抽象的
几内亚猪气道的电场刺激(EFS),体外唤起兴奋性的非肾上腺素能量(ENANC)收缩,所述无感觉神经末梢释放Tachykinins介导。齿素(WAL 801CL)是一种在某些其他受体中具有结合亲和力的抗组胺药药物,包括α-肾上腺素能受体和各种血清素(5-HT)受体亚型。它用于哮喘治疗;但是,它的行动机制仍有待完全定义。我们研究了卓越素是否可以在体外调节豚鼠气道中的ENANC收缩,并试图阐明其受体机制。卓越素(0.1-100 microM)产生浓度依赖性抑制非胆管能收缩,最大抑制为100微米,最大抑制91 +/- 7%。用组合的5-HT1 / 5-HT2拮抗剂,甲虫合剂(1 microm)或甲硫酸(0.1 microm)进行预处理,显着减弱了梭子对非胆管能收缩的抑制作用。用对象异(1 microm),5-HT3拮抗剂,ketanserin(10 microm),5-HT2拮抗剂,硫代酰胺(10 microm),组胺H3拮抗剂或芬兰胺(10 microM),α-肾上腺素能拮抗剂,但是,没有任何影响。在没有明显的5-HT受体结合亲和力的情况下,另一种组胺H1受体拮抗剂的另一种组胺H1受体拮抗剂不会产生任何抑制ENANC收缩。 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.