雷诺定受体介导的BK通道开放在他克莫司对大鼠胸主动脉舒张中的作用

发布时间：2019-03-19 20:34

【摘要】：目的:探究他克莫司对大鼠胸主动脉的舒张作用及其机制。方法:采用多道生理记录仪测定大鼠胸主动脉环张力,观察他克莫司对去甲肾上腺素诱导收缩的胸主动脉血管环的舒张作用,并观察伊比蝎毒素(选择性大电导钙离子激活的钾离子通道抑制剂)和雷诺定(Ryanodine,肌浆网钙离子释放抑制剂)对他克莫司舒张曲线的影响。结果:他克莫司对去甲肾上腺素(NE1.0×10-6 mol·L-1)预收缩有内皮和去内皮大鼠胸主动脉环均有显著地舒张作用,且非内皮依赖性途径在他克莫司对血管的舒张作用中起着重要作用,他克莫司对NE预收缩的去内皮大鼠胸主动脉环的舒张作用,可被雷诺定(10μmol·L-1)和iberiotoxin(100 nmol·L-1)抑制,分别从(17.41±1.94)%降至(12.38±1.17)%(雷诺定孵育前后比较,P0.05,n=7)和(16.69±2.66)%降至(10.46±1.17)%(iberiotoxin孵育前后比较,P0.05,n=7)。结论:他克莫司对血管的舒张作用主要是通过雷诺定受体引起钙火花的释放,从而激活大电导钙离子激活的钾离子通道(BK通道)开放引起的。
[Abstract]:Objective: To study the effect of tacrolimus on the relaxation of thoracic aorta in rats and its mechanism. Methods: The tension of the thoracic aortic rings was measured by a multi-channel physiological recorder, and the relaxation effect of tacrolimus on the vascular ring of the thoracic aorta induced by norepinephrine was observed. The effects of IbScorpion toxin (K + ion-channel inhibitor) and RENAULT (Ryanodine, sarcoplasmic reticulum calcium ion release inhibitor) on the relaxation curve of tacrolimus were also observed. Results: Tacrolimus has a significant effect on the pre-contraction of norepinephrine (NE1.0-10-6 mol 路 L-1), and the endothelium and the endothelium-dependent rat thoracic aortic rings, and the non-endothelium-dependent approach plays an important role in the relaxation of the blood vessel. The effect of tacrolimus on the relaxation of the thoracic aortic rings of NE pre-contracted endothelium was inhibited by Reno (10. mu.mol 路 L-1) and iberiotoxin (100 nmol 路 L-1), from (17.41-1.94)% to (12.38-1.17)% (P <0.05). N = 7) and (16.69% 2.66)% decreased to (10.46-1.17)% (before and after iberiotoxin incubation, P0.05, n = 7). Conclusion: The relaxation effect of tacrolimus on the blood vessel is mainly caused by the release of the calcium spark by the reno-fixed receptor, so that the activation of the large-conductance calcium ion-activated potassium channel (BK channel) is open.
【作者单位】：华中科技大学同济医学院基础医学院药理学系;
【基金】：华中科技大学自主创新基金(2013年) 国家自然科学研究基金(青年基金项目)(编号:81102439)
【分类号】：R965

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