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Titolo:
PHARMACOLOGICAL CHARACTERISTICS OF ENDOTHELIN RECEPTORS IN THE RABBITVENTRICULAR MYOCARDIUM - THE NONSELECTIVE ENDOTHELIN RECEPTOR ANTAGONIST PD-145065 ANTAGONIZES THE POSITIVE INOTROPIC EFFECT OF ENDOTHELIN-3 BUT NOT OF ENDOTHELIN-1
Autore:
NOROTA I; ENDOH M;
Indirizzi:
YAMAGATA UNIV,SCH MED,DEPT PHARMACOL,2-2-2 IIDA NISHI YAMAGATA 99023 JAPAN YAMAGATA UNIV,SCH MED,DEPT PHARMACOL YAMAGATA 99023 JAPAN
Titolo Testata:
Molecular and cellular biochemistry
, volume: 161, anno: 1996,
pagine: 67 - 74
SICI:
0300-8177(1996)161:<67:PCOERI>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
LIGAND-BINDING SYSTEMS; SELECTIVE-INHIBITION; RAT ATRIA; HYDROLYSIS; SUBTYPE; PHOSPHOINOSITIDE; CELLS; PHOSPHATIDYLINOSITOL; CONTRACTION; PHYSIOLOGY;
Keywords:
ENDOTHELIN-1; ENDOTHELIN-3; POSITIVE INOTROPIC EFFECT; PD 145065; NONSELECTIVE ENDOTHELIN RECEPTOR ANTAGONIST; [I-125] ENDOTHELIN-1; [I-125] ENDOTHELIN-3; RECEPTOR BINDING; RABBIT VENTRICULAR MYOCARDIUM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
I. Norota e M. Endoh, "PHARMACOLOGICAL CHARACTERISTICS OF ENDOTHELIN RECEPTORS IN THE RABBITVENTRICULAR MYOCARDIUM - THE NONSELECTIVE ENDOTHELIN RECEPTOR ANTAGONIST PD-145065 ANTAGONIZES THE POSITIVE INOTROPIC EFFECT OF ENDOTHELIN-3 BUT NOT OF ENDOTHELIN-1", Molecular and cellular biochemistry, 161, 1996, pp. 67-74

Abstract

Endothelin-3 (ET-3) elicited a concentration-dependent positive inotropic effect on rabbit papillary muscle, the maximal response being approximately 65% of the maximal response to isoproterenol. ET-1 induced a positive inotropic effect over the concentration range below 10(-9) M, at which ET-3 did not produce a positive inotropic effect, but the maximal response to ET-1 was equivalent to or slightly lower than thatof ET-3. The nonselective ET receptor antagonist PD 145065 effectively antagonized the positive inotropic effect of ET-3 in a concentration-dependent manner and abolished it at 10(-5) M. PD 145065 decreased the positive inotropic effect induced by ET1 at lower concentrations (< 10(-9) M) but it did not affect the main portion of the concentration-response curve for the positive inotropic effect, i.e., the effect induced by high concentrations (> 10(-9) M) of ET-1. PD 145065 antagonized also the positive inotropic effect of sarafotoxin S6c. PD 145065 inhibited the specific binding of [I-125]ET-1 and of [I-125]ET-3 with a high- and a low-affinity site for competition. ET(B) selective ligands,RES-701-1 and sarafotoxin S6c, displaced [I-125(uc)]ET-3 with high affinity but they scarcely affected the [I-125]ET-1 binding. These findings indicate that different subtypes of the ET receptor are responsible for the induction of the positive inotropic effect of ET-3 and ET-1. ET receptors involved in the production of the positive inotropic effect in the rabbit ventricular myocardium have pharmacological characteristics that are different from those of conventional ET receptors originally classified based on the pharmacological findings in noncardiactissues. The positive inotropic effect of ET-3 in the rabbit ventricular muscle may be mediated predominantly by ET(A1) receptors that are susceptible to PD 145065 as well as BQ-123 and FR139317, and partiallymediated by ET(B) receptors that are inhibitable with RES-701-1. ET(A2) receptors that are resistant to ET(A) selective as well as nonselective antagonists may mainly be responsible for the positive inotropic effect of ET-1 in the rabbit ventricular muscle.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/09/20 alle ore 20:48:18