Journal
JOURNAL OF PHARMACY AND PHARMACOLOGY
Volume 52, Issue 11, Pages 1431-1434Publisher
WILEY-BLACKWELL
DOI: 10.1211/0022357001777441
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We have investigated the endothelium-independent vasorelaxant effect of the new flavonoid dioclein (5,2',5'-trihydroxy-6-7-dimethoxyflavanone) in the rat aorta. In endothelium-denuded vessels, dioclein induced a concentration-dependent relaxation of aortic rings precontracted with noradrenaline (IC50 = 3.5 +/- 0.89 x 10(-4) M) and KCl (IC50 = 5.2 +/- 1.2 x 10(-4) M). In the absence of extracellular calcium, dioclein reduced the contraction induced by noradrenaline (maximal reduction approximately 33%) but not that induced by caffeine. Dioclein also produced a concentration-dependent inhibition of the sustained contractions induced by the phorbol ester 12-O-tetradecanoyl phorbol-13-acetate in normal (IC50 = 4.0 +/- 0.2 x 10(-4) M) and Ca2+-free solution (IC50 = 4.0 +/- 0.3 x 10(-4) M). The results indicate that the endothelium-independent vasorelaxant effect of dioclein may be explained by inhibition of contractions dependent on activation of protein kinase C, voltage-dependent Ca2+ influx and on the release of intracellular Ca2+ stores sensitive to noradrenaline.
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