The P2Y12 receptor as a therapeutic target in cardiovascular disease

Platelets

Volumn 12, Issue 4, 2001, Pages 197-209

  Storey, R F ^a  

^a QUEEN S MEDICAL CENTRE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ABCIXIMAB; ACETYLSALICYLIC ACID; ADENOSINE TRIPHOSPHATE DERIVATIVE; ANTITHROMBOCYTIC AGENT; CANGRELOR; CLOPIDOGREL; FIBRINOGEN RECEPTOR ANTAGONIST; IOPAMIDOL; PURINE ANTAGONIST; PURINE P2Y RECEPTOR; PYRIDINE DERIVATIVE; RECEPTOR SUBTYPE; THIENOPYRIDINE DERIVATIVE; TICLOPIDINE; UNCLASSIFIED DRUG; MEMBRANE PROTEIN; P2RY12 PROTEIN, HUMAN; PURINE P2 RECEPTOR; PURINE P2Y12 RECEPTOR;

CARDIOVASCULAR DISEASE; CLINICAL TRIAL; CORONARY ARTERY THROMBOSIS; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG SAFETY; DRUG TARGETING; DRUG TOLERABILITY; HUMAN; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; REVIEW; THROMBOCYTE ACTIVATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOCYTE RELEASE REACTION; ANIMAL; DRUG ANTAGONISM; DRUG EFFECT; PATHOPHYSIOLOGY; PHYSIOLOGY; SIGNAL TRANSDUCTION; THROMBOCYTE;

THROMBUS;

ANIMALS; BLOOD PLATELETS; CARDIOVASCULAR DISEASES; HUMANS; MEMBRANE PROTEINS; PLATELET ACTIVATION; PLATELET AGGREGATION INHIBITORS; RECEPTORS, PURINERGIC P2; SIGNAL TRANSDUCTION;

EID: 0034954596     PISSN: 09537104     EISSN: None     Source Type: Journal    
DOI: 10.1080/09537100120058739     Document Type: Review

References (156)

