Bonne C, Latour E, Muller A, de Kozak Y, Faure J P, Malet F, Colin J, Tissot M, Giroud J P, Maghni K
Centre de Recherches, Laboratoire Chauvin, Montpellier, France.
Arzneimittelforschung. 1989 Oct;39(10):1246-50.
The paper describes the topical anti-inflammatory activity of 2-(2-hydroxy-4-methylphenyl)aminothiazole hydrochloride (CBS-113 A), a dual inhibitor of cyclooxygenase/lipoxygenase and a potent free radical scavenger. When applied in eye drops (0.01 to 0.1% according to the model used), the drug inhibited inflammation in experimental conjunctivitis and uveitis induced by various procedures (e.g. paracentesis, endotoxin, S-antigen, albumin, Fe2+). The compound also inhibited leukocyte infiltration and histamine release when administered locally in pleural cavity with carrageenan. CBS-113 A could decrease plasma leakage induced by arachidonic acid or platelet activating factor in skin and airway, respectively. However, it was devoid of any activity when administered by systemic route. The compound appears as a potentially useful anti-inflammatory drug, in particular in ophthalmology and as an alternative to glucocorticoids, since it does not present the side effects of these steroids (e.g. worsening of herpetic keratitis).
本文描述了盐酸2-(2-羟基-4-甲基苯基)氨基噻唑（CBS-113 A）的局部抗炎活性，它是一种环氧化酶/脂氧合酶双重抑制剂和强效自由基清除剂。当制成眼药水应用时（根据所使用的模型为0.01%至0.1%），该药物可抑制由各种方法（如穿刺、内毒素、S抗原、白蛋白、Fe2+）诱导的实验性结膜炎和葡萄膜炎中的炎症。当在胸腔内与角叉菜胶一起局部给药时，该化合物还可抑制白细胞浸润和组胺释放。CBS-113 A可分别减少花生四烯酸或血小板活化因子在皮肤和气道中诱导的血浆渗漏。然而，当通过全身途径给药时，它没有任何活性。该化合物似乎是一种潜在有用的抗炎药物，特别是在眼科领域，可作为糖皮质激素的替代品，因为它没有这些类固醇的副作用（如疱疹性角膜炎恶化）。
