摘要
比较了蝙蝠葛碱（Ｄａｕ）及其衍生物对离体兔胸主动脉条收缩的影响，与维拉帕米（Ｖｅｒ）对照表明，这些衍生物都非竞争性拮抗ＮＥ，ＫＣｌ和ＣａＣｌ２所致动脉条收缩，能抑制外钙内流及内钙释放引起的收缩，表明这些衍生物为钙通道阻滞剂。其中衍生物Ｄ７，Ｄ１０，Ｄ２０抑制ＮＥ激活ＲＯＣ、ＫＣｌ激活ＰＤＣ、ＮＥ激发胞内钙释放引起的收缩，其作用较Ｄａｕ为强。除Ｄ９外，其余８个衍生物对ＮＥ去极化后ＣａＣｌ２引起的收缩及ＮＥ致胞外钙内流引起的收缩较Ｄａｕ有更强的抑制作用。
With the Verapamil(Ver) and dauricine(Dau)as references,the effects of nine kinds of Dau derivatives inhibiting rabbit thoracic aortic strips in normal Krebs solution were compared.The results indicated that Dau derivatives can shift the dose-response curve of NE,KCl and CaCl2 to the right and depress their maximal responses──showed non-competitive antagonistic manner,and Dau derivatives also inhibited the contractions induced by intracellular Ca2+ and extracel ular Ca2+ after NE administration──were antagonistic reagents of calcium channel.Dau derivative D7,D10,D20 exhibited stronger inhibitions than Dau to contractions induced by(1) NE activating ROC(receptor operated calcium channel);(2)KCl activating PDC(potential dependent calcium channel); (3) release of intracellular Ca2+ after NE. Except for D9,other Dau derivatives showed deeper depressions than Dau to contractions induced by(1) CaCl2 after NE;(2) excelullar Ca2+ after NE.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1994年第5期303-305,共3页
Journal of China Pharmaceutical University
关键词
蝙蝠葛碱衍生物
受体
离子通道
钙通道阻滞剂
Dauricine derivatives
Verapamil
Thoracic aortic strips
Calcium channel