1. Thrombosis and acute coronary-artery lesions in sudden cardiac ischemic death
2. Pathophysiology and clinical recognition
3. Overview of haemostasis
4. Release of prostaglandins and thromboxane into the coronary circulation in patients with ischemic heart disease
5. Platelet activation in unstable coronary disease
6. Biochemical evidence of platelet activation in patients with persistent unstable angina
7. Comparative arterial antithrombotic activity of clopidogrel and acetylsalicylic acid in the pig
8. Antithrombotic effects of MK-0852, a platelet fibrinogen receptor antagonist, in canine models of thrombosis
9. Antithrombotic activity of SR 46349, a novel, potent and selective 5-HT2 receptor antagonist
10. 2T receptor: A novel approach to antithrombotic therapy
11. Mode of action of aspirin-like drugs
12. Platelet aggregation and thromboxane release induced by arachidonic acid, collagen, ADP and platelet-activating factor following low dose acetylsalicylic acid in man
13. Persistent inhibition of platelet function during long-term treatment with 75mg acetylsalicylic acid daily in men with unstable coronary artery disease
14. Factors responsible for ADP-induced release reaction of human platelets
15. Adenosine diphosphate-induced platelet aggregation and release reaction in heparinized platelet rich plasma and the influence of added citrate
16. The effects of citrate and extracellular calcium ions on the platelet release reaction induced by adenosine diphosphate and collagen
17. Dependence of human platelet functional responses on divalent cations: Aggregation and secretion in heparin- and hirudin-anticoagulated platelet-rich plasma and the effects of chelating agents
18. 2+ in the suspending medium on the responses of human and rabbit platelets to aggregating agents
19. Aspirin does not inhibit adenosine diphosphate-induced platelet alpha-granule release
20. Aspirin does not affect the flow cytometric detection of fibrinogen binding to, or release of alpha-granules or lysosomes from, human platelets
21. 2T receptor in amplification of human platelet activation, aggregation, secretion and procoagulant activity
22. Collaborative overview of randomised trials of antiplatelet therapy. I: Prevention of death, myocardial infarction and stroke by prolonged antiplatelet therapy in various categories of patients
23. Marked platelet activation in vivo after intravenous streptokinase in patients with acute myocardial infarction
24. 2 modulate the response to tissue-type plasminogen activator
25. Coronary reocclusion following therapeutic thrombolysis: Prevention by thromboxane antagonism and thrombin inhibition
26. Randomised trial of intravenous streptokinase, oral aspirin, both, or neither among 17,187 cases of suspected acute myocardial infarction: ISIS-2
27. Protective effects of aspirin against acute myocardial infarction and death in men with unstable angina: Results of a Veterans Administration Cooperative Study
28. Aspirin, sulfinpyrazone, or both in unstable angina. Results of a Canadian multicenter trial
29. Aspirin, heparin, or both to treat acute unstable angina
30. Aspirin (75 mg/day) after an episode of unstable coronary artery disease: Long-term effects on the risk of myocardial infarction, occurrence of severe angina and the need for revascularization
31. Aspirin in the primary prevention of angina pectoris in a randomised trial of United States physicians
32. Low-dose aspirin therapy for chronic stable angina: A randomised, placebo-controlled clinical trial
33. Double-blind trial of aspirin in primary prevention of myocardial infarction in patients with stable chronic angina pectoris
34. Functional characterization of platelet ADP receptors
35. Identification of the platelet ADP receptor targeted by antithrombotic drugs
36. Molecular basis for ADP-induced platelet activation: I. Evidence for three distinct ADP receptors on human platelets
37. 1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets
38. Coactivation of two different G protein-coupled receptors is essential for ADP-induced platelet aggregation
39. 1 receptor null mice
40. 1 receptor is necessary for adenosine-5′-diphosphate-induced platelet aggregation
41. The roles of P2X1 and P2TAC receptors in ADP-evoked calcium signalling in human platelets
42. 1 receptor, and is this mediated by a fall in basal cAMP
43. Ticlopidine selectively inhibits human platelet responses to adenosine diphosphate
44. Mechanisms of platelet aggregation
45. Effects of ticlopidine administered to healthy volunteers on platelet function in whole blood
46. A key role of adenosine diphosphate in the irreversible platelet aggregation induced by the PAR-1 activating peptide through the late activation of phosphoinositide 3-kinase
47. Deficiency of (33P)2MeS-ADP binding sites on platelets with secretion defect, normal granule stores and normal thromboxane A2 production: Evidence that ADP potentiates platelet secretion independently of the formation of large platelet aggregates and thromboxane A2 production
48. 1 receptor is normal in a patient presenting a severe deficiency of ADP-induced platelet aggregation: Further evidence for a distinct P2 receptor responsible for adenylyl cyclase inhibition
49. Molecular mechanism of thromboxane A(2)-induced platelet aggregation. Essential role for P2T(ac) and alpha(2a) receptors
50. 1 ADP receptor in the phosphatidylserine exposure of activated platelets
51. Inhibition of thrombin induced aggregation of human platelets by heparin
52. The platelet aggregating effect of eight commercial heparins
53. On the mechanism of platelet aggregation induced by heparin, protamine and polybrene
54. The potentiation of platelet aggregation and adhesion by heparin in vitro and in vivo
55. Platelet aggregation following heparin and protamine administration
56. 2 production
