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MN9202降压作用的实验研究(PDF)

《心脏杂志》[ISSN:1009-7236/CN:61-1268/R]

期数:
2003年第4期
页码:
296-299
栏目:
实验研究
出版日期:
2003-07-01

文章信息/Info

Title:
The experimental study of decrease blood pressure with MN9202
作者:
弥曼1; 袁秉祥2; 胡玉珍3; 朱肖星4; 梅其炳4
1.陕西省高等医学专科学校药理学教研室,陕西 西安 710068;2.西安交通大学医学院药理学教研室,陕西 西安 710061;第四军医大学:3.生理学教研室,4.药理学教研室,陕西 西安 710032
Author(s):
MI Man1;  YUAN Bing-xiang2;  HU Yu-zhen3;  ZHU Xiao-xing4;  MEI Qi-bing4
Department of Pharmacology, Shaanxi Medical College, Xi'an, Shaanxi 710068, China
关键词:
MN9202; 钙通道阻滞剂; 高血压
Keywords:
methyl pentyl 1;  4-dihydro-2;  6-dimethyl-4-(3-nitrophenyl)-3;  5-pyridine dicarboxylate(MN9202);  calcium channel blockers;  hypertension
分类号:
R544.1;R972.4
DOI:
-
文献标识码:
A
摘要:
目的:探讨2,6-二甲基-4-(3-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸-3-甲酯-5-正戊酯(MN9202)的降压作用及其机制。方法:应用清醒大鼠及肾性高血压大鼠,观察MN9202的降压作用,并采用离体兔胸主动脉张力实验观察MN9202的扩血管作用。结果:腹腔注射MN920210,30,100μg/kg对正常动物和肾性高血压大鼠均可产生明显的降压作用,具有明显的剂量依赖关系。MN9202和Nitrendipine对抗KCl引起家兔主动脉收缩的IC50分别为2.1μmol/L和3.1μmol/L,Emax则为68.8%和54.9%;对抗NE引起收缩的IC50分别是2.0μmol/L和2.2μmol/L,Emax是34.6%和32.2%;其作用不受内皮的影响;MN9202可显著抑制NE的依赖细胞外Ca2+收缩反应,而对内Ca2+收缩反应则无明显抑制作用。结论:MN9202具有明显的扩血管效应,其作用与其抑制电压依赖性钙通道,减少Ca2+内流有关。
Abstract:
AIM: To study the vasodilative and hypotensive effects of methylpenty l1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate(MN9202), a novel dihydropyidine calcium channel blocker. METHODS: Conscious rats and the rats with renal arterial occlusion hypertension were used to observe the reducing blood pressure activity. Rabbit aorta with endothelium or without endothelium were used to study the dilatory actions of the drug. RESULTS: MN9202 at dose of 10, 30 and 100μg/kg had obvious hypotensive effects on conscious rats and the rats with renal arterial occlusion hypertension, at dose-response manners. Both MN9202 and Nitrendipine could inhibitthe rabbit aorta contraction-induced by high-K+ depolarization, and their IC50 was 2.1μmol/L and 3.1μmol/L, Emax was 68.8% and 54.9% respectively. They could also inhibit the contraction-induced by NE, their IC50 was 2.0μmol/L and 2.2μmol/L, and Emax was 34.6% and 32.2% respectively. MN9202 obviously inhibited the extracellular Ca2+-dependent component of NE-induced contraction, but had no effectson intracellular Ca2+-dependent component. CONCLUSION: MN9202 has significant vasodilator effects and can decrease blood pressure. Its mechanisms mainly inhibit transmembrane inflow of extracellular Ca2+ through voltage dependent calciumc hannel.

参考文献/References

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备注/Memo

备注/Memo:
收稿日期：2002-01-17.
更新日期/Last Update: 2003-07-01