Pearce F L, Al-Laith M, Bosman L, Brostoff J, Cunniffe T M, Flint K C, Hudspith B N, Jaffar Z H, Johnson N M, Kassessinoff T A
Department of Chemistry, University College London, United Kingdom.
Drugs. 1989;37 Suppl 1:37-43; discussion 69-77. doi: 10.2165/00003495-198900371-00009.
Nedocromil sodium and sodium cromoglycate inhibited histamine release from rat peritoneal mast cells. Tachyphylaxis was observed with both drugs. The 2 compounds were extremely selective in their action, being less active against peritoneal mast cells from the hamster and completely ineffective against mast cells from the mouse. Human basophil leucocytes, tissue mast cells of the guinea-pig and rat intestinal mast cells were also unresponsive. Both drugs inhibited immunological histamine release from human pulmonary mast cells obtained by bronchoalveolar lavage (BAL) and, less effectively, from lung parenchyma. Nedocromil sodium was about 1 order of magnitude more potent than sodium cromoglycate in each case. Tachyphylaxis was observed with the dispersed lung, but not with the cells obtained by BAL, and the degree of inhibition varied inversely with the magnitude of the secretory response. The possible clinical significance of these observations is discussed.
奈多罗米钠和色甘酸钠可抑制大鼠腹腔肥大细胞释放组胺。两种药物均出现快速减敏现象。这两种化合物的作用具有极高的选择性，对仓鼠腹腔肥大细胞的活性较低，对小鼠肥大细胞则完全无作用。人嗜碱性白细胞、豚鼠组织肥大细胞和大鼠肠道肥大细胞也无反应。两种药物均抑制通过支气管肺泡灌洗（BAL）获得的人肺肥大细胞的免疫性组胺释放，对肺实质组胺释放的抑制作用较弱。在每种情况下，奈多罗米钠的效力比色甘酸钠强约1个数量级。在分散的肺组织中观察到快速减敏现象，但在通过BAL获得的细胞中未观察到，抑制程度与分泌反应的强度呈反比。讨论了这些观察结果可能的临床意义。
