Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
CALCIUM-CHANNEL BLOCKING PROPERTIES OF SM-6586 IN RAT-HEART AND BRAINAS ASSESSED BY RADIOLIGAND BINDING ASSAY
Autore:
QU YL; SUGIYAMA K; NAGATOMO T; MANIWA T; MIYAGISHI A;
Indirizzi:
NIIGATA COLL PHARM,DEPT PHARMACOL,5-13-2 KAMISHINEI CHO NIIGATA 95021JAPAN SUMITOMO PHARMACEUT CO LTD,RES LABS OSAKA 554 JAPAN
Titolo Testata:
Japanese Journal of Pharmacology
fascicolo: 2, volume: 63, anno: 1993,
pagine: 165 - 169
SICI:
0021-5198(1993)63:2<165:CBPOSI>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
RECEPTORS; ISOMERS;
Keywords:
SM-6586; H-3-PN200-110 BINDING; TISSUE (RAT); CA2+ CHANNEL; CA2+ ANTAGONISTIC EFFECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
12
Recensione:
Indirizzi per estratti:
Citazione:
Y.L. Qu et al., "CALCIUM-CHANNEL BLOCKING PROPERTIES OF SM-6586 IN RAT-HEART AND BRAINAS ASSESSED BY RADIOLIGAND BINDING ASSAY", Japanese Journal of Pharmacology, 63(2), 1993, pp. 165-169

Abstract

The interaction of SM-6586 (methyl lyl-5-yl}-4-(3-nitrophenyl)pyridine-5-carboxylate) with the specific binding of H-3-PN200-110 to rat heart and brain membranes was characterized and compared with those of other Ca2+ antagonists. The blockade of H-3-PN200-110 binding sites induced by nifedipine, nitrendipine and nimodipine was reversed by washing, whereas the blockade by SM-6586 was not readily reversed under theseconditions. No significant difference was found in irreversibility between SM-6586 enantiomers. When rat aortic strips were pretreated withSM-6586, the contractions induced by 50 mM KCl were inhibited even though SM-6586 was not present in the extracellular medium. This residual inhibitory effect was much stronger than that of nicardipine. The inhibition of KCl-induced contractions by nifedipine and nitrendipine was easily reversed by washing. Thus, we suggest that (+)SM-6586 is a novel 1,4-dihydropyridine derivative having a very slow rate of dissociation from the binding site. This property may explain its long-lastingantihypertensive effect.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/11/20 alle ore 19:33:19