caa a22 4500 477057640 CHVBK 20180405111351.0 cr unu---uuuuu 170330e19960701xx s 000 0 eng 10.1007/s002280050126 doi (NATIONALLICENCE)springer-10.1007/s002280050126 Antimuscarinic effect of tiquizium bromide in vitro and in vivo [Elektronische Daten] [T. Shioya, M. Kagaya, M. Sano, M. Itaba, T. Shindo, M. Miura] Objective: We studied the bronchodilatory effect of tiquizium bromide [3-(di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide; TQZ], an antimuscarinic agent, on airway smooth muscle in vitro, and also in patients with chronic obstructive pulmonary disease (COPD). Methods: In the first experiment, canine tracheal smooth muscle was used to measure the pA2 of TQZ in vitro. The selectivity of TQZ for muscarinic receptor subtypes was also examined with a radioligand binding assay. Results: The pA2 value of TQZ was 8.75. The pK i values of TQZ for M1, M2, and M3 were 8.70, 8.94, and 9.11, respectively. In an open pilot experiment, the effects of TQZ inhalation were studied in seven patients with COPD (seven men, mean age 68.5 years). TQZ significantly increased forced vital capacity (FVC) and forced expiratory volume in 1 s (FEV1) in a dose-dependent manner. The mean maximum increases in FVC and FEV1 caused by inhaled TQZ (2.0 mg) were 24% and 29%, respectively, and they were measured 1 h after the drug had been inhaled. The FVC and FEV1 were still significantly higher than the control values even 8 h after the drug had been inhaled. No adverse effects were observed after inhalation of TQZ. Conclusion: These data suggest that TQZ is an effective antimuscarinic agent, and that it causes significant bronchodilation in patients with COPD. Springer-Verlag Berlin Heidelberg, 1996 Key words Tiquizium bromide nationallicence Muscarinic receptor subtype nationallicence Chronic obstructive pulmonary disease nationallicence airway smooth muscle nationallicence antimuscarinic agent nationallicence Shioya T. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Kagaya M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Sano M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Itaba M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Shindo T. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Miura M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut https://doi.org/10.1007/s002280050126 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050126 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Shioya T. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut NATIONALLICENCE 700 1- Kagaya M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut NATIONALLICENCE 700 1- Sano M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut NATIONALLICENCE 700 1- Itaba M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut NATIONALLICENCE 700 1- Shindo T. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut NATIONALLICENCE 700 1- Miura M. Second Department of Internal Medicine, Akita University School of Medicine, 1-1-1 Hondo, Akita 010, Japan aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer