Vargaftig B B, Lefort J, Wal F, Chignard M, Medeiros M C
Eur J Pharmacol. 1982 Aug 27;82(3-4):121-30. doi: 10.1016/0014-2999(82)90500-3.
The non-steroidal anti-inflammatory drugs (NSAID) indomethacin, aspirin and salicylic acid, as well as the anti-histamine, mepyramine, and the anti-serotonin, methysergide, fail to interfere with bronchoconstriction, thrombo-cytopenia and hypotension induced by platelet-activating factor (PAF-acether, 1-O-octadecyl-2-acetyl-sn-3-glycerylphosphorylcholine) in the guinea-pig. When one of the NSAID was given combined with mepyramine and with methysergide, bronchoconstriction was suppressed, but thrombocytopenia and hypotension persisted. Platelets prepared from blood collected from animals treated with the NSAID or with mepyramine and/or methysergide, aggregated to a similar extent to PAF-acether; however, the accompanying release of ATP was inhibited in those animals which had been treated with the drug combination effective in vivo against bronchoconstriction. In vitro application to platelets of the drugs effective in vivo and ex vivo was ineffective in blocking the platelet-release reaction. This suggests the existence of in vivo sites of action for the synergistic inhibitory activity of NSAID and anti-histamine/anti-serotonin drugs on bronchoconstriction and on platelet secretion. PAF-acether possible releases from the platelets a bronchoconstrictor component, distinguishable from thromboxane A2 and depleted by reserpine administration to the animals, which could account for the in vivo effects on the bronchopulmonary system.
非甾体抗炎药吲哚美辛、阿司匹林和水杨酸,以及抗组胺药美吡拉敏和抗5-羟色胺药甲基麦角新碱,均不能抑制血小板活化因子(PAF-乙醚,1-O-十八烷基-2-乙酰基-sn-3-甘油磷酸胆碱)诱导的豚鼠支气管收缩、血小板减少和低血压。当其中一种非甾体抗炎药与美吡拉敏和甲基麦角新碱联合使用时,支气管收缩受到抑制,但血小板减少和低血压仍然存在。用非甾体抗炎药或美吡拉敏和/或甲基麦角新碱处理过的动物血液制备的血小板,对PAF-乙醚的聚集程度相似;然而,在体内对支气管收缩有效的药物组合处理过的动物中,伴随的ATP释放受到抑制。在体内和体外对血小板应用在体内有效的药物,对阻断血小板释放反应无效。这表明非甾体抗炎药和抗组胺药/抗5-羟色胺药对支气管收缩和血小板分泌的协同抑制活性存在体内作用位点。PAF-乙醚可能从血小板释放出一种支气管收缩成分,与血栓素A2不同,给动物注射利血平可使其耗竭,这可以解释其对支气管肺系统的体内作用。