【摘要】 目的:研究川芎素(SF)对犬冠脉的舒张作用及机制。方法:以犬冠脉为标本,用去甲肾上腺素(NE)和氯化钾(KCl)刺激标本收缩,研究SF对NE和KCl致动脉收缩量效曲线的影响并测定pD2ˊ以考察其对电压依赖性和受体操纵性钙通道的影响;制作SF对NE和KCl致动脉收缩的抑制作用量效曲线以测定其IC50,进一步判断SF阻滞钙通道的作用强度;观察SF对NE致动脉收缩两种组分的影响,考察其对受体操纵性外钙内流和内钙释放的影响。结果:SF使NE和KCl收缩冠脉的量效曲线非平行右移,其非竞争性阻断NE和KCl的pD2ˊ分别为3.65±0.22和3.58±0.10。SF剂量依赖性地抑制NE和KCl引起的冠脉收缩,IC50分别为1.04±0.68×10-4和1.53±0.34×10-4M。SF剂量依赖性地抑制NE依内、外源性钙收缩。结论:SF可抑制NE和KCl引起的冠脉收缩,机制涉及抑制平滑肌细胞电压依赖性钙通道和受体操纵钙通道介导的外钙内流和内钙释放,但作用不强。更多还原

【Abstract】 Objective:To study the relaxation of sodium ferulate(SF) on dog’s coronary artery and its action mechanism.Methods:Using norepinephrine(NE) and potassium chloride(KCl) to stimulate the contraction of coronary artery circle,the effect of SF on NE or KCl-induced artery contraction dose-effect curve and pD2’ were investigated to deduce the effects of SF on voltage-dependent and receptor-operated calcium channel.The inhibition dose-effect curve of SF on NE or KCl-induced artery contraction was made to measure IC50 for deducing block action potency.The effects of SF on two components of NE-induced artery contraction were studied to observe the influences of SF on receptor-operated extra-calcium influx and intra-calcium release.Results:SF caused the dose-effect curve of NE or KCl-induced coronary artery contraction to move to the right side non-parallel and pD2’ of SF blocking NE and KCl noncompetitively were 3.65 ± 0.22 and 3.58 ± 0.10 respectively.SF inhibited NE or KCl-induced artery contraction dose-dependently and its IC50 were 1.04 ± 0.68 × 10-4 and 1.53 ± 0.34 × 10-4 mol/L respectively.SF also inhibited NE-induced intrinsic and extrinsic source calcium contraction.Conclusion:SF inhibited NE or KCl-induced coronary contraction and these involved in blocking the extra-calcium influx or intra-calcium release mediated by voltage-dependent and receptor-operated calcium channel of smooth muscle cell,but the effects were not strong.更多还原