA sequencing to identify novel genetic risk factors for cerebral vein thrombosis.

    abstract:BACKGROUND:Cerebral vein thrombosis (CVT) is a rare, life-threatening disease affecting one adult per 100,000 per year. Genetic risk factors are deficiencies of the natural anticoagulant proteins antithrombin, protein C, protein S or single nucleotide polymorphisms such as factor V Leiden and prothrombin 20210A. In 20%...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Gorski MM,de Haan HG,Mancini I,Lotta LA,Bucciarelli P,Passamonti SM,Cairo A,Pappalardo E,van Hylckama Vlieg A,Martinelli I,Rosendaal FR,Peyvandi F

    更新日期:2018-09-01 00:00:00

  • D-dimer specific monoclonal antibodies react with fibrinogen aggregates.

    abstract::Human fibrinogen exposed to 46.5 degrees C was subjected to gel permeation chromatography. The protein eluted in two distinct peaks. The first peak appeared in the void volume containing soluble fibrinogen aggregates, while the other peak represented monomeric fibrinogen. In contrast to the monomeric peak material, th...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Bennick A,Haddeland U,Brosstad F

    更新日期:1996-04-15 00:00:00

  • Use of antifibrinolytic therapy to reduce transfusion in patients undergoing orthopedic surgery: a systematic review of randomized trials.

    abstract:BACKGROUND:Minimizing bleeding and transfusion is desirable given its cost, complexity and potential for adverse events. Concerns have been heightened by recent data demonstrating that bleeding events may predict worse outcomes and by warnings about the safety of erythropoietic stimulating agents. Prior small studies s...

    journal_title:Thrombosis research

    pub_type: 杂志文章,meta分析,评审


    authors: Kagoma YK,Crowther MA,Douketis J,Bhandari M,Eikelboom J,Lim W

    更新日期:2009-03-01 00:00:00

  • Murine models of vascular endothelial injury: Techniques and pathophysiology.

    abstract::Vascular endothelial injury (VEI) triggers pathological processes in various cardiovascular diseases, such as coronary heart disease and hypertension. To further elucidate the in vivo pathological mechanisms of VEI, many animal models have been established. For the easiness of genetic manipulation and feeding, murine ...

    journal_title:Thrombosis research

    pub_type: 杂志文章,评审


    authors: Wu Y,Su SA,Xie Y,Shen J,Zhu W,Xiang M

    更新日期:2018-09-01 00:00:00

  • "HERDOO2" clinical decision rule to guide duration of anticoagulation in women with unprovoked venous thromboembolism. Can I use any d-Dimer?

    abstract:BACKGROUND:The "HERDOO2 rule" is a prospectively validated clinical decision rule used to identify low-risk women who can safely discontinue anticoagulants after completing 5-12 months of anticoagulant treatment for unprovoked venous thromboembolism. The VIDAS®d-Dimer (DD) assay, a component of the rule, was used in th...

    journal_title:Thrombosis research

    pub_type: 杂志文章


    authors: Rodger MA,Le Gal G,Langlois NJ,Gin B,Mallick R,Giulivi A,Freedman M,Kovacs MJ,REVERSE II investigators.

    更新日期:2018-09-01 00:00:00