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Titolo:
The P2Y(12) receptor as a therapeutic target in cardiovascular disease
Autore:
Storey, RF;
Indirizzi:
Univ Nottingham Hosp, Queens Med Ctr, Nottingham NG7 2UH, England Univ Nottingham Hosp Nottingham England NG7 2UH tingham NG7 2UH, England
Titolo Testata:
PLATELETS
fascicolo: 4, volume: 12, anno: 2001,
pagine: 197 - 209
SICI:
0953-7104(200106)12:4<197:TPRAAT>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
INDUCED PLATELET ACTIVATION; ACUTE MYOCARDIAL-INFARCTION; STREPTOKINASE-INDUCED THROMBOLYSIS; ANTIPLATELET GPIIB/IIIA ANTIBODY; TISSUE PLASMINOGEN-ACTIVATOR; REFRACTORY UNSTABLE ANGINA; MOLECULAR-WEIGHT HEPARIN; COMBINED BOLUS INJECTION; LONG-TERM TREATMENT; HIGH-RISK PATIENTS;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
156
Recensione:
Indirizzi per estratti:
Indirizzo: Storey, RF Univ Nottingham Hosp, Queens Med Ctr, Nottingham NG7 2UH, England Univ Nottingham Hosp Nottingham England NG7 2UH 2UH, England
Citazione:
R.F. Storey, "The P2Y(12) receptor as a therapeutic target in cardiovascular disease", PLATELETS, 12(4), 2001, pp. 197-209

Abstract

Coronary thrombosis complicating rupture of atherosclerotic plaque is the predominant cause of acute coronary syndromes and platelets play a crucial role in this thrombus formation. Whilst aspirin has been successful in reducing cardiovascular morbidity and mortality, appreciation of its limited antiplatelet effects has stimulated the search for more effective antiplatelet agents. The thienopyridines, ticlopidine and clopidogrel, act, via metabolites, on the platelet ADP receptor subtype now designated P2Y(12) (formerly P-2T, P2T(AC), P2Y(ADP) or P2Y(cyc)) and these agents have proven clinical efficacy, Analogues of the natural P2Y(12) receptor antagonist ATP have been developed that act directly on the receptor and have a rapid onset of action. One such antagonist, AR-C69931MX, is being developed for clinical use, AR-C69931MX is a potent antagonist of ADP-induced platelet activation, aggregation and secretion and also antagonises platelet responses, includingprocoagulant activity, induced by all other agonists in view of the central role of the P2Y(12) receptor in amplifying platelet responses. Phase II studies of intravenous AR-C69931MX in patients with acute coronary syndromesshow that this agent has a rapid onset of action, rapidly achieving steady-state inhibition of platelet aggregation, with a half-life of only a few minutes, AR-C69931MX appears to be safe and well tolerated as adjunctive therapy in these patients, and more effective inhibition of platelet function is achieved than with clopidogrel. Orally active ATP analogues are also being developed that may be more effective than clopidogrel. Limitations of platelet glycoprotein IIb/IIIa antagonists leave scope for development of alternative antiplatelet agents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 02:13:57