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Titolo:
Dual inhibition of angiotensin converting enzyme and neutral endopeptidaseby omapatrilat in rat in vivo
Autore:
Backlund, T; Palojoki, E; Gronholm, T; Eriksson, A; Vuolteenaho, O; Laine, M; Tikkanen, I;
Indirizzi:
Minerva Fdn, Inst Med Res, FIN-00290 Helsinki, Finland Minerva Fdn Helsinki Finland FIN-00290 Res, FIN-00290 Helsinki, Finland Univ Helsinki, Cent Hosp, Dept Med, FIN-00014 Helsinki, Finland Univ Helsinki Helsinki Finland FIN-00014 ed, FIN-00014 Helsinki, Finland Univ Oulu, Dept Physiol, Oulu, Finland Univ Oulu Oulu FinlandUniv Oulu, Dept Physiol, Oulu, Finland
Titolo Testata:
PHARMACOLOGICAL RESEARCH
fascicolo: 5, volume: 44, anno: 2001,
pagine: 411 - 418
SICI:
1043-6618(200111)44:5<411:DIOACE>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
NATRIURETIC PEPTIDES; INVITRO AUTORADIOGRAPHY; HYPERTENSION; BRADYKININ; HUMANS; HEART;
Keywords:
vasopeptidase inhibitors; omapatrilat; natriuretic peptides;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
22
Recensione:
Indirizzi per estratti:
Indirizzo: Laine, M Minerva Fdn, Inst Med Res, Haartmaninkatu 8, FIN-00290 Helsinki, Finland Minerva Fdn Haartmaninkatu 8 Helsinki Finland FIN-00290 Finland
Citazione:
T. Backlund et al., "Dual inhibition of angiotensin converting enzyme and neutral endopeptidaseby omapatrilat in rat in vivo", PHARMAC RES, 44(5), 2001, pp. 411-418

Abstract

The pharmacological profile of a vasopeptidase inhibitor is dependent on the ratio of neutral endopeptidase (NEP) vs angiotensin converting enzyme (ACE) inhibition of the particular drug. We used in vitro autoradiography to determine the local renal and cardiac NEP and ACE inhibition after oral treatment with the dual NEP/ACE inhibitor omapatrilat in rat. Maximal inhibition of both renal NEP and ACE was achieved at the omapatrilat dose of 40 mg kg(-1) day(-1). Effective local ACE inhibition was detected also in the myocardium. The haemodynamic effects were similar to captopril, but omapatrilat treatment produced more favorable effect on natriuretic peptide levels. In conclusion, good tissue penetration of omapatrilat and balanced NEP/ACE inhibition may prove to be useful in the treatment of hypertension and heartfailure. (C) 2001 Academic Press.

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Documento generato il 25/01/20 alle ore 19:46:50