Effects of orally administered olopatadine hydrochloride on the ocular allergic reaction in rats
Effects of orally administered olopatadine hydrochloride on the ocular allergic reaction in rats
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口服盐酸奥洛他定对大鼠眼部过敏反应的影响
DOI：
10.1046/j.1440-1592.2003.00281.x
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发表时间：
2003
影响因子：
6.8
通讯作者：
A. Karasawa
中科院分区：
文献类型：
--
作者：
T. Tamura;Hitoshi Sato;I. Miki;Kazuo T. Suzuki;K. Ohmori;A. Karasawa
摘要背景盐酸奥洛他定是一种具有组胺H1受体拮抗作用的抗过敏药.我们研究了奥洛他定对被动过敏反应和化合物48/80诱导的大鼠结膜炎的影响。方法将大鼠抗卵清蛋白（OVA）血清注射于大鼠右眼上结膜下，然后静脉注射抗原和伊文思蓝染料，诱导大鼠被动致敏，建立过敏性结膜炎模型。30分钟后，测量渗入结膜的染料量。通过注射化合物48/80在大鼠中诱导非过敏性结膜炎。在激发前1h口服奥洛他定或其他参比化合物。结果口服奥洛他定0.01 ~ 1 mg/kg可显著抑制被动过敏反应后染料渗漏入结膜的量，ID 50值为0.093mg/kg。对照组结膜及睑缘皮肤组织病理检查可见水肿及淋巴细胞浸润。0.03和0.3mg/kg奥洛他定可降低这些病理学发现的级别。其他抗过敏药物（1 mg/kg氯雷他定、0.3 mg/kg依匹斯汀、0.3 mg/kg西替啶、1 mg/kg依巴斯汀、30 mg/kg非索非那定和3 mg/kg扑尔敏）经口给药时，可抑制被动过敏反应诱导的结膜血管通透性增高，与盐酸奥洛他定的情况相同。结膜下给药化合物48/80诱导血管通透性过高，推测其由组胺释放介导。经口给予0.1和1 mg/kg奥洛他定可显著抑制染料渗漏量。结论口服奥洛他定有望改善过敏性结膜炎。
ABSTRACT Background Olopatadine hydrochloride is an antiallergic agent with histamine H 1 receptor antagonistic action. We investigated the effects of olopatadine on passive anaphylaxis reaction- and compound 48/80-induced conjunctivitis in rats. Methods Allergic conjunctivitis was induced in rats passively sensitized by injection of rat anti-ovalbumin (anti-OVA) serum into the upper subconjunctiva of the right eye, followed by intravenous administration of the antigen and Evans blue dye. After 30min, the amount of dye leaking into the conjunctiva was measured. Non-allergic conjunctivitis was induced in rats by injection of compound 48/80. Olopatadine or other reference compounds were orally given 1h before the challenge. Results The amount of dye leaking into the conjunctiva following passive anaphylaxis was significantly inhibited by oral administration of 0.01-1mg/kg olopatadine and the ID 50 value was 0.093mg/kg. In the control group, pathological examination revealed edema and lymphocyte infiltration in the conjunctiva and the palpebral skin. Olopatadine, at 0.03 and 0.3mg/kg, reduced the grade of these pathological findings. The other antiallergic drugs (1mg/kg loratadine, 0.3mg/kg epinastine, 0.3mg/kg cetiridine, 1mg/kg ebastine, 30mg/kg fexofenadine and 3mg/kg chlorpheniramine), when administered orally, inhibited the passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva, as was the case with olopatadine hydrochloride. Subconjunctival administration of compound 48/80 induced vascular hyperpermeability, which is presumably mediated by histamine release. Oral administration of 0.1 and 1mg/kg olopatadine significantly inhibited the amount of dye leakage. Conclusion Orally administered olopatadine is expected to improve allergic conjunctivitis.
过敏原过敏受试者结膜激发时炎症介质的释放。
DOI：
10.1016/0091-6749(90)90075-f
发表时间：
1990
期刊：
The Journal of allergy and clinical immunology
影响因子：
--
作者：
Proud,D;Sweet,J;Stein,P;Settipane,RA;Kagey-Sobotka,A;Friedlaender,MH;Lichtenstein,LM
通讯作者：
Lichtenstein,LM
奥洛他定抑制抗免疫球蛋白 E 刺激的结膜肥大细胞上调结膜上皮细胞上 ICAM-1 的表达。
DOI：
10.1016/s1081-1206(10)62926-2
发表时间：
2001
期刊：
Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology
影响因子：
--
作者：
Cook,EB;Stahl,JL;Barney,NP;Graziano,FM
通讯作者：
Graziano,FM