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青藤碱诱导大鼠主动脉舒张的研究。

A study of glaucine-induced relaxation of rat aorta.

作者信息

Loza I, Orallo F, Verde I, Gil-Longo J, Cadavid I, Calleja J M

机构信息

Departamento de Farmacología, Farmacia y Tecnología Farmaceutica, Facultad de Farmacia, Universidad de Santiago, Santiago de Compostela, Spain.

出版信息

Planta Med. 1993 Jun;59(3):229-31. doi: 10.1055/s-2006-959657.

DOI:10.1055/s-2006-959657
PMID:8316591
Abstract

The vasorelaxant effect of glaucine, the major alkaloid of Platycapnos spicata (L.) Bernh., was studied. At concentrations of 10 microM-0.3 mM in normal Krebs solution it was almost equieffective in relaxing K(+)-induced and noradrenaline-induced tension in rat aortic rings without endothelium, with IC50 values of 160 +/- 16 microM and 90 +/- 14 microM respectively. In experiments in a calcium-free medium, 10 microM glaucine strongly inhibited noradrenaline-induced contractions. Glaucine (0.3 mM) did not affect basal uptake of 45Ca, but induced uptake was reduced to 100% (K+) and 97.7% (noradrenaline) of the basal value. These results suggest that glaucine has an intracellular effect and also acts on the cell membrane by blocking voltage-dependent and receptor-operated calcium channels.

摘要

研究了荷包牡丹(Platycapnos spicata (L.) Bernh.)主要生物碱青藤碱的血管舒张作用。在正常Krebs溶液中,浓度为10微摩尔/升至0.3毫摩尔/升时,它在舒张无内皮大鼠主动脉环中钾离子诱导和去甲肾上腺素诱导的张力方面几乎具有同等效力,IC50值分别为160±16微摩尔/升和90±14微摩尔/升。在无钙培养基实验中,10微摩尔/升青藤碱强烈抑制去甲肾上腺素诱导的收缩。青藤碱(0.3毫摩尔/升)不影响45钙的基础摄取,但诱导摄取量分别降至基础值的100%(钾离子)和97.7%(去甲肾上腺素)。这些结果表明,青藤碱具有细胞内作用,并且还通过阻断电压依赖性和受体操纵性钙通道作用于细胞膜。

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引用本文的文献

1
Study of the in vivo and in vitro cardiovascular effects of (+)-glaucine and N-carbethoxysecoglaucine in rats.(+)-青藤碱和N-乙氧羰基去甲青藤碱对大鼠体内和体外心血管作用的研究。
Br J Pharmacol. 1995 Apr;114(7):1419-27. doi: 10.1111/j.1476-5381.1995.tb13364.x.