Mellemkjaer S, Nielsen-Kudsk J E, Nielsen C B, Siggaard C
Institute of Pharmacology, University of Aarhus, Denmark.
Eur J Pharmacol. 1989 Aug 22;167(2):275-80. doi: 10.1016/0014-2999(89)90588-8.
The relaxant activity of pinacidil, a proposed K+ channel opener, was compared in isolated guinea-pig trachea, aorta and pulmonary artery. In preparations precontracted by histamine or PGF2 alpha, pinacidil produced complete tracheal relaxation but only partial relaxation of vascular tissues. The order of responsiveness was: pulmonary artery greater than trachea greater than aorta. The slope of the pinacidil concentration-effect (C/E) curve was much steeper in the tracheal than in the vascular preparations. The pinacidil C/E curves for relaxation were similar when the three types of preparations were precontracted by 124 mM K+. Pretreatment with pinacidil caused a parallel shift of the tracheal histamine C/E curve to the right, whereas the maximal response to histamine was markedly depressed in the pulmonary artery.
将拟作为钾通道开放剂的匹那地尔的舒张活性,在离体豚鼠气管、主动脉和肺动脉中进行了比较。在由组胺或前列腺素F2α预收缩的标本中,匹那地尔可使气管完全舒张,但仅使血管组织部分舒张。反应性顺序为:肺动脉>气管>主动脉。匹那地尔浓度-效应(C/E)曲线的斜率在气管中比在血管标本中陡得多。当三种类型的标本用124 mM钾预收缩时,匹那地尔舒张的C/E曲线相似。用匹那地尔预处理使气管组胺C/E曲线平行右移,而肺动脉对组胺的最大反应明显降低。