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Titolo:
EVIDENCE THAT BKCA CHANNEL ACTIVATION CONTRIBUTES TO K-ARTERY( CHANNEL OPENER INDUCED RELAXATION OF THE PORCINE CORONARY)
Autore:
BALWIERCZAK JL; KRULAN CM; KIM HS; DELGRANDE D; WEISS GB; HU SL;
Indirizzi:
CIBA GEIGY CORP,DIV PHARMACEUT,RES DEPT,556 MORRIS AVE SUMMIT NJ 07901
Titolo Testata:
Naunyn-Schmiedeberg's archives of pharmacology
fascicolo: 2, volume: 352, anno: 1995,
pagine: 213 - 221
SICI:
0028-1298(1995)352:2<213:ETBCAC>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
SMOOTH-MUSCLE CELLS; RAT PORTAL-VEIN; SENSITIVE POTASSIUM CHANNELS; CROMAKALIM; GLIBENCLAMIDE; MODULATION; PINACIDIL; BRL-34915; LEVCROMAKALIM; CHARYBDOTOXIN;
Keywords:
K-ATP CHANNEL; BKCA CHANNEL; CORONARY ARTERY SMOOTH MUSCLE; BENZOPYRANS; CYANOGUANIDINES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
J.L. Balwierczak et al., "EVIDENCE THAT BKCA CHANNEL ACTIVATION CONTRIBUTES TO K-ARTERY( CHANNEL OPENER INDUCED RELAXATION OF THE PORCINE CORONARY)", Naunyn-Schmiedeberg's archives of pharmacology, 352(2), 1995, pp. 213-221

Abstract

The rank order of potency of a series of benzopyran and cyanoguanidine K+ channel openers (KCOs) for causing relaxation of the PGF(2 alpha)-precontracted porcine coronary artery was determined. Glyburide, an inhibitor of K-ATP channels, showed an apparent competitive inhibition of the vasorelaxant activity of the KCOs. The pA(2) values of glyburide when cromakalim and CGP 14877 (P1060) were used as vasorelaxants were 7.66 and 7.83, respectively. Charybdotoxin (40 nM), an inhibitor of BKCa channels, also caused a significant inhibition of the cromakalim mediated relaxation of the porcine coronary artery. In order to clarify the site of action of these KCOs, we identified a K+ channel currentin single porcine coronary arterial cells and measured channel activity in the presence of these compounds. The prominent K+ ion current inthese cells had characteristics typical of the conventional large Ca2-activated K+ channel (BKCa) present in other smooth muscle cells. Using symmetrical K+ concentrations, the channel had a conductance of 214 pS and was found to be sensitive to [Ca2+](i) and membrane potential. The KCOs were found to reversibly increase the open probability (P-o) of the channel without changing channel conductance. The potency of the KCOs to increase K+ channel opening was similar to the potency of these compounds to cause coronary artery relaxation. These results indicate that the porcine coronary artery contains the BKCa channel and that this channel, along with other types of K+ channels (K-ATP), mediate the vasorelaxant effects of K+ channel openers.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/09/20 alle ore 12:27:04