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替米沙坦对大鼠离体肠系膜动脉环的血管舒张作用。

The vasodilatory action of telmisartan on isolated mesenteric artery rings from rats.

作者信息

Chen Xiao-Ping, Qian Li-Ren

机构信息

Department of Hematology, Navy General Hospital of PLA, Beijing, China.

出版信息

Iran J Basic Med Sci. 2015 Oct;18(10):974-8.

Abstract

OBJECTIVES

Angiotensin II type 1 receptor blockers (ARBs) represent one of the widely used antihypertensive agents. In addition to anti-hypertension effect, some ARBs also show other molecular effects such as activating peroxisome proliferator-activated receptor-γ and so on. Here we studied the effects of telmisartan on the rat isolated mesenteric artery rings pre-contracted by phenylephrine (PE).

MATERIALS AND METHODS

Rat mesenteric artery rings were pre-contracted with 10 μM PE, and cumulative concentration-response curves to telmisartan were obtained. The endothelium-dependent mechanisms were investigated by mechanical removal of the endothelium. K(+) channels were investigated by pretreatment of the artery rings with various K(+) channel blockers.

RESULTS

Telmisartan produced concentration-dependent relaxation of the artery rings pre-contracted by 10 μM PE. Denudation of the endothelium did not affect the relaxant effect of telmisartan. Pretreatment with BaCl2 nearly inhibited the relaxation induced by the 0.5, 1, 5 and 10 μM telmisartan, but did not affect the relaxation induced by the 50 and 100 μM telmisartan. While the relaxation induced by telmisartan was not affected by pretreatment with TEA, 4-AP and glibenclamide.

CONCLUSION

These findings demonstrated that telmisartan produces concentration dependent vasodilation in isolated rat mesenteric artery rings with or without endothelium pre-contracted by PE. KIR channel may be involved in such a relaxant effect of telmisartan.

摘要

目的

血管紧张素II 1型受体阻滞剂(ARBs)是广泛使用的抗高血压药物之一。除抗高血压作用外,一些ARBs还显示出其他分子效应,如激活过氧化物酶体增殖物激活受体γ等。在此,我们研究了替米沙坦对苯肾上腺素(PE)预收缩的大鼠离体肠系膜动脉环的影响。

材料与方法

用10μM PE预收缩大鼠肠系膜动脉环,获得替米沙坦的累积浓度-反应曲线。通过机械去除内皮来研究内皮依赖性机制。用各种钾通道阻滞剂预处理动脉环来研究钾通道。

结果

替米沙坦使10μM PE预收缩的动脉环产生浓度依赖性舒张。内皮剥脱不影响替米沙坦的舒张作用。用BaCl2预处理几乎抑制了0.5、1、5和10μM替米沙坦诱导的舒张,但不影响50和100μM替米沙坦诱导的舒张。而替米沙坦诱导的舒张不受TEA、4-AP和格列本脲预处理的影响。

结论

这些发现表明,替米沙坦在有或无PE预收缩的离体大鼠肠系膜动脉环中均产生浓度依赖性血管舒张。钾离子内向整流通道可能参与替米沙坦的这种舒张作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dec3/4686581/aaca11125150/IJBMS-18-974-g001.jpg

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