Yoshikawa S, Fukunaga Y, Takeuchi T, Nishio H, Hata F
Department of Veterinary Pharmacology, Osaka Prefectural University, Sakai, Japan.
Eur J Pharmacol. 1993 Aug 3;239(1-3):261-4. doi: 10.1016/0014-2999(93)91008-b.
Eicosatetraenoic acid, an inhibitor of 5- and 12-lipoxygenase, and AA861, a selective inhibitor of 5-lipoxygenase, dose dependently inhibited acetylcholine release from the myenteric plexus of guinea-pig ileum induced by electrical field stimulation. Metabolites of arachidonic acid produced by the 5-lipoxygenase