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Titolo:
ELECTRICAL AND MECHANICAL EFFECTS OF A NOVEL ANTIHYPERTENSIVE QUINAZOLINE DERIVATIVE, (METHYLTHIO)-2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE, ONGUINEA-PIG VENTRICULAR MUSCLES
Autore:
YANG JM; YUEN TC; CHANG CW; JIN JS; YEN MH; CHERN JW;
Indirizzi:
NATL DEF MED CTR,DEPT PHYSIOL & BIOPHYS,POB 90048-503 TAIPEI TAIWAN NATL DEF MED CTR,DEPT PHARMACOL TAIPEI TAIWAN NATL TAIWAN UNIV,COLL MED,SCH PHARM TAIPEI TAIWAN
Titolo Testata:
Journal of cardiovascular pharmacology
fascicolo: 2, volume: 30, anno: 1997,
pagine: 229 - 234
SICI:
0160-2446(1997)30:2<229:EAMEOA>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-KINASE-C; PAPILLARY-MUSCLES; CARDIAC-MUSCLE; HEART-CELLS; K+ CURRENT; ALPHA-1-ADRENOCEPTORS; MYOCARDIUM; EXCHANGE; CA-2+; MICROELECTRODES;
Keywords:
ALPHA(1)-ADRENOCEPTOR; ARRHYTHMIA; INTRACELLULAR NA+ ACTIVITY; NA+/CA2+ EXCHANGE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
22
Recensione:
Indirizzi per estratti:
Citazione:
J.M. Yang et al., "ELECTRICAL AND MECHANICAL EFFECTS OF A NOVEL ANTIHYPERTENSIVE QUINAZOLINE DERIVATIVE, (METHYLTHIO)-2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE, ONGUINEA-PIG VENTRICULAR MUSCLES", Journal of cardiovascular pharmacology, 30(2), 1997, pp. 229-234

Abstract

Electrical and mechanical effects of -(methylthio)-2,3-dihydroimidazo[1,2-c]quinazoline (DL-017), a new synthesized antihypertensive agent,were studied in guinea-pig ventricular papillary muscles. In muscle fibers driven at 1 Hz, DL-017 decreased the twitch force in a concentration-dependent manner and significantly increased the action-potentialduration and decreased intracellular Na+ activity (a(Na)(i)) and maximal rate of upstroke of action-potential ((V) over dot(max)) when concentrations were greater than 1 mu M. Phenylephrine in the presence of 1 mu M propranolol produced a concentration-dependent positive inotropy. DL-017 (0.01 mu M) antagonized the positive inotropic effect of phenylephrine and shifted the concentration-response curve to the right. In K+-depolarized muscle fibers, 0.1 mu M DL-017 significantly decreased the contractile force without changing the slow action potential. In low-[K+](0) and high-[Ca2+](0) solutions, a train of stimuli triggered a spontaneous rhythm that could be abolished by 3 mu M DL-017. Our results suggest that DL-017 not only exhibits an alpha(1)-antagonisticeffect but also induces negative inotropy by a decrease in myofibrillar calcium sensitivity and inhibits Na+ channels at higher concentrations, contributing to the drug's negative inotropic and type-I antiarrhythmic effects.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 09:04:11