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血浆中CPU - 86017的浓度与抑制哇巴因诱导的豚鼠心律失常及降低心率的关系。

Plasma CPU-86017 concentrations regarding suppression of ouabain-induced cardiac arrhythmias and decrease of heart rate in guinea pigs.

作者信息

Khan H H, Dai D Z, Xiao D W, Lin S, Wang Z Z, Lou S, Qing Q

机构信息

Research Division of Pharmacology, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Acta Pharmacol Sin. 2000 Nov;21(11):1039-42.

PMID:11501061
Abstract

AIM

To determine the effective plasma levels of CPU-86017 which could suppress the cardiac arrhythmias induced by i.v. ouabain in guinea pigs.

METHODS

The cardiac arrhythmias and the heart rate were monitored by ECG traces. Blood samples were collected to determine plasma levels using HPLC assay. TXB2 and 6-keto-PGF1 alpha were measured in plasma.

RESULTS

The plasma concentrations of CPU-86017 which were effective to suppress ventricular fibrillation (VF) and heart rate were 0.13-0.23 mg/L and 0.13-0.31 mg/L, respectively. A reduction of TXB2 levels and an elevation of 6-keto-PGF1 alpha levels were observed after CPU-86017 i.v. administration.

CONCLUSION

The arrhythmia-suppressing and heart rate-slowing effect of CPU-86017 followed a linear relationship with its concentrations in plasma.

摘要

目的

确定能够抑制静脉注射哇巴因诱导的豚鼠心律失常的CPU-86017有效血浆水平。

方法

通过心电图监测心律失常和心率。采集血样,采用高效液相色谱法测定血浆水平。检测血浆中TXB2和6-酮-前列腺素F1α的含量。

结果

有效抑制室颤(VF)和心率的CPU-86017血浆浓度分别为0.13 - 0.23 mg/L和0.13 - 0.31 mg/L。静脉注射CPU-86017后,观察到TXB2水平降低,6-酮-前列腺素F1α水平升高。

结论

CPU-86017的抗心律失常和减慢心率作用与其血浆浓度呈线性关系。

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