Kohno S W, Hashii H, Ogino K, Yamamura H, Ohata K
Department of Pharmacology, Kyoto Pharmaceutical University, Japan.
Jpn J Pharmacol. 1989 Aug;50(4):455-66. doi: 10.1254/jjp.50.455.
Effects of oxitropium bromide (Ba253), which was administered by inhalation, on the resting and stimulus-induced airway resistance were examined in the artificially ventilated guinea pig and compared with those of ipratropium bromide (Sch1000), atropine and isoproterenol. Results obtained were as follows: 1) Ba253 as well as other reference compounds hardly affected the resting resistance. 2) Ba253 strongly and persistently inhibited the acetylcholine (ACh)-induced resistance. Sch1000 caused a similar but relatively weaker inhibition than Ba253. Either atropine or isoproterenol caused only a transient inhibition. 3) The increase in resistance induced by histamine, serotonin, leukotriene D4 or antigen was prevented by Ba253. Atropine, Sch1000 and isoproterenol also inhibited these reactions, but the effects and the duration were generally weaker and shorter than those of Ba253. 4) Repeated inhalations of Ba253 for 7 days did not influence the inhibition of the ACh-induced increase in airway resistance by this drug. However, isoproterenol tended to attenuate the suppression of the resistance by the drug. From these results, it is suggested that Ba253 is a useful inhalant drug for asthma.
在人工通气的豚鼠中,研究了吸入用氧托溴铵(Ba253)对静息和刺激诱导的气道阻力的影响,并与异丙托溴铵(Sch1000)、阿托品和异丙肾上腺素进行了比较。结果如下:1)Ba253与其他参比化合物一样,对静息阻力几乎没有影响。2)Ba253强烈且持续地抑制乙酰胆碱(ACh)诱导的阻力。Sch1000产生了类似的抑制作用,但比Ba253相对较弱。阿托品或异丙肾上腺素仅引起短暂抑制。3)Ba253可防止组胺、5-羟色胺、白三烯D4或抗原诱导的阻力增加。阿托品、Sch1000和异丙肾上腺素也抑制这些反应,但效果和持续时间通常比Ba253弱且短。4)连续7天重复吸入Ba253不会影响该药物对ACh诱导的气道阻力增加的抑制作用。然而,异丙肾上腺素倾向于减弱该药物对阻力的抑制作用。从这些结果表明,Ba253是一种用于哮喘的有用吸入药物。