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钾通道 opener P1075 对人体大隐静脉和人体内乳动脉的作用。

The effects of potassium channel opener P1075 on the human saphenous vein and human internal mammary artery.

机构信息

Department of Clinical Pharmacology, Pharmacology and Toxicology, Faculty of Medicine, University Belgrade, Belgrade, Serbia.

出版信息

J Cardiovasc Pharmacol. 2011 Jun;57(6):648-55. doi: 10.1097/FJC.0b013e3182145850.

Abstract

Because adrenergic contractions can contribute to the development of life-threatening spasm of coronary artery bypass graft, this study was performed to investigate the effect of adenosine 3-phosphate (ATP)-sensitive K channel (KATP) opener P1075 on contractions of isolated human saphenous vein (HSV) and human internal mammary artery (HIMA). Phasic contractions were evoked by electric field stimulation (20 Hz) and noradrenaline. The sustained contractions were evoked by phenylephrine. The presence of pore-forming Kir6.1 and Kir6.2 subunits of the KATP channels in the HIMA and only Kir6.2 in the HSV was confirmed immunomorphologically. P1075 inhibited in the HSV only, the electrical field stimulation contractions more strongly than noradrenaline contractions. In addition, the phenylephrine contractions of HSV were more sensitive to P1075 in comparison to those of HIMA. Glibenclamide, a KATP channel blocker antagonized the vasodilatation produced by P1075 in both grafts differently, because its effect was more prominent on the P1075-induced inhibition of contractions of HSV than of HIMA. We conclude that P1075 has a vasorelaxant effect and inhibited adrenergic contractions of the tested grafts. This effect is graft and vasoconstrictor selective and seems to be mediated by Kir6.1- and/or Kir6.2-containing KATP channels. Thus, P1075 can be considered as a potential drug in the prevention of graft spasm.

摘要

由于肾上腺素能收缩可能导致冠状动脉旁路移植术发生危及生命的痉挛,因此进行本研究旨在探讨三磷酸腺苷(ATP)敏感钾通道(KATP)开放剂 P1075 对离体人隐静脉(HSV)和人内乳动脉(HIMA)收缩的影响。电刺激(20 Hz)和去甲肾上腺素可诱发时相性收缩,而苯肾上腺素可诱发持续性收缩。免疫形态学证实了 KATP 通道的孔形成 Kir6.1 和 Kir6.2 亚单位存在于 HIMA 中,而仅存在于 HSV 中。P1075 仅在 HSV 中抑制电刺激收缩的作用强于去甲肾上腺素收缩。此外,与 HIMA 相比,HSV 的苯肾上腺素收缩对 P1075 更为敏感。KATP 通道阻滞剂格列本脲对两种移植物的 P1075 引起的血管舒张作用的拮抗作用不同,因为其对 P1075 抑制 HSV 收缩的作用比对 HIMA 的作用更为明显。我们得出结论,P1075 具有血管舒张作用,并抑制了所测试移植物的肾上腺素能收缩。这种作用具有移植物和血管收缩选择性,似乎由含有 Kir6.1 和/或 Kir6.2 的 KATP 通道介导。因此,P1075 可以被认为是预防移植物痉挛的潜在药物。

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