Folco G C, Passoni E, Viganò T, Daffonchio L, Rossoni G, Brunelli G, Berti F
Institute of Pharmacology and Pharmacognosy, University of Milan, Italy.
Pharmacol Res Commun. 1983 Nov;15(10):909-21. doi: 10.1016/s0031-6989(83)80021-6.
The selectivity of procaterol for beta 2-adrenoceptors vs beta 1-adrenoceptors in animals has been already described. In these studies the ability of procaterol to protect guinea-pig against bronchoconstriction induced by various spasmogens such as histamine, LTC4 and acetylcholine is demonstrated. The results obtained both in anaesthetized animals and in perfused lungs clearly show that procaterol antagonizes not only the direct effect of the bronchoconstrictors quoted above but also their ability to activate arachidonic acid metabolism and to augment the generation of TXA2. Procaterol (0, 3-3 micrograms/Kg i.v.) is more potent than salbutamol in protecting passively sensitized guinea-pig from massive bronchoconstriction following antigen challenge: a phenomenon which is paralleled by an increment of the circulating TXA2. The possibility that the adenylate-cyclase-stimulating properties of procaterol may explain its antiasthmatic activity is discussed.
丙卡特罗对动物β2肾上腺素能受体与β1肾上腺素能受体的选择性已有描述。在这些研究中，证实了丙卡特罗保护豚鼠免受组胺、白三烯C4和乙酰胆碱等各种致痉剂诱导的支气管收缩的能力。在麻醉动物和灌注肺中获得的结果清楚地表明，丙卡特罗不仅拮抗上述支气管收缩剂的直接作用，而且还拮抗它们激活花生四烯酸代谢和增加血栓素A2生成的能力。丙卡特罗（0.3 - 3微克/千克静脉注射）在保护被动致敏豚鼠免受抗原攻击后大规模支气管收缩方面比沙丁胺醇更有效：这一现象与循环血栓素A2的增加平行。讨论了丙卡特罗刺激腺苷酸环化酶的特性可能解释其抗哮喘活性的可能性。
