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沙丁胺醇和茶碱抑制豚鼠速发型过敏性结膜炎的能力。

The ability of salbutamol and theophylline to suppress immediate allergic conjunctivitis in the guinea pig.

作者信息

Gautheron P, Sugrue M F

机构信息

Centre de Recherche, Merck Sharp & Dohme-Chibret, Riom, France.

出版信息

Graefes Arch Clin Exp Ophthalmol. 1987;225(5):331-4. doi: 10.1007/BF02153399.

Abstract

Topically administered salbutamol was extremely effective in suppressing immediate allergic conjunctivitis in the guinea pig; a dose as low as 0.1% elicited 98% inhibition. Topical pretreatment with 1% propranolol completely blocked the suppressant action of 0.1% salbutamol. This was also the case after systemic propranolol (1 mg/kg SC); the beta-adrenoceptor antagonist itself has no effect on antigen-induced inflammation. The effect of 0.1% salbutamol was unaltered by pretreatment with the specific beta 1-adrenoceptor antagonist betaxolol (1 mg/kg SC). In marked contrast, the suppressant action of 0.1% salbutamol was profoundly inhibited by pretreatment with the selective beta 2-adrenoceptor antagonist ICI-118,551 (0.5 mg/kg SC). The experiments employing beta-adrenoceptor antagonists unequivocally demonstrate that the salbutamol suppression of immediate allergic conjunctivitis in the guinea pig is mediated via the activation of beta 2-adrenoceptors. The methylxanthine phosphodiesterase inhibitor theophylline was active after oral administration, 50 mg/kg eliciting an 80% inhibition. Theophylline was inactive topically at 1% and 5%, but this could be due to the fact that the compound was insoluble at these concentrations. Thus, procedures that elevate cyclic-AMP levels suppress immediate hypersensitivity reactions in the guinea pig conjunctiva. Whether or nor this offers an alternative approach to treat allergic conjunctivitis in humans remains to be determined.

摘要

局部应用沙丁胺醇对抑制豚鼠速发型过敏性结膜炎极为有效;低至0.1%的剂量可产生98%的抑制作用。用1%普萘洛尔进行局部预处理可完全阻断0.1%沙丁胺醇的抑制作用。全身应用普萘洛尔(1mg/kg皮下注射)后也是如此;β-肾上腺素能受体拮抗剂本身对抗原诱导的炎症无作用。0.1%沙丁胺醇的作用不受特异性β1-肾上腺素能受体拮抗剂倍他洛尔(1mg/kg皮下注射)预处理的影响。形成鲜明对比的是,0.1%沙丁胺醇的抑制作用被选择性β2-肾上腺素能受体拮抗剂ICI-118,551(0.5mg/kg皮下注射)预处理显著抑制。使用β-肾上腺素能受体拮抗剂的实验明确表明,豚鼠速发型过敏性结膜炎中沙丁胺醇的抑制作用是通过β2-肾上腺素能受体的激活介导的。甲基黄嘌呤磷酸二酯酶抑制剂茶碱口服给药后有活性,50mg/kg可产生80%的抑制作用。茶碱在1%和5%浓度下局部应用无活性,但这可能是由于该化合物在这些浓度下不溶。因此,提高环磷酸腺苷水平的方法可抑制豚鼠结膜中的速发型超敏反应。这是否为治疗人类过敏性结膜炎提供了另一种方法仍有待确定。

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