Löfdahl C G, Svedmyr N
Allergy. 1984 Aug;39(6):485-9. doi: 10.1111/j.1398-9995.1984.tb01973.x.
A new beta 2-adrenoceptor agonist D2343 has been shown in a human i.v. study to be less potent than terbutaline. Animal experiments showed an increased affinity to lung tissue and a longer bronchodilating effect than terbutaline when inhaled. In a randomized single-blind, crossover comparison, 2.5 and 5 mg D2343 and 5 mg terbutaline were inhaled by eight asthma patients. We found that 5 mg of D2343 was equipotent to 5 mg terbutaline in bronchodilatory effect measured with FEV1. The duration was longer with an increased bronchodilation (P less than 0.01) 6 h after D2343 inhalation compared with terbutaline. The mean fall in FEV1 3-6 h after inhalation was significantly greater with terbutaline than with D2343 (P less than 0.05). Thus, this study shows that inhaled D2343 has a longer bronchodilating effect than terbutaline.
一项人体静脉注射研究表明,新型β2肾上腺素能受体激动剂D2343的效力低于特布他林。动物实验显示,吸入时D2343对肺组织的亲和力增加,支气管扩张作用比特布他林更持久。在一项随机单盲交叉对照试验中,8名哮喘患者分别吸入2.5毫克和5毫克的D2343以及5毫克的特布他林。我们发现,就用第一秒用力呼气量(FEV1)衡量的支气管扩张作用而言,5毫克的D2343与5毫克的特布他林等效。与特布他林相比,吸入D2343 6小时后,支气管扩张作用增强(P<0.01),且持续时间更长。吸入后3至6小时,特布他林导致的FEV1平均下降幅度显著大于D2343(P<0.05)。因此,本研究表明,吸入D2343的支气管扩张作用比特布他林更持久。