Folco G, Omini C, Rossoni G, Viganò T, Berti F
Eur J Pharmacol. 1982 Feb 26;78(2):159-65. doi: 10.1016/0014-2999(82)90232-1.
Various doses of histamine, bradykinin and leukotriene C4 caused bronchoconstriction in anaesthetized guinea-pigs which were breathing spontaneously or artificially ventilated; there was a simultaneous, dose-related increase in circulating TXA2. The animals were prepared for continuous recording of extracorporeal circulation in order to detect the appearance in the blood of bioassayable levels of TXA2 -like substance. Furthermore, a TXA2 derivative, the mono-O-Me-TXB2, was radioimmunoassayed. Atropine, oxytropium bromide and ipratropium bromide given in mumol doses prevented both the increased airway resistance and the release of TXA2-like substance in the blood Pirenzepine dihydrochloride was the least active of the drugs tested. The protecting activity of anticholinergics and the relationship with their ability to affect TXA2-like substance generation suggest a new site of action for these drugs besides the blockade of muscarinic receptors.
不同剂量的组胺、缓激肽和白三烯C4可使自主呼吸或人工通气的麻醉豚鼠发生支气管收缩;同时,循环中的血栓素A2(TXA2)也会出现与剂量相关的增加。对动物进行体外循环的连续记录,以检测血液中生物活性水平的TXA2样物质的出现。此外,对一种TXA2衍生物单-O-甲基-TXB2进行放射免疫分析。以微摩尔剂量给予阿托品、氧托溴铵和异丙托溴铵可预防气道阻力增加和血液中TXA2样物质的释放。盐酸哌仑西平是所测试药物中活性最低的。抗胆碱能药物的保护活性及其与影响TXA2样物质生成能力的关系表明,除了阻断毒蕈碱受体外,这些药物还有一个新的作用位点。