Department of Pharmacology, Faculty of Pharmaceutical Sciences, Yasuda Women's University , 6-13-1 Yasuhigashi, Asaminami-Ku, Hiroshima 731-0153 , Japan.
Immunopharmacol Immunotoxicol. 2013 Oct;35(5):545-8. doi: 10.3109/08923973.2013.812653. Epub 2013 Jul 16.
The present study was performed to investigate the histamine-induced airway effect of levocetirizine, an active enantiomer of cetirizine, by intranasal application using ddY mice. Nasal rubbing and sneezing after histamine application into the nasal cavity were used as an index of histamine-induced airway effect in mice. Intranasal application of levocetirizine inhibited both nasal rubbing and sneezing concentration-dependently, and the ED50 values were 0.62 (0.51-0.77) and 0.70 (0.51-1.02) %/site for nasal rubbing and sneezing, respectively. ED50 values of cetirizine were 1.24 (1.02-1.59) and 1.35 (1.02-2.08) %/site for nasal rubbing and sneezing, respectively. Levocetirizine also inhibited nasal rubbing and sneezing when administered orally. These results clearly indicate that levocetirizine was about two times more potent than cetirizine by intranasal application, similar to the findings of the former's affinity for human histamine H1 receptors. In addition, the present findings raise the expectation of the development of levocetirizine nasal drops.
本研究旨在通过滴鼻应用左西替利嗪（西替利嗪的活性对映体）来研究组胺诱导的气道效应，使用 ddY 小鼠。鼻腔内应用组胺后引起的鼻摩擦和打喷嚏被用作小鼠组胺诱导气道效应的指标。左西替利嗪的滴鼻应用浓度依赖性地抑制鼻摩擦和打喷嚏，鼻摩擦和打喷嚏的 ED50 值分别为 0.62（0.51-0.77）和 0.70（0.51-1.02）%/部位。西替利嗪的 ED50 值分别为 1.24（1.02-1.59）和 1.35（1.02-2.08）%/部位。左西替利嗪口服给药也抑制鼻摩擦和打喷嚏。这些结果清楚地表明，左西替利嗪通过滴鼻应用的效力约为西替利嗪的两倍，与前者对人组胺 H1 受体的亲和力的发现相似。此外，本研究结果提高了开发左西替利嗪滴鼻剂的期望。
