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目的:比较口服福莫特罗(rac-FMT)和(R,R)-福莫特罗(R,R-FMT)的支气管扩张和抗炎作用。方法:分别采用抗原气雾攻击致敏豚鼠和小鼠,观察豚鼠的肺功能变化以及小鼠肺内炎症细胞的集聚反应。结果:模型组豚鼠在抗原激发后1-30min的气道阻力(R_L)平均值增加101％±34％,动态肺顺应性(C_(dyn))降低42％±7％。rac-FMT 0.5,1.0和2.0 mg/g,R,R-FMT 0.25,0.5和1.0mg/kg灌胃给药(ig)呈剂量依赖抑制抗原引起的支气管收缩反应,rac-FMT的ID_(50)(95％可信限)分别为0.96(0.86-1.07)和1.59(1.32-1.92)mg/g;R,R-FMT分别为0.52(0.45-0.59)和0.43(0.37-0.51)mg/g。rac-FMT抑制抗原攻击引起的致敏小鼠肺内总炎症细胞和嗜 酸性粒细胞聚集,ID_(50)(95％C1)分别为1.48(1.22-1.81)和0.80(0.62-1.04)mg/g;RR-FMT分别为0.80(0.57-1.13)和0.60(0.43-0.83)mg/g。结论:R,R-FMT保护豚鼠哮喘模型抗原攻击引起的R_1和C_(dyn)变化,抑制致敏小鼠的气道炎症,其作用强于rac-FMT约2倍。
OBJECTIVE: To compare the bronchodilatory and anti-inflammatory effects of oral formoterol (rac-FMT) and (R, R) -formoterol (R, R-FMT). Methods: Allergen guinea pigs and mice were challenged with antigen aerosol. The changes of lung function in guinea pigs and the agglutination of inflammatory cells in the lungs of mice were observed. Results: The mean airway resistance (R_L) increased by 101% ± 34% and the dynamic lung compliance (C dyn) decreased by 42% ± 7% in the model group at 1-30min after antigen challenge. rac-FMT 0.5, 1.0 and 2.0 mg / g, R, R-FMT 0.25, 0.5 and 1.0 mg / kg intragastrically administered ig dose-dependent inhibition of antigen-induced bronchoconstriction reaction, rac-FMT ID_ ) Were 0.96 (0.86-1.07) and 1.59 (1.32-1.92) mg / g, respectively; the R and R-FMT were 0.52 (0.45-0.59) and 0.43 (0.37-0.51) mg / g . rac-FMT inhibited the total inflammatory cells and eosinophil accumulation in the lungs of sensitized mice induced by antigen challenge with ID50 (95% CI) of 1.48 (1.22-1.81) and 0.80 (0.62-1.04) mg / g; RR-FMT was 0.80 (0.57-1.13) and 0.60 (0.43-0.83) mg / g, respectively. CONCLUSION: R, R-FMT can protect against airway inflammation in sensitized mice by up-regulating R_1 and C_ (dyn) induced by antigen challenge in guinea pig asthma model, which is about 2 times stronger than rac-FMT.