Ono T, Ohtsuka M, Sakai S, Ohno S, Kumada S
Jpn J Pharmacol. 1977 Dec;27(6):889-98. doi: 10.1254/jjp.27.889.
The interrelation of the inhibitory effect of aspirin-like drugs on the resting tonus of tracheal chain in guinea pigs, arachidonic acid-induced contraction in rat stomach fundus strips and bradykinin-induced bronchoconstriction in guinea pigs in vivo was investigated. All the drugs tested produced a dose-related inhibitory action on the resting tonus of the tracheal chain in comparatively low doses. Diclofenac was the most potent of all the drugs and was equal in activity to isoproterenol, followed in descending order by flufenamic acid, mefenamic acid, indomethacin, ibuprofen, phenylbutazone, oxyphenbutazone and aspirin. These aspirin-like drugs also inhibited arachidonic acid-induced contraction in rat stomach fundus strips. A highly significant correlation was observed between the potency of inhibition of the arachidonic acid-induced contraction and the relaxant effect on the tracheal chain. Moreover, the drugs antagonized bradykinin-induced bronchoconstriction in guinea pigs in vivo and the order of potency roughly paralleled that of the tracheal chain. These results suggest that the aspirin-like drugs produce a reduction in resting tonus of the isolated guinea pig tracheal chain by inhibition of intramural biosynthesis of prostaglandin endoperoxides.
研究了阿司匹林类药物对豚鼠气管链静息张力的抑制作用、对大鼠胃底条花生四烯酸诱导收缩的影响以及对豚鼠体内缓激肽诱导支气管收缩的影响之间的相互关系。所有受试药物在相对低剂量时均对气管链的静息张力产生剂量相关的抑制作用。双氯芬酸是所有药物中作用最强的，其活性与异丙肾上腺素相当，其次依次为氟芬那酸、甲芬那酸、吲哚美辛、布洛芬、保泰松、羟布宗和阿司匹林。这些阿司匹林类药物也抑制大鼠胃底条花生四烯酸诱导的收缩。在抑制花生四烯酸诱导收缩的效力与对气管链的松弛作用之间观察到高度显著的相关性。此外，这些药物在豚鼠体内拮抗缓激肽诱导的支气管收缩，其效力顺序大致与气管链的情况平行。这些结果表明，阿司匹林类药物通过抑制壁内前列腺素内过氧化物的生物合成，使离体豚鼠气管链的静息张力降低。
