医药导报
醫藥導報
의약도보
HERALD OF MEDICINE
2014年
6期
726-728,729
,共4页
陈密%崔海东%郝素芳%卢云%郭莲军
陳密%崔海東%郝素芳%盧雲%郭蓮軍
진밀%최해동%학소방%로운%곽련군
蝙蝠葛诺林碱%基底动脉%舒张作用
蝙蝠葛諾林堿%基底動脈%舒張作用
편복갈낙림감%기저동맥%서장작용
Daurinoline%Basilar artery%Relaxation
目的:探讨蝙蝠葛诺林碱对家兔基底动脉血管平滑肌的舒张作用。方法制备家兔基底动脉血管环,采用半对数摩尔浓度累积给药方法,观察给予蝙蝠葛诺林碱对家兔基底动脉血管平滑肌的舒张作用。结果蝙蝠葛诺林碱对甲氧胺、5-羟色胺、氯化钾和组胺所致的家兔基底动脉收缩均有明显的扩张作用,最大舒张50%( IC50)浓度分别为8.67×10-5,1.78×10-6,6.79×10-7,4.98×10-4 mol·L-1。同时对甲氧胺、5-羟色胺、氯化钾和组胺所致量效曲线的影响,均显示为非竞争性拮抗作用。结论蝙蝠葛诺林碱通过非竞争性拮抗作用,能有效舒张家兔基底动脉血管平滑肌,改善脑循环。
目的:探討蝙蝠葛諾林堿對傢兔基底動脈血管平滑肌的舒張作用。方法製備傢兔基底動脈血管環,採用半對數摩爾濃度纍積給藥方法,觀察給予蝙蝠葛諾林堿對傢兔基底動脈血管平滑肌的舒張作用。結果蝙蝠葛諾林堿對甲氧胺、5-羥色胺、氯化鉀和組胺所緻的傢兔基底動脈收縮均有明顯的擴張作用,最大舒張50%( IC50)濃度分彆為8.67×10-5,1.78×10-6,6.79×10-7,4.98×10-4 mol·L-1。同時對甲氧胺、5-羥色胺、氯化鉀和組胺所緻量效麯線的影響,均顯示為非競爭性拮抗作用。結論蝙蝠葛諾林堿通過非競爭性拮抗作用,能有效舒張傢兔基底動脈血管平滑肌,改善腦循環。
목적:탐토편복갈낙림감대가토기저동맥혈관평활기적서장작용。방법제비가토기저동맥혈관배,채용반대수마이농도루적급약방법,관찰급여편복갈낙림감대가토기저동맥혈관평활기적서장작용。결과편복갈낙림감대갑양알、5-간색알、록화갑화조알소치적가토기저동맥수축균유명현적확장작용,최대서장50%( IC50)농도분별위8.67×10-5,1.78×10-6,6.79×10-7,4.98×10-4 mol·L-1。동시대갑양알、5-간색알、록화갑화조알소치량효곡선적영향,균현시위비경쟁성길항작용。결론편복갈낙림감통과비경쟁성길항작용,능유효서장가토기저동맥혈관평활기,개선뇌순배。
Objective To investigate the effect of daurinoline on basilar artery vascular smooth muscle. Methods The tension of isolated basilar artery ring of rabbit was measured. The effects of daurinoline on the basilar artery contracted by methoxamine,5-hydroxytryptamine(5-HT),KCl and Histamine( His)were also examined. Dose-response curves of 5-HT and KCl were observed as well. Results Daurinoline exerted obvious relaxation effect on the basilar artery vascular ring contracted by methoxamine,5-HT,KCl and His in a concentration-dependent manner. IC50 of daurinoline in methoxamine,5-HT,KCl and His-treated rabbits was 8.67×10-5,1.78×10-6,6.79×10-7 and 4.98×10-4 mol·L-1,respectively. The change of concentration-response curves of methoxamine,5-HT,KCl and His showed that daurinoline was a non-competitive antagonist. Conclusion Daurinoline exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism. The mechanism of relaxation action may be related to blockage of voltage-dependent or receptor-dependent calcium channels.