INHIBITION OF VASOCONSTRICTION BY TETRAMETHYLPYRAZINE - DOES IT ACT BY BLOCKING THE VOLTAGE-DEPENDENT CA CHANNEL
INHIBITION OF VASOCONSTRICTION BY TETRAMETHYLPYRAZINE - DOES IT ACT BY BLOCKING THE VOLTAGE-DEPENDENT CA CHANNEL
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DOI：
10.1097/00005344-199001000-00025
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发表时间：
1990-01-01
影响因子：
3
通讯作者：
CHEN, MC
中科院分区：
文献类型：
--
作者：
KWAN, CY;DANIEL, EE;CHEN, MC
采用犬肠系膜动脉环制剂，研究了川芎嗪（tetramethylpyrazine， TMP，又称川芎嗪）的体外血管作用。川芎嗪是一种从Ligustium Wollichii Franchat中提取的血管活性成分；一种广泛用于治疗心血管疾病的中草药成分。TMP对血管肌肉的静息力没有影响，但对血管对KCl和苯肾上腺素（PHE）的收缩反应有剂量依赖性抑制。这些抑制作用是可逆的，并且在较低的激动剂浓度下更为突出。在50 .mu的无ca培养基中，TMP对PHE也有抑制作用。M EGTA提示细胞内Ca2+释放的作用。因此，TMP不是先前声称的特定ca通道阻滞剂。它的血管扩张作用是通过抑制钙内流以及细胞内Ca2+的释放来介导的。
Using dog mesenteric arterial ring preparations, we studied the in vitro vascular effects of tetramethylpyrazine (TMP, also known as Ligustrazine), a vasoactive component derived from Ligustium Wollichii Franchat; a widely used ingredient in Chinese herbal medicine for the treatment of cardiovascular diseases. TMP has no effect on the resting force of the vascular muscle, but it caused a dose-dependent inhibition of vascular contractile responses to KCl and phenylephrine (PHE). These inhibitory effects of TMP were reversible and more prominent at lower agonist concentrations. TMP also inhibited the responses to PHE in Ca-free medium containing 50 .mu.M EGTA suggesting the action on the release of intracellular Ca2+. Therefore, TMP is not a specific Ca-channel blocker as claimed previously. Its vasodilatory effect is mediated by the inhibition of Ca influx, as well as the release of intracellular Ca2+.