Ikegami K, Hata H, Fuchigami J, Tanaka K, Kohjimoto Y, Uchida S, Tasaka K
Department of Pharmacology, Kawanishi Pharma Research Institute, Nippon Boehringer Ingelheim Co., Ltd., Yato, Japan.
Eur J Pharmacol. 1997 Jun 5;328(1):75-81. doi: 10.1016/s0014-2999(97)83031-2.
We studied the effects of apafant (WEB 2086 BS), a specific and potent platelet activating factor (PAF) receptor antagonist, on the early and late airway responses in conscious and actively sensitized guinea pigs. An increase in airway resistance (Rs) was seen 1 min after the inhaled antigen challenge (early airway response), followed by another increase in Rs which peaked between 4 and 8 h after the provocation (late airway response). Oral administration of apafant as well as theophylline inhibited both early and late airway responses. Ozagrel, an inhibitor of thromboxane A2 synthetase, salbutamol, a beta2-adrenoceptor agonist, and dexamethasone significantly inhibited either the early or the late airway response only. Disodium cromoglycate inhibited neither the early nor the late airway response. The results showed that apafant inhibited both the early and late airway responses in sensitized guinea pigs and its effect was comparable or superior to that of anti-asthmatic drugs used clinically.
我们研究了特异性强效血小板活化因子（PAF）受体拮抗剂阿帕泛（WEB 2086 BS）对清醒且已主动致敏的豚鼠早期和晚期气道反应的影响。吸入抗原激发后1分钟可见气道阻力（Rs）增加（早期气道反应），随后Rs在激发后4至8小时达到峰值（晚期气道反应）。口服阿帕泛以及茶碱可抑制早期和晚期气道反应。血栓素A2合成酶抑制剂奥扎格雷、β2肾上腺素能受体激动剂沙丁胺醇和地塞米松仅能显著抑制早期或晚期气道反应。色甘酸钠对早期和晚期气道反应均无抑制作用。结果表明，阿帕泛可抑制致敏豚鼠的早期和晚期气道反应，其效果与临床使用的抗哮喘药物相当或更佳。
