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Titolo:
The Na+/H+ exchange inhibitor cariporide: preclinical profile and approachto clinical development
Autore:
Scholz, W;
Indirizzi:
Hoechst AG, Hoechst Marion Roussel Deutschland GmbH, DG Cardiovasc Res, D-6230 Frankfurt, Germany Hoechst AG Frankfurt Germany D-6230 ovasc Res, D-6230 Frankfurt, Germany
Titolo Testata:
EUROPEAN HEART JOURNAL SUPPLEMENTS
fascicolo: K, volume: 1, anno: 1999,
pagine: K45 - K49
SICI:
1520-765X(199907)1:K<K45:TNEICP>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
H+ EXCHANGE; VENTRICULAR ARRHYTHMIAS; CARDIAC ISCHEMIA; RAT-HEART; REPERFUSION; HOE-694; ENERGY; HOE642;
Keywords:
cariporide; NHE inhibitor; GUARDIAN; myocardial ischaemia reperfusion;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
18
Recensione:
Indirizzi per estratti:
Indirizzo: Scholz, W Unterortstr 30, D-65760 Eschborn, Germany Unterortstr 30 Eschborn Germany D-65760 5760 Eschborn, Germany
Citazione:
W. Scholz, "The Na+/H+ exchange inhibitor cariporide: preclinical profile and approachto clinical development", EUR H J SUP, 1(K), 1999, pp. K45-K49

Abstract

NHE-1 has been identified as an ion transport system which plays a crucialrole in the pathophysiology of myocardial ischaemia/reperfusion. By inhibition of the NHE, intracellular Na+ and Ca2+ overload can be reduced and theprogression of the myocardium from ischaemia to necrosis can be delayed. The specific and potent NHE-1 inhibitor cariporide has been characterized inerythrocytes, platelets fibroblasts and myocardial cells from different species, including humans. Protective effects in ischaemia/reperfusion have been demonstrated in numerous experiments in isolated cells, isolated heartsand in in vivo models in different species. The NHE inhibitor was protective against all kinds of ischaemia/reperfusion injury of the heart such as arrhythmias, contracture, stunning and necrosis. The protective effects of the compound were most pronounced when it was given before the ischaemic event and less pronounced when it was given on reperfusion only. According to this profile, cariporide was tested in a patient population at high risk ofan ischaemic cardiac event, in a large clinical phase II/III trial, which is currently under evaluation.

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Documento generato il 04/04/20 alle ore 11:49:32