Nagai H, Kitagaki K, Goto S, Suda H, Koda A
Department of Pharmacology, Gifu Pharmaceutical University, Japan.
Jpn J Pharmacol. 1991 May;56(1):13-21. doi: 10.1254/jjp.56.13.
The anti-allergic and anti-asthmatic activities of three potassium (K+) channel openers, cromakalim, pinacidil, and nicorandil, were investigated. 1) Forty-eight-hour homologous passive cutaneous anaphylaxis (PCA) in mice was not affected by cromakalim, pinacidil, or nicorandil. Ketotifen significantly inhibited the reaction. 2) Antigen-induced histamine release from sensitized guinea pig lung tissue was not affected by cromakalim, pinacidil or nicorandil (except for 10(-4) M nicorandil). Salbutamol inhibited the release of histamine. 3) Histamine, serotonin and LTC4-induced vasculitis in rat back skin was not affected by any of these three K+ channel openers. 4) Antigen-induced constriction of isolated sensitized guinea pig tracheal muscle was relaxed by each of the K+ channel openers. 5) Constrictions of isolated guinea pig tracheal muscle caused by high potassium, histamine, LTC4, or U-46619 were clearly relaxed by each of the three K+ channel openers. 6) Increases of airway resistance caused by histamine, LTD4, or U-46619 in guinea pigs in vivo were inhibited by administration of each of the three K+ channel openers. 7) Experimental asthma caused by the IgE antibody and antigen system in guinea pigs was inhibited by each of the three K+ channel openers.
研究了三种钾（K+）通道开放剂——克罗卡林、匹那地尔和尼可地尔的抗过敏和抗哮喘活性。1）小鼠48小时同源被动皮肤过敏反应（PCA）不受克罗卡林、匹那地尔或尼可地尔影响。酮替芬显著抑制该反应。2）致敏豚鼠肺组织中抗原诱导的组胺释放不受克罗卡林、匹那地尔或尼可地尔影响（10^(-4) M尼可地尔除外）。沙丁胺醇抑制组胺释放。3）组胺、5-羟色胺和白三烯C4诱导的大鼠背部皮肤血管炎不受这三种K+通道开放剂中任何一种的影响。4）抗原诱导的离体致敏豚鼠气管肌肉收缩被每种K+通道开放剂松弛。5）三种K+通道开放剂中的每一种都能明显松弛高钾、组胺、白三烯C4或U-46619引起的离体豚鼠气管肌肉收缩。6）三种K+通道开放剂中的每一种给药后，均可抑制组胺、白三烯D₄或U-46619在豚鼠体内引起的气道阻力增加。7）三种K+通道开放剂中的每一种均可抑制豚鼠中由IgE抗体和抗原系统引起的实验性哮喘。
