摘要
观察内皮素受体拮抗剂CPU0213能否阻断异丙肾上腺素(isoprenaline,ISO)所致大鼠心肌细胞搏动加速及凋亡。分离大鼠心肌细胞。给ISO(10-7M)的同时给CPU0213(10-7、10-6、10-5M),并以普萘洛尔(10-6M)作为阳性药对照,观察各组心肌细胞的搏动次数。采用吖啶橙/碘化丙啶(AO/PI)染色法检测成年大鼠心肌细胞凋亡率的变化。普萘洛尔明显抑制ISO效应(P<0.001)。内皮素受体拮抗剂CPU0213明显抑制ISO所致的心肌细胞搏动和细胞凋亡,且呈浓度依赖性。大剂量CPU0213对ISO生物效应的阻断作用(P<0.001)与普萘洛尔相仿。内皮素受体拮抗剂CPU0213阻断ISO所致的心肌细胞搏动加速和增加细胞凋亡率等生物学效应,提示内皮素介导β-受体效应。
To investigate whether CPU 0213 could inhibit adult cardiac myocytes beats accelerating and apoptosis induced by isoprenaline. Add isoprenaline （ISO, 107M） and CPU 0213 （10^-7. 10^-6. 10^-5M） in the same pore simultaneously, respectively. Propranolol （10^-6 M） was used as a positive control. We counted cardiomyocytes beats within lmin and the ratio of apoptosis in cultured adult rat cardiac myocytes using AO/PI fluorescent dye. ISO increased cardiomyocytes beat and rate of apoptosis significantly, Propranolol was effective to suppress the biological effects of ISO. CPU 0213 could inhibit cardiomyocytes beats accelerating and apoptosis induced by ISO in a dose dependent manner. Endothelin receptor antagonist CPU0213 inhibits apoptosis and Other biological effects in adult rat cardiac myocytes induced by ISO. Endothelin may mediate biological effects of -receptor activation.
出处
《中国药事》
CAS
2007年第11期874-877,共4页
Chinese Pharmaceutical Affairs
基金
国家自然科学基金资助项目
No.30572193
