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Titolo:
Effects of carvedilol on isolated heart mitochondria: Evidence for a protonophoretic mechanism
Autore:
Oliveira, PJ; Marques, MPM; de Carvalho, LAEB; Moreno, AJM;
Indirizzi:
Univ Coimbra, Dept Zool, Ctr Neurociencias Coimbra, P-3049 Coimbra, Portugal Univ Coimbra Coimbra Portugal P-3049 s Coimbra, P-3049 Coimbra, Portugal Univ Coimbra, Dept Bioquim, P-3049 Coimbra, Portugal Univ Coimbra Coimbra Portugal P-3049 t Bioquim, P-3049 Coimbra, Portugal Univ Coimbra, Fac Ciencias & Tecnol, Unidade I&D Quim Fis Mol, P-3049 Coimbra, Portugal Univ Coimbra Coimbra Portugal P-3049 m Fis Mol, P-3049 Coimbra, Portugal
Titolo Testata:
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
fascicolo: 1, volume: 276, anno: 2000,
pagine: 82 - 87
SICI:
0006-291X(20000916)276:1<82:EOCOIH>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-ADRENOCEPTOR ANTAGONIST; PHOSPHORYLATION; REPERFUSION; BUPIVACAINE; VASODILATOR; ISCHEMIA; RELEASE; DRUG;
Keywords:
rat heart mitochondria; carvedilol; uncoupler; ab initio SCF-MO calculations;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Moreno, AJM Univ Coimbra, Dept Zool, Ctr Neurociencias Coimbra, P-3049 Coimbra, Portugal Univ Coimbra Coimbra Portugal P-3049 -3049 Coimbra, Portugal
Citazione:
P.J. Oliveira et al., "Effects of carvedilol on isolated heart mitochondria: Evidence for a protonophoretic mechanism", BIOC BIOP R, 276(1), 2000, pp. 82-87

Abstract

Carvedilol ({1-[carbazolyl-(4)-oxyl-3-[2-methoxyphenoxyethyl)amino]-propanol-(2)}) is a novel compound used in clinical practice for the treatment ofcongestive heart failure, mild to moderate hypertension, and myocardial infarction, Carvedilol was also shown to protect cardiac mitochondria from oxidative stress events. Because mitochondria are the main suppliers of ATP for cardiac muscle work, a study of the effects of carvedilol in mitochondrial bioenergetics is necessary to fully understand the basis of its protective role in myocardial energetics. In this work we show that carvedilol actsas an uncoupler of oxidative phosphorylation, decreasing mitochondrial electric potential (Delta Psi) by a weak protonophoretic mechanism. Theoretical studies were carried out to determine the relevance of conformation and proton affinity of the protonable amino side-chain group in the proton-shuttling activity across the inner mitochondrial membrane. BM910228, a hydroxylated metabolite of carvedilol, was also studied for comparison with the parent compound, Implications for the protective role of carvedilol in heart mitochondrial bioenergetics are discussed. (C) 2000 Academic Press.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/07/20 alle ore 14:32:52