Saito W, Noguchi K, Okazaki K, Matsuda T, Kato Y, Tanaka H, Shigenobu K
Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba, Japan.
J Cardiovasc Pharmacol. 1998 Feb;31(2):327-9. doi: 10.1097/00005344-199802000-00021.
The effects of K+ channel openers, NIP-121, cromakalim, and pinacidil, on isolated myocardium and aorta were investigated at two different temperatures, 23 degrees C and 37 degrees C. In right ventricular myocardium, NIP-121 shortened the action-potential duration with little influence on other action-potential parameters at 37 degrees C, but not at 23 degrees C. In whole-cell clamped ventricular myocytes, NIP-121 induced a glibenclamide-sensitive outward current at 37 degrees C but not at 23 degrees C. No difference in tissue adenosine triphosphate (ATP) concentration was detected between ventricular myocardia incubated at 37 degrees C and at 23 degrees C. In aortic preparations precontracted with norepinephrine, NIP-121, cromakalim, and pinacidil produced endothelium-independent relaxation at 37 degrees C, which was antagonized by glibenclamide. The vasorelaxant effects were greatly reduced at 23 degrees C. Thus we demonstrated that the effects of K+ channel openers on the myocardium and vascular smooth muscle are temperature sensitive.
在23摄氏度和37摄氏度这两种不同温度下,研究了钾通道开放剂NIP - 121、克罗卡林和吡那地尔对离体心肌和主动脉的影响。在右心室心肌中,NIP - 121在37摄氏度时缩短动作电位时程,而对其他动作电位参数影响较小,但在23摄氏度时则无此作用。在全细胞钳制的心室肌细胞中,NIP - 121在37摄氏度时诱导出一种对格列本脲敏感的外向电流,但在23摄氏度时则无此现象。在37摄氏度和23摄氏度孵育的心室心肌之间未检测到组织三磷酸腺苷(ATP)浓度的差异。在预先用去甲肾上腺素预收缩的主动脉制剂中,NIP - 121、克罗卡林和吡那地尔在37摄氏度时产生非内皮依赖性舒张,这一作用被格列本脲拮抗。在第23摄氏度时,血管舒张作用大大减弱。因此,我们证明了钾通道开放剂对心肌和血管平滑肌的作用是温度敏感的。