当前位置： SCI文献检索 > JOURNAL OF CARDIOTHORACIC AND VASCULAR ANESTHESIA期刊下所有文献 > Effects of a novel benzodiazepine derivative, JM-1232(-), on human gastroepiploic artery in vitro.

Effects of a novel benzodiazepine derivative, JM-1232(-), on human gastroepiploic artery in vitro.

Abstract：

OBJECTIVE:To investigate the effects of JM-1232(-) on norepinephrine (10(-6) mol/L)- and high K(+) (40 mmol/L)-induced contractions in isolated human gastroepiploic arteries (GEA), and to compare them with the effects of midazolam and propofol. In addition, to investigate whether the benzodiazepine-receptor antagonist, flumazenil, or μ-opioid-receptor antagonist, naloxone, influenced the vascular effects of JM-1232(-). DESIGN:An in vitro experimental study. SETTING:University laboratory. PARTICIPANTS:GEA segments were used from 69 patients undergoing coronary artery bypass graft surgery. MEASUREMENTS AND MAIN RESULTS:JM-1232(-) produced dose-dependent relaxation effects in the rings. Although these effects of JM-1232(-) were greater than those of midazolam and propofol at high concentrations (10(-5)-10(-4) mol/L), there were no significantly different relaxation effects at the clinical concentrations of 3 × 10(-6) mol/L JM-1232(-), 3 × 10(-6) mol/L midazolam, and 1 × 10(-5) mol/L propofol. In addition, all these effects were independent of the presence of a functional endothelium. Vasorelaxation induced by JM-1232(-) on norepinephrine-preconstricted GEA was inhibited by flumazenil, but not by naloxone. CONCLUSIONS:These results indicate that JM-1232(-) dose-dependently relaxes smooth muscle in human GEA, this effect being independent of the endothelium. Within the ranges of plasma concentrations achieved in clinical practice, JM-1232(-) had similar vasorelaxation effects to midazolam and propofol. JM-1232(-)-induced vasorelaxation was inhibited by flumazenil, indicating that JM-1232(-)-induced vasorelaxation occurred via peripheral benzodiazepine receptor activation in the GEA.

journal_name

J Cardiothorac Vasc Anesth

journal_title

Journal of cardiothoracic and vascular anesthesia

authors

Moriyama T,Tsuneyoshi I,Kanmura Y

doi

10.1053/j.jvca.2010.03.013

subject

Has Abstract

pub_date

2011-02-01 00:00:00

pages

72-7

issue

1

eissn

1053-0770

issn

1532-8422

pii

S1053-0770(10)00107-2

journal_volume

25

pub_type

杂志文章

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