Inhibition of Leukotriene (SRS‐A)‐Mediated Acute Lung Anaphylaxis by Azelastine in Guinea Pigs
Inhibition of Leukotriene (SRS‐A)‐Mediated Acute Lung Anaphylaxis by Azelastine in Guinea Pigs
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氮卓斯汀对豚鼠白三烯 (SRS-A) 介导的急性肺部过敏反应的抑制作用
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发表时间：
1986
期刊：
影响因子：
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通讯作者：
R. Sofia
中科院分区：
文献类型：
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作者：
N. Chand;K. Nolan;W. Diamantis;J. Perhach;R. Sofia
氮卓斯汀盐酸盐，化学名称为l(2H)-酞嗪酮，4-[(4-氯苯基)甲基]-2-(六氢-l-甲基-1H-氮杂-4-基)-，单盐酸盐，是一种新型、口服有效、长效的抗过敏/平喘药。研究了氮卓斯汀和选定的抗过敏药物抑制豚鼠 SRS-A（白三烯）介导的急性肺部过敏反应的能力（Konzett-Rossler 方法）。氮卓斯汀和酮替芬口服给药。抗原攻击前2小时和24小时；静脉注射色甘酸二钠（DSCG）。就在抗原攻击之前。抑制白三烯介导的过敏性支气管痉挛50%（ID50：mg/kg）所需的氮卓斯汀口服剂量为2小时0.063和24小时0.120。酮替芬剂量为 0.05 至 10 mg/kg，2 小时和 24 小时口服，DSCG 剂量为 0.3 至 10 mg/kg，0 分钟静脉注射，产生微弱、不一致且与剂量无关的抗过敏作用。氮卓斯汀是一种口服有效的长效体内白三烯合成和/或释放抑制剂。
Azelastine hydrochloride, chemically known as l(2H)‐phthalazinone, 4‐[(4‐chlorophenyl)methyl] ‐2‐(hexahydro‐l‐methyl‐lH‐azepine‐4‐yl)‐, monohydrochloride, is a novel, orally effective, long‐acting, antiallergic/antiasthmatic agent. The ability of azelastine and selected antiallergic drugs to inhibit SRS‐A (leukotriene)‐mediated acute lung anaphylaxis in guinea pigs (Konzett‐Rossler method) was investigated. Azelastine and ketotifen were administered p.o. 2 and 24 h before antigen challenge; disodium cromoglycate (DSCG) was administered i.v. immediately before antigen challenge. The oral dose of azelastine required to inhibit leukotriene‐mediated allergic bronchospasm by 50% (ID50: mg/kg) was 0.063 at 2 h and 0.120 at 24 h. Ketotifen at a dose of 0.05 to 10 mg/kg at 2 and 24 h, p.o., as well as DSCG at a dosage of 0.3 to 10 mg/kg at 0 min, i.v., produced weak, inconsistent and nondose‐related antianaphylactic effects. Azelastine is an orally effective and long‐acting inhibitor of in vivo synthesis and/or release of leukotrienes.