Yin K S, Taki F, Takagi K, Satake T
1st Affiliated Hospital of Nanjing Medical College.
Zhonghua Jie He He Hu Xi Za Zhi. 1991 Jun;14(3):149-51, 189-90.
The effect of azelastine, a new on the down-regulation of beta-receptor agonist was investigated. Male Hartley guinea pigs received injections of saline or terbutaline (T.) and/or azelastine (A.) for successive 7 days. The radioligand binding assays for beta-adrenoceptors in the lung membranes of the guinea pigs were performed. The results showed the differences of numbers of maximal binding sites (Bmax) among four groups were significant. The Bmax of beta-adrenoceptor in T. group was less than that in control group (P less than 0.02). The Bmax in A. group was more than that in control group (P less than 0.05). The Bmax in T. plus A. was more than that in T. group, and there was no significant difference between Bmax in T. group and in T. plus A. group (P greater than 0.1). The differences of affinity (Kd) of beta-adrenoceptor among four groups were not significant. Azelastine increased the density of beta-adrenoceptors and partially prevented the down-regulation of beta-adrenoceptor caused by terbutaline.
研究了一种新型β受体激动剂氮卓斯汀对β受体下调的影响。雄性Hartley豚鼠连续7天注射生理盐水或特布他林（T.）和/或氮卓斯汀（A.）。对豚鼠肺膜中的β肾上腺素能受体进行放射性配体结合测定。结果显示，四组之间最大结合位点（Bmax）数量的差异具有显著性。T.组中β肾上腺素能受体的Bmax低于对照组（P<0.02）。A.组中的Bmax高于对照组（P<0.05）。T.加A.组中的Bmax高于T.组，且T.组与T.加A.组的Bmax之间无显著差异（P>0.1）。四组之间β肾上腺素能受体亲和力（Kd）的差异不显著。氮卓斯汀增加了β肾上腺素能受体的密度，并部分阻止了由特布他林引起的β肾上腺素能受体下调。
