摘要
目的 研究CPU 86 0 17及L 甲状腺素对血管平滑肌收缩的影响及对α1A、α1B亚型的选择性。方法 以有钙、无钙液中由累积浓度去甲肾上腺素 (norepinephrine ,NE)引起的大鼠胸主动脉环的收缩 ,比较CPU 86 0 17(30 μmol·L-1)对正常及慢性甲状腺给药组 (Thy)大鼠血管平滑肌 (VSM)的α1受体的抑制作用。结果 在无钙液中由α1B引起的内钙释放所致VSM收缩占有钙液中VSM最大收缩的百分率 ,正常组和Thy组分别为 4 8 8%± 8 1%和 6 9.4 %± 9 7% (P <0 .0 1) ,复钙后由α1A引起的外钙内流所致VSM收缩百分率 ,分别为正常组 4 7 7%± 5 0 % ,Thy组为 2 2 1%± 9 4 % (P <0 .0 1)。加入CPU 86 0 17(30 μmol·L-1)后 ,对内钙释放所致的收缩 % ,正常对照组为 35 2 %± 10 1% ,Thy组为 35 2 %± 10 2 % ;而对外钙内流引起的收缩百分率则分别为 13 9%± 7 1%及 2 0 7%± 7 5 %。结论 L 甲状腺素使α1B的作用增强 ,而减弱α1A的作用。CPU 86 0
AIM To study the influence of CPU 86017 and L thyroxin on vascular smooth muscle(VSM) contractions and the selective effect on α 1A and α 1B subtype. METHODS The contractions of rat thoracic aortic rings in two groups were studied to compare the inhibitory effect of CPU 86017 (30 μmol·L -1 ) on vascular smooth muscle from normal and levothyroxin treated rats and the selective effect on the Ca 2+ entry via receptor operated channel (α 1A ) and intracellular Ca 2+ release (α 1B ) stimulated by norepinephrine. RESULTS The percentage of VSM contraction induced by intracellular calcium release through activation of α 1B receptor in Ca 2+ free medium was 48.8±8.1 and 69.4±9.7 ( P <0.01) respectively in normal and L thyroxin treated groups. On the other hand, the percentage of VSM contraction induced by calcium entry through α 1A receptor was 47.7±5.0 and 22.1±9.4 ( P <0.01) respectively in two groups. While CPU 86017(30 μmol·L\+\{-1\}) was added, the contraction percentage induced by intracellular calcium release was 35.2±10.1 and 35.2±10.2 respectively, the contraction percentage induced by calcium entry was 13.9±7.1 and 20.7±7.5 respectively. CONCLUSION CPU 86017 has significant inhibitory effect on α 1A and α 1B subtype in the normal and L thyroxin treated rats. L thyroxin enhances effects on α 1B receptor and has relatively less effect on α 1A subtype.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2002年第3期245-249,共5页
Journal of China Pharmaceutical University
基金
国家自然科学基金资助项目 (No .3 9670 83 5 )
