药学学报
藥學學報
약학학보
ACTA PHARMACEUTICA SINICA
2001年
4期
241-245
,共5页
吴宁%任维华%霍笑风%陈强%王锐
吳寧%任維華%霍笑風%陳彊%王銳
오저%임유화%곽소풍%진강%왕예
内吗啡肽%降血压%内皮依赖性%构效关系
內嗎啡肽%降血壓%內皮依賴性%構效關繫
내마배태%강혈압%내피의뢰성%구효관계
目的研究内吗啡肽(EMs)及其类似物对心血管系统的影响,初步探讨其作用机理。方法测定EMs及其类似物对大鼠平均动脉压和后肢血管阻力、蟾蜍肠系膜微动脉内径、兔离体胸主动脉条张力的影响。结果 EMs及其类似物剂量依赖(10-9-10-6 mol*L-1,iv)且Nx敏感地降低麻醉大鼠平均动脉压、后肢血管灌流压和扩张蟾蜍肠系膜微动脉。EMs对去内皮兔离体胸主动脉条张力无影响;但剂量依赖地显著降低完整内皮胸主动脉条张力并被Nx和L-NNA阻断。结论 EMs及其类似物通过降低外周阻力而显著降低动脉血压,其作用与血管内皮细胞释放NO有关。
目的研究內嗎啡肽(EMs)及其類似物對心血管繫統的影響,初步探討其作用機理。方法測定EMs及其類似物對大鼠平均動脈壓和後肢血管阻力、蟾蜍腸繫膜微動脈內徑、兔離體胸主動脈條張力的影響。結果 EMs及其類似物劑量依賴(10-9-10-6 mol*L-1,iv)且Nx敏感地降低痳醉大鼠平均動脈壓、後肢血管灌流壓和擴張蟾蜍腸繫膜微動脈。EMs對去內皮兔離體胸主動脈條張力無影響;但劑量依賴地顯著降低完整內皮胸主動脈條張力併被Nx和L-NNA阻斷。結論 EMs及其類似物通過降低外週阻力而顯著降低動脈血壓,其作用與血管內皮細胞釋放NO有關。
목적연구내마배태(EMs)급기유사물대심혈관계통적영향,초보탐토기작용궤리。방법측정EMs급기유사물대대서평균동맥압화후지혈관조력、섬서장계막미동맥내경、토리체흉주동맥조장력적영향。결과 EMs급기유사물제량의뢰(10-9-10-6 mol*L-1,iv)차Nx민감지강저마취대서평균동맥압、후지혈관관류압화확장섬서장계막미동맥。EMs대거내피토리체흉주동맥조장력무영향;단제량의뢰지현저강저완정내피흉주동맥조장력병피Nx화L-NNA조단。결론 EMs급기유사물통과강저외주조력이현저강저동맥혈압,기작용여혈관내피세포석방NO유관。
AIM To analyze the effects of endomorphins (EMs) and their analogs ([D-Pro2]EM-1, [D-Ala2]EM-1, [D-Pro2]EM-2 and [D-Ala2]EM-2) on the cardiovascular system of anesthetized rats and to study its mechanism. METHODS Responses to EMs and their analogs were investigated in the systemic vascular bed of rats and the mesenteric microarteria of Bufo gargarizans. Responses to EMs were investigated on the hindquarters of the rat vascular bed under constant-flow conditions and on the isolated rabbit thoracic aorta strips. RESULTS The EMs and their analogs showed dose-related (10-9-10-6 mol*L-1, iv) and naloxone-sensitive (2 mg*kg-1, iv) hypotension in mean arterial pressure of rats with similar duration and vasodilatation in mesenteric microarteria of Bufo gargarizans. The sequence of potencies was EMs > [D-Pro2]EM-2 > [D-Ala2]EM-2 > [D-Ala2]EM-1 > [D-Pro2]EM-1. EMs were shown not to relax the isolated rabbit thoracic aorta strips without endothelium. EMs, however, relaxed them with endothelium significantly. This action was blocked by Nx (10-5 mol*L-1) and L-NNA (10-4 mol*L-1). CONCLUSION The significant hypotensive activity of EMs and their analogs is mainly associated with their vasodilatation, which is related to the release of NO from vascular endothelium, and their potency is not completely related to their affinity for μ-opiate receptor.