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Titolo:
EFFECTS OF PIMOBENDAN AND ITS METABOLITE ON MYOFIBRILLAR CALCIUM RESPONSIVENESS AND ATPASE ACTIVITY IN THE PRESENCE OF INORGANIC-PHOSPHATE
Autore:
VANMEEL JCA; ENTZEROTH M; REDEMANN N; HAIGH RM;
Indirizzi:
DR KARL THOMAE GMBH,DEPT BIOL RES,MOLEC PHARMACOL GRP D-88397 BIBERACH GERMANY
Titolo Testata:
Arzneimittel-Forschung
fascicolo: 2, volume: 45-1, anno: 1995,
pagine: 136 - 141
SICI:
0004-4172(1995)45-1:2<136:EOPAIM>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
SKINNED HEART-MUSCLE; CONTRACTILE FAILURE; HUMAN MYOCARDIUM; CARDIAC-MUSCLE; FERRET HEART; TROPONIN-C; ACIDIC PH; FIBERS; FORCE; HYPOXIA;
Keywords:
ATPASE, MYOFIBRILLAR; CALCIUM SENSITIVITY, MYOFIBRILLAR; CAS 118428-36-7; PIMOBENDAN; UD-CG 115 BS, METABOLITE, PHARMACOLOGY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
J.C.A. Vanmeel et al., "EFFECTS OF PIMOBENDAN AND ITS METABOLITE ON MYOFIBRILLAR CALCIUM RESPONSIVENESS AND ATPASE ACTIVITY IN THE PRESENCE OF INORGANIC-PHOSPHATE", Arzneimittel-Forschung, 45-1(2), 1995, pp. 136-141

Abstract

The effects of the cardiotonic agent pimobendan (CAS 118428-36-7, UD-CG 115 BS) and its main metabolite UD-CG 212 on dog cardiac myofibrillar calcium responsiveness and ATPase activity were studied at nominal free inorganic phosphate (P-i) and at 5 mmol/l P-i. A rightward shift of the pCa-tension relationship with a marked depression of maximal tension was observed in the presence of 5 mmol/l P-i. Pimobendan increased myofibrillar calcium responsiveness at concentrations greater than or equal to 10(-5) mol/l. These effects of pimobendan, were significantly greater at 5 mmol/l P-i than at nominally free P-i. UD-CG 212 had no influence on myofibrillar calcium responsiveness at nominally free P-i however significant effects were observed at 10(-9) mol/l UD-CG 212 in the presence of 5 mmol/l P-i. UD-CG 212 (10(-8) mol/l) did not influence myofibrillar ATPase activity at pCa's 6.23, 5.99, and 4.36 with or without 5 mmol/l P-i whereas pimobendan (10(-4) mmol/l) had an effect only at pCa = 5.99 (without P-i) and pCa = 4.36 (+ 5 mmol/l P-i). The data suggest that the increase in myofibrillar calcium responsiveness at submaximal calcium concentrations by pimobendan and UD-CG 212 in the presence of 5 mmol/l P-i is brought about by a change in crossbridge kinetics or by enhancement of thin filament activation by adjacent strong cross-bridges. At maximal calcium activation, pimobendan mayadditionally, increase the population of strong cross-bridges.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 16:29:57