当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Effects of (+)-S-12967 and (-)-S-12968, two enantiomers of a new slow-acting 1,4-dihydropyridine, on rat coronary resistance arteries.

Effects of (+)-S-12967 and (-)-S-12968, two enantiomers of a new slow-acting 1,4-dihydropyridine, on rat coronary resistance arteries.

Abstract：

:The action of (+)-S-12967 and (-)-S-12968, two isomers of a new 1,4-dihydropyridine molecule (2-(-7-amino-2,5-dioxaheptyl)-3-ethoxycarbonyl-4-(2,3-dichlorop hen yl)-5-methoxycarbonyl-6-methyl 1,4-dihydropyridine), was studied on responses of rat isolated coronary resistance arteries (i.d. about 230 microns) to K+, Ca2+, and 5-hydroxytryptamine (5-HT). Both isomers slowly relaxed coronary arteries contracted with 125 mM K+, reaching a maximal effect in about 2 h. In contrast, the maximal relaxing effect of nifedipine was obtained within 20 min. The response to 125 mM K+ did not recover within the 2-h washout period in vessels exposed to the isomers but returned to pre-drug levels within 40 min in vessels exposed to nifedipine. Nifedipine was 4 times more potent than the (-)-isomer which again was about 200 times more potent that the (+)-isomer. The IC50[M] values were approximately 1 nM, 4 nM and 0.8 microM, respectively. The relaxing effect of the isomers, which has a pKa of 8.6, was dependent on the extracellular pH being greater at high than low pH. Both isomers antagonized the vessel responses to K+ and Ca2+ and 5-HT. Higher concentrations of the isomers were required to antagonize responses to K+ and 5-HT than to Ca2+, probably due to the more depolarized state of the vascular smooth muscle in the latter experiments. In conclusion, the results demonstrate extracellular pH dependence as well as stereoselectivity regarding potency of (+)-S-12967 and (-)-S-12968 in rat coronary arteries.(ABSTRACT TRUNCATED AT 250 WORDS)

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Prieto D,Mulvany MJ,Nyborg NC

doi

10.1016/0014-2999(93)90501-8

subject

Has Abstract

pub_date

1993-07-06 00:00:00

pages

27-35

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(93)90501-8

journal_volume

238

pub_type

杂志文章

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