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Titolo:
A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reducesischemic myocardial injury in vitro and in vivo
Autore:
Knight, DR; Smith, AH; Flynn, DM; Macandrew, JT; Ellergy, SS; Kong, JX; Marala, RB; Wester, RT; Guzman-Perez, A; Hill, RJ; Magee, WP; Tracey, WR;
Indirizzi:
Pfizer Inc, Pfizer Global Res & Dev, Dept Cardiovasc & Metab Dis, Groton, CT 06340 USA Pfizer Inc Groton CT USA 06340 rdiovasc & Metab Dis, Groton, CT 06340 USA
Titolo Testata:
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 1, volume: 297, anno: 2001,
pagine: 254 - 259
SICI:
0022-3565(200104)297:1<254:ANSEII>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
NA+-H+ EXCHANGE; MOLECULAR-CLONING; CARDIAC ISCHEMIA; INFARCT SIZE; RAT-HEART; CARIPORIDE; REPERFUSION; ANTIPORTER; AMILORIDE; EXPRESSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Tracey, WR Pfizer Inc, Pfizer Global Res & Dev, Dept Cardiovasc & Metab Dis, MS8220-3125 Eastern Point Rd, Groton, CT 06340 USA Pfizer Inc MS8220-3125 Eastern Point Rd Groton CT USA 06340 USA
Citazione:
D.R. Knight et al., "A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reducesischemic myocardial injury in vitro and in vivo", J PHARM EXP, 297(1), 2001, pp. 254-259

Abstract

The cardioprotective efficacy of zoniporide (CP-597,396), a novel, potent,and selective inhibitor of the sodium-hydrogen exchanger isoform 1 (NHE-1), was evaluated both in vitro and in vivo using rabbit models of myocardialischemia-reperfusion injury. In these models, myocardial injury was elicited with 30 min of regional ischemia and 120 min of reperfusion. Zoniporide elicited a concentration-dependent reduction in infarct size (EC50 of 0.25 nM) in the isolated heart (Langendorff) and reduced infarct size by 83% (50nM). This compound was 2.5- to 20-fold more potent than either eniporide or cariporide (EC50 of 0.69 and 5.11 nM, respectively), and reduced infarct size to a greater extent than eniporide (58% reduction in infarct size). Inopen-chest, anesthetized rabbits, zoniporide also elicited a dose-dependent reduction in infarct size (ED50 of 0.45 mg/kg/h) and inhibited NHE-1-mediated platelet swelling (maximum inhibition 93%). Furthermore, zoniporide did not cause any in vivo hemodynamic (mean arterial pressure, heart rate, rate pressure product) changes. Zoniporide represents a novel class of potentNHE-1 inhibitors with potential utility for providing clinical cardioprotection.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 14:41:03