57. Effect of heparin and heparin fractions on platelet aggregation
58. Heparin counteracts the antiaggregating effect of prostacyclin by potentiating platelet aggregation
59. Heparin and low molecular weight heparin but not hirudin stimulate platelet aggregation in whole blood from acetylsalicylic acid treated healthy volunteers
60. Platelet activation with unfractionated heparin at therapeutic concentrations and comparisons with a low-molecular-weight heparin and with a direct thrombin inhibitor
61. 1 receptor pathways
62. Differential effects of three radiographic contrast media on platelet aggregation and degranulation: Implications for clinical practice?
63. 1 and P2cyc receptors
64. Thromboregulation by endothelial cells: Significance for occlusive vascular diseases
65. Effects of ticlopidine, a new platelet aggregation inhibitor in man
66. The basic pharmacology of ticlopidine and clopidogrel
67. Broad spectrum anti-platelet activity of ticlopidine and PCR 4099 involves the suppression of the effects of released ADP
68. 1
69. Ticlopidine and clopidogrel (SR 25990C) selectively neutralize ADP inhibition of PGE1-activated platelet adenylate cyclase in rats and rabbits
70. Clopidogrel inhibits the binding of ADP analogues to the receptor mediating inhibition of platelet adenylate cyclase
71. The antiaggregating activity by clopidogrel is due to a metabolic activation by the hepatic cytochrome P450-1A
72. ADP receptors on platelets
73. Evidence for the existence of two different ADP-binding sites on rat platelets
74. 1 purinoceptor in ADP-induced platelet activation
75. Ligand specificity and ticlopidine effects distinguish three human platelet ADP receptors
76. AC ADP receptor-mediated signaling by the antiplatelet drug clopidogrel
77. Structure and activity of the active metabolite of clopidogrel
78. Platelet antiaggregating activity and tolerance of clopidogrel in atherosclerotic patients
79. Single-dose pharmacodynamics of clopidogrel
80. Repeated-dose pharmacodynamics of clopidogrel in healthy subjects
81. The Canadian American ticlopidine study (CATS) in thromboembolic stroke
82. A randomized trial comparing ticlopidine hydrochloride with aspirin for the prevention of stroke in high-risk patients
83. Ticlopidine. A review of its pharmacology, clinical efficacy and tolerability in the prevention of cerebral ischaemia and stroke
84. Antiplatelet treatment with ticlopidine in unstable angina: A controlled multicenter clinical trial
85. A randomized comparison of antiplatelet and anticoagulant therapy after the placement of coronary-artery stents
86. Randomized multicenter comparison of conventional anticoagulation versus antiplatelet therapy in unplanned and elective coronary stenting: The Full Anticoagulation Versus Aspirin and Ticlopidine (FANTASTIC) Study
87. A clinical trial comparing three antithrombotic-drug regimens after coronary-artery stenting
88. Double-blind study of the safety of clopidogrel with and without a loading dose in combination with aspirin compared with ticlopidine in combination with aspirin after coronary stenting: The clopidogrel aspirin stent international cooperative study (CLASSICS)
89. The Clopidogrel in Unstable angina to prevent Recurrent Events (CURE) trial programme: Rationale, design and baseline characteristics including a meta-analysis of the effects of thienopyridines in vascular disease
90. A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE)
91. Thrombotic thrombocytopenic purpura associated with clopidogrel
92. 2T purinoceptor antagonists: Definition of the role of ADP in arterial thrombosis
93. Pharmacology of AR-C69931MX and related compounds: From pharmacological tools to clinical trials
94. 2T-purinoceptor antagonist, FPL 67085 in vitro and in the anaesthetized rat in vivo
95. 2T-receptor antagonists as novel antithrombotic agents
96. 2T-purinoceptor antagonist, FPL 67085, reliably, reversibly and safely inhibits ADP-induced platelet aggregation ex vivo in man
97. 2T receptor antagonist AR-C69931MX on ex vivo adenosine diphosphate-induced platelet aggregation and bleeding time in healthy volunteers
98. 2T receptor antagonist AR-C69931MX assessing safety, tolerability and activity in patients with acute coronary syndromes
99. Medical management of unstable angina
100. Tolerance and safety of cangrelor, a novel purin receptor antagonist, used as a platelet aggregation inhibitor in the acute coronary syndrome
101. 2T antagonist on platelet aggregation, platelet activation and platelet-leukocyte conjugate formation in vitro and following administration to patients with unstable angina
102. The biology of P-selectin glycoprotein ligand-1: Its role as a selectin counterreceptor in leukocyte-endothelial and leukocyte-platelet interaction
103. P-Selectin-β2-integrin cross-talk: A molecular mechanism for polymorphonuclear leukocyte recruitment at the site of vascular damage
104. Synergism between platelets and neutrophils in provoking cardiac dysfunction after ischemia and reperfusion: Role of selectins
105. 2T antagonist AR-C69931MX is a more effective inhibitor of ADP-induced platelet aggregation than clopidogrel
106. 2T antagonist AR-C69931MX
107. Superior antiplatelet effects of AR-C69931MX compared to clopidogrel in patients with ischemic heart disease
108. 2T receptor antagonists - Towards novel orally active antithrombotics
109. Thrombolytic therapy
110. Platelets and thrombolytic therapy
111. Link between the angiographic substudy and mortality outcomes in a large randomized trial of myocardial reperfusion: Importance of early and complete infarct artery reperfusion
112. Adverse long-term effects of reocclusion after coronary thrombolysis
113. Myocardial perfusion patterns related to thrombolysis in myocardial infarction perfusion grades after coronary angioplasty in patients with acute anterior wall myocardial infarction
114. Left ventricular function at 3 months after successful thrombolysis. Impact of reocclusion without reinfarction on ejection fraction, regional function, and remodeling
115. Studies on the release of a plasminogen activator inhibitor by human platelets
116. The roles of alpha 2-antiplasmin and plasminogen activator inhibitor 1 (PAI-1) in the inhibition of clot lysis
117. Effects of reteplase and alteplase on platelet aggregation and major receptor expression during the first 24 hours of acute myocardial infarction treatment
118. Effects of streptokinase and recombinant tissue plasminogen activator on platelet aggregation in whole blood
119. Platelet-coagulant protein interactions
120. Rapid and sustained coronary artery recanalization with combined bolus injection of recombinant tissue-type plasminogen activator and monoclonal antiplatelet GPIIb/IIIa antibody in a canine preparation
121. 2 and serotonin after thrombolysis with tissue-type plasminogen activator in a canine preparation of coronary thrombosis
122. Prevention of reoccluding platelet-rich thrombi in canine femoral arteries with a novel peptide antagonist of platelet glycoprotein IIb/IIIa receptors
123. Thromboxane synthetase inhibition with CGS 13080 improves coronary blood flow after streptokinase-induced thrombolysis
124. Augmentation of streptokinase-induced thrombolysis by heparin and prostacyclin
125. Influence of selective endoperoxide/thromboxane A2 receptor antagonism with sulotroban on lysis time and reocclusion rate after tissue plasminogen activator-induced coronary thrombolysis in the dog
126. PGE1 accelerates thrombolysis by tissue plasminogen activator
127. Lysis of plasminogen activator-resistant platelet-rich coronary artery thrombus with combined bolus injection of recombinant tissue-type plasminogen activator and antiplatelet GPIIb/IIIa antibody
128. 2T-receptor antagonist AR-C69931 in a canine model
129. Function and regulation of the B3 integrins in hemostasis and vascular biology
130. Platelet activation: Signal transduction via membrane receptors
131. Phosphorylation and dephosphorylation mechanisms in platelet function: A tightly regulated balance
132. IIbB3
133. A murine monoclonal antibody that completely blocks the binding of fibrinogen to platelets produces a thromboasthenic-like state in normal platelets and binds to glycoproteins IIb and/or IIIa
134. Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty
135. Platelet glycoprotein IIb/IIIa receptor blockade and low-dose heparin during percutaneous coronary revascularization
136. Randomised placebo-controlled trial of abciximab before and during coronary intervention in refractory unstable angina: The CAPTURE study
137. Novel dosing regimen of eptifibatide in planned coronary stent implantation (ESPRIT): A randomised, placebo-controlled trial. Enhanced Suppression of the Platelet IIb/IIIa Receptor with Integrilin Therapy
138. Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes
139. Inhibition of the platelet glycoprotein IIb/IIIa receptor with tirofiban in unstable angina and non-Q-wave myocardial infarction
140. Troponin concentrations for stratification of patients with acute coronary syndromes in relation to therapeutic efficacy of tirofiban
141. Benefit of abciximab in patients with refractory unstable angina in relation to serum troponin T levels
142. Oral Glycoprotein IIb/IIIa Inhibition With Orbofiban in Patients With Unstable Coronary Syndromes (OPUS-TIMI 16) Trial
143. Comparison of sibrafiban with aspirin for prevention of cardiovascular events after acute coronary syndromes: A randomised trial: Sibrafiban versus aspirin to yield maximum protection from ischemic heart events post-acute coronary syndromes
144. Long-term treatment with a platelet glycoprotein-receptor antagonist after percutaneous coronary revascularization. EXCITE Trial Investigators. Evaluation of oral xemilofiban in controlling thrombotic events
145. Randomized trial of a GPIIb/IIIa platelet receptor blocker in refractory unstable angina
146. Multicenter, randomized, double-blind, placebo-controlled trial of the platelet integrin glycoprotein IIb/IIIa blocker Integrilin in elective coronary intervention
147. Differential inhibition of platelet aggregation induced by adenosine diphosphate or a thrombin receptor-activating peptide in patients treated with bolus chimeric 7E3 Fab: Implications for inhibition of the internal pool of GPIIb/IIIa receptors
148. Pharmacodynamic efficacy, clinical safety, and outcomes after prolonged platelete glycoprotein IIb/IIIa receptor blockade with oral xemilofiban: Results of a multicenter, placebo-controlled, randomized trial
149. Randomized, double-blind, placebo-controlled dose-ranging study of tirofiban (MK-383) platelet IIb/IIIa blockade in high risk patients undergoing coronary angioplasty
150. First chronic platelet glycoprotein IIb/IIIa integrin blockade: A randomized, placebo-controlled pilot study of xemilofiban in unstable angina with percutaneous coronary interventions
151. Increased potency and decreased elimination of lamifiban, a GPIIb-IIIa antagonist, in patients with severe renal dysfunction
152. A whole blood assay of inhibition of platelet aggregation by glycoprotein IIb/IIIa antagonists: Comparison with other aggregation methodologies
153. Attainment and maintenance of platelet inhibition through standard dosing of abciximab in diabetic and nondiabetic patients undergoing percutaneous coronary intervention
154. Increased mortality with oral platelet glycoprotein IIb/IIIa antagonists: A meta-analysis of phase III multicenter randomized trials
155. 2T receptor antagonism as an alternative strategy to glycoprotein IIb/IIIa receptor antagonism
156. 2T platelet receptor antagonist, in patients undergoing percutaneous coronary interventions - Preliminary results from a placebo or active controlled trial