TY -的T1 Epinastine(犯下801 cl)调节noncholinergic收缩在豚鼠气道体外prejunctional 5-HT1-like受体JF -欧洲呼吸杂志》乔和J SP - 1433 LP - 1438欧元六世- 9 - 7非盟-杜邦,LJ AU -米德,CJ盟——Demedts MG非盟- Verleden通用Y1 - 1996/07/01 UR - //www.qdcxjkg.com/content/9/7/1433.abstract N2 -电场刺激(EFS)豚鼠气道,在体外,引起一种兴奋性非肾上腺素能非胆碱能(eNANC)收缩，由感觉神经末梢释放速激肽介导。Epinastine (WAL 801CL)是一种抗组胺药物，对某些其他受体具有结合亲和力，包括α -肾上腺素能受体和各种5-羟色胺(5-HT)受体亚型。它被用于治疗哮喘;然而，其作用机制仍有待充分界定。我们研究了依匹斯汀在体外是否能调节豚鼠气道eNANC收缩，并试图阐明其受体机制。Epinastine (0.1-100 microM)对非胆碱能收缩产生浓度依赖性抑制，在100 microM时最大抑制率为91 +/- 7%。联合5-HT1/5-HT2拮抗剂、甲硫菊胺(1微米)或甲硫菊素(0.1微米)预处理后，依匹斯丁对非胆碱能收缩的抑制作用显著减弱。然而，用tropistron (1 microM)、5-HT3拮抗剂、ketanserin (10 microM)、5-HT2拮抗剂、硫operamide (10 microM)、组胺H3拮抗剂或酚妥拉明(10 microM)、α -肾上腺素能拮抗剂预处理均无效果。氯苯那敏(10微米)是另一种组胺H1受体拮抗剂，没有明显的5-HT受体结合亲和力，对eNANC收缩没有任何抑制作用。 Epinastine (100 microM) did not displace the dose-response curve to exogenously applied substance P (0.01-10 microM). These results suggest that epinastine, although identified as a 5-HT antagonist, acts as a 5-HT1 agonist and that it inhibits the noncholinergic contraction in guinea-pig airways through stimulation of a prejunctional 5-HT1-like receptor, located to sensory nerves. ER -