Indacaterol is a novel beta2-adrenoceptor agonist in development for the once-daily treatment of asthma and chronic obstructive pulmonary disease. The present study evaluated the relaxant effect of indacaterol on isolated human bronchi obtained from lungs of patients undergoing surgery for lung carcinoma. Potency (-logEC50), maximal relaxant effect (Emax) and onset of action were determined at resting tone. Duration of action was determined against cholinergic neural contraction induced by electrical field stimulation (EFS). At resting tone, -logEC50 and Emax values were 8.82+/-0.41 and 77+/-5% for indacaterol, 9.84+/-0.22 and 94+/-1% for formoterol, 8.36+/-0.16 and 74+/-4% for salmeterol, and 8.43+/-0.22 and 84+/-4% for salbutamol, respectively. In contrast to salmeterol, indacaterol did not antagonise the isoprenaline response. Indacaterol's onset of action (7.8+/-0.7 min) was not significantly different from that of formoterol (5.8+/-0.7 min) or salbutamol (11.0+/-4.0 min), but it was significantly faster than that of salmeterol (19.4+/-4.3 min). EFS-induced contractions were inhibited with -logIC50 values of 6.96+/-0.13 (indacaterol), 8.96+/-0.18 (formoterol), 7.18+/-0.34 (salmeterol) and 6.39+/-0.26 (salbutamol). Duration of action was >12 h for indacaterol and salmeterol, and 35.3+/-8.8 and 14.6+/-3.7 min for formoterol and salbutamol, respectively. In isolated human bronchi, indacaterol behaved as a long-acting beta2-adrenoceptor agonist with high intrinsic efficacy and fast onset of action.

译文

:茚达特罗是一种新型的β2-肾上腺素受体激动剂,正在开发中,用于每日一次治疗哮喘和慢性阻塞性肺疾病。本研究评估了茚达特罗对从接受肺癌手术的患者的肺中分离出的人支气管的舒张作用。在静息时测定效力(-logEC 50),最大松弛作用(E max)和作用开始。确定作用持续时间以抵抗电场刺激(EFS)诱导的胆碱能神经收缩。在静息状态下,茚达特罗的-logEC50和Emax值为8.82 /-0.41和77 / -5%,福莫特罗为9.84 /-0.22和94 / -1%,沙美特罗为8.36 /-0.16和74 / -4%,以及沙丁胺醇分别为8.43 /-0.22和84 / -4%。与沙美特罗相反,茚达特罗没有拮抗异丙肾上腺素的反应。茚达特罗的起效时间(7.8 /-0.7分钟)与福莫特罗(5.8 /-0.7分钟)或沙丁胺醇(11.0 /-4.0分钟)的起效没有显着差异,但显着快于沙美特罗(19.4 /-4.3)分钟)。 EFS诱导的收缩受到抑制,其-logIC50值分别为6.96 /-0.13(茚达特罗),8.96 /-0.18(福莫特罗),7.18 /-0.34(沙美特罗)和6.39 /-0.26(沙丁胺醇)。茚达特罗和沙美特罗的作用时间> 12 h,福莫特罗和沙丁胺醇的作用时间分别为35.3 /-8.8和14.6 /-3.7分钟。在分离的人支气管中,茚达特罗表现为一种长效的β2肾上腺素受体激动剂,具有很高的内在功效和起效快。

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