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伐地那非作为大鼠肺动脉钙通道阻滞剂的评价。

An evaluation of vardenafil as a calcium channel blocker in pulmonary artery in rats.

作者信息

Minareci Edibe, Sadan Gulay

机构信息

Department of Pharmacology, School of Medicine, Akdeniz University, Antalya 07070, Turkey.

出版信息

Indian J Pharmacol. 2014 Mar-Apr;46(2):185-90. doi: 10.4103/0253-7613.129315.

DOI:10.4103/0253-7613.129315
PMID:24741191
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3987188/
Abstract

OBJECTIVE

Vardenafil was reported to relax rat pulmonary artery through endothelium-dependent mechanisms. The aim of this in vitro study was to investigate other related mechanisms for this effect.

MATERIALS AND METHODS

Endothelium-intact and denuded artery rings were suspended in order to record isometric tension. In the rings with or without endothelium, the concentration-response curves for vardenafil were generated. In the rings without endothelium the contractile response induced by phenylephrine (Phe) or KCl was assessed in the presence or absence of vardenafil. In the last set of experiments, pulmonary artery rings were exposed to calcium-free isotonic depolarizing solution and the contractile response induced by the addition of calcium was evaluated in the presence or absence of vardenafil, nifedipine, verapamil or 1H-[1,2,4] oxadiazolo[4,3-a] quinoxalin-1-one (ODQ).

RESULTS

Vardenafil attenuated pulmonary artery contraction induced by phenylephrine in the presence and absence of endothelium. In addition, vardenafil attenuated both Phe or KCl-induced contraction but, it's effect on the KCl dose-response curve was more significant. Vardenafil also inhibited the contractile response induced by calcium in a dose-dependent manner. Addition of nifedipine or verapamil did not significantly alter this effect while ODQ incubation significantly inhibited vardenafil-induced relaxation.

CONCLUSION

From these findings, it was proposed that vardenafil relaxed rat pulmonary artery through inhibiting calcium influx.

摘要

目的

据报道，伐地那非可通过内皮依赖性机制舒张大鼠肺动脉。本体外研究的目的是探究此效应的其他相关机制。

材料与方法

将完整内皮和去内皮的动脉环悬挂起来以记录等长张力。在有或无内皮的动脉环中，生成伐地那非的浓度-反应曲线。在无内皮的动脉环中，评估在有或无伐地那非情况下苯肾上腺素（Phe）或氯化钾（KCl）诱导的收缩反应。在最后一组实验中，将肺动脉环置于无钙等渗去极化溶液中，并评估在有或无伐地那非、硝苯地平、维拉帕米或1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮（ODQ）情况下添加钙后诱导的收缩反应。

结果

无论有无内皮，伐地那非均可减弱苯肾上腺素诱导的肺动脉收缩。此外，伐地那非减弱了Phe或KCl诱导的收缩，但它对KCl剂量-反应曲线的影响更显著。伐地那非还以剂量依赖性方式抑制钙诱导的收缩反应。添加硝苯地平或维拉帕米并未显著改变此效应，而ODQ孵育显著抑制了伐地那非诱导的舒张。

结论

基于这些发现，提出伐地那非通过抑制钙内流来舒张大鼠肺动脉。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/87b2d91ff8f6/IJPharm-46-185-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/396cdef4ba74/IJPharm-46-185-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/e0fe888a2826/IJPharm-46-185-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/c88297aef506/IJPharm-46-185-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/87b2d91ff8f6/IJPharm-46-185-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/396cdef4ba74/IJPharm-46-185-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/e0fe888a2826/IJPharm-46-185-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/c88297aef506/IJPharm-46-185-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c61f/3987188/87b2d91ff8f6/IJPharm-46-185-g004.jpg

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