Sarpogrelate, a 5-HT2 receptor blocker, may have a preconditioning-like effect in patients with coronary artery disease
Sarpogrelate, a 5-HT2 receptor blocker, may have a preconditioning-like effect in patients with coronary artery disease
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DOI：
10.1253/circj.68.68
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发表时间：
2004-01-01
影响因子：
3.3
通讯作者：
Fujiwara, H
中科院分区：
文献类型：
--
作者：
Horibe, E;Nishigaki, K;Fujiwara, H
背景沙格雷酯是一种血清素受体阻滞剂，通过血小板抗聚集作用和/或血管舒张作用来增加络脉。然而，最近的一份报告显示，沙格雷酯的预处理作用可增强心肌细胞 PKC-ε: 的易位，随后通过抑制缺血期间血小板释放血清素来打开线粒体 KATP 通道，从而保护无侧支兔心脏免受细胞损伤。本研究采用经皮冠状动脉介入治疗（PCI）模型来明确沙格雷酯对人类冠状动脉疾病缺血性损伤的保护作用及其机制。 方法和结果该研究纳入了20名患有近端左前降支（LAD）动脉单支血管病变75%或90%狭窄的患者，进行了冠状动脉造影（CAG）。患者被随机分为对照组（n=10）和沙格雷酯组（n=10）。沙格雷酯组在充气后后期（即 90 秒和 120 秒）记录的 12 导联心电图上的 DeltaSTmax（最大 ST 抬高）和 2 ST（ST 抬高之和）明显小于对照组。左右CAG或两组之间的侧枝循环没有显着差异。结论沙格雷酯改善PCI期间的缺血性损伤，可能与预处理样机制有关，而不是刺激侧枝发育。
Background Sarpogrelate, a serotonin receptor blocker, increases collaterals via a platelet anti-aggregation effect and/or vasodilatation. However, a recent report showed a preconditioning effect of sarpogrelate that enhances the translocation of PKC-epsilon: of cardiomyocytes, followed by opening of the mitochondrial KATP channel via inhibition of serotonin release from platelets during ischemia, protecting against cellular injury in rabbit hearts without collaterals. The present study used a percutaneous coronary intervention (PCI) model to define the protective effect of sarpogrelate against ischemic injury and its mechanism in human coronary artery disease.Methods and results The study enrolled 20 patients with single vessel disease of 75% or 90% stenosis in the proximal left anterior descending (LAD) artery on coronary angiography (CAG). Patients were randomly divided into a control group (n=10) and a sarpogrelate group (n=10). The DeltaSTmax (maximum ST elevation) and 2 ST (sum of ST elevation) on the 12-lead ECG recorded in the late stages (ie, 90 s and 120 s) after inflation were significantly smaller in the sarpogrelate group than in the controls. There was no significant difference in collaterals on the right and left CAG or between the 2 groups.Conclusions Sarpogrelate improves ischemic injury during PCI and may be related to a preconditioning-like mechanism rather than to stimulating collateral development.