Tagaya E, Tamaoki J, Takemura H, Chiyotani A, Konno K
First Department of Medicine, Tokyo Women's Medical College.
Kansenshogaku Zasshi. 1995 Apr;69(4):404-7. doi: 10.11150/kansenshogakuzasshi1970.69.404.
To elucidate whether the new quinolone ciprofloxacin affects cholinergic neuto-effector transmission in the airway, we studied canine isolated bronchial segments under isometric conditions in vitro. Intrapulmonary lobar or segmental bronchi were suspended in the organ chambers filled with Krebs-Henseleit solution, and the isometric tension was continuously recorded by a force-displacement transducer. Addition of ciprofloxacin (2 x 10(-3) M) attenuated the contractile responses to electrical field stimulation (EFS), so that the stimulus frequency required to produce a half-maximal contraction (ES50) increased from 1.2 +/- 0.2 to 1.5 +/- 0.2 Hz (p < 0.05), whereas it was without effect on those to exogenously administered acetylcholine. The decrease in the EFS-induced contraction produced by ciprofloxacin was concentration-dependent and was not influenced by propranolol or tetraethylammonium, but partially inhibited by ouabain. These results suggest that ciprofloxacin may inhibit cholinergic neuro-effector transmission in the airway smooth muscle by inhibiting the exocytotic release of acetylcholine, probably involving the stimulation of Na(+)-K(+)-ATPase and concomitant repolarization/hyperpolarization of cholinergic nerve terminals.
为阐明新型喹诺酮类药物环丙沙星是否影响气道中的胆碱能神经效应器传递,我们在体外等长条件下研究了犬离体支气管节段。肺内叶支气管或段支气管悬浮于充满克雷布斯-亨塞尔特溶液的器官浴槽中,等长张力由力-位移换能器连续记录。加入环丙沙星(2×10⁻³ M)减弱了对电场刺激(EFS)的收缩反应,使得产生半数最大收缩所需的刺激频率(ES50)从1.2±0.2 Hz增加至1.5±0.2 Hz(p<0.05),而对给予外源性乙酰胆碱的反应无影响。环丙沙星引起的EFS诱导收缩的降低呈浓度依赖性,不受普萘洛尔或四乙铵影响,但部分受哇巴因抑制。这些结果提示,环丙沙星可能通过抑制乙酰胆碱的胞吐释放来抑制气道平滑肌中的胆碱能神经效应器传递,这可能涉及对Na⁺-K⁺-ATP酶的刺激以及胆碱能神经末梢随之发生的复极化/超极化。