摘要
蛇床子素30μmol·L^(-1)及100μmol·L^(-1)使NE、CaCl_2和高K^+除极化所致的家兔主动脉条收缩量—效曲线右移,最大反应降低.表明蛇床子素有松弛血管平滑肌作用,并与Ca^(2+)呈非竞争性拮抗作用.和阻滞α受体或激动β受体无关;选择性作用于电位依赖性Ca^(2+)通道,抑制细胞外Ca^(2+)内流;在100μmol·L^(-1)时,明显减弱NE诱导的依赖细胞内Ca^(2+)收缩。证明蛇床子素松弛血管平滑肌作用可能与其Ca^(2+)拮抗作用有关。
It was reported that Os-thole(Ost) was isolated from the fruits of Cnidium monnieri(L. ) Cusson, possesses
anti - arrhythmic action and depressed the aortic pressure action in animal studies. Its calcium -antagonistic effects were studied on the isolated rabbit aortic strips.
Ost shifted the dose response curves for NE, CaCl2 and KC1 nonparallelly to the right, and depressed their maximal response; pD2' value is 3. 16, 4. 28 and 4. 39 respectively. It produced neither β- a-drenoceptic stimulating nor α - adreno-ceptic blocking effects. At the concentration of 100 μmol · L-1, Ost significantly inhibited the intra cellular Ca2+ dependent component of NE - induced contraction of the aortic strips, however, it didn't in-
hibit the extra cellular Ca2+ dependent component of NE - induced contraction of the aortic strips, These results indicated that Ost produced relaxation on vascular smooth muscle might result from its antagonistic effect to Ca2+ and mainly blocked calcium influx through PDC, and the mode of its anta -gonism is similar to that of verapamil.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1992年第3期227-231,共5页
Chinese Pharmacological Bulletin
关键词
蛇床子素
主动脉条
细胞内外钙
osthole
rabbit aortic strip
Drug dose response. curve
Intra and extra cellular calcium
