Little M M, Casale T B
Department of Internal Medicine, Veterans Administration Medical Center, Iowa City, Iowa.
J Allergy Clin Immunol. 1989 May;83(5):862-5. doi: 10.1016/0091-6749(89)90096-1.
To examine the mechanism potentially contributing to therapeutic efficacy of azelastine in allergic rhinitis and asthma, we studied the effect of azelastine on stimulated histamine release from basophils prepared as a mixed leukocyte suspension from human blood. Azelastine was found to significantly inhibit anti-IgE-stimulated basophil histamine release. Time-course experiments indicated that the inhibitory effect of azelastine was immediate and that preincubation of basophils in azelastine was not necessary. In dose-response experiments with azelastine, 1 to 100 mumol/L, significant inhibition of histamine release was consistently observed in azelastine concentrations greater than or equal to 10 mumol/L. This inhibition was dose dependent (r = 0.96; p less than 0.001) with maximal mean inhibition of 91 +/- 8% at 100 mumol/L of azelastine.
为研究氮卓斯汀治疗变应性鼻炎和哮喘的潜在作用机制，我们研究了氮卓斯汀对从人血中制备的混合白细胞悬液嗜碱性粒细胞组胺释放的影响。发现氮卓斯汀能显著抑制抗IgE刺激的嗜碱性粒细胞组胺释放。时间进程实验表明，氮卓斯汀的抑制作用是即时的，无需将嗜碱性粒细胞预先在氮卓斯汀中孵育。在1至100μmol/L氮卓斯汀的剂量反应实验中，当氮卓斯汀浓度大于或等于10μmol/L时，始终观察到组胺释放受到显著抑制。这种抑制呈剂量依赖性（r = 0.96；p < 0.001），在100μmol/L氮卓斯汀时平均最大抑制率为91±8%。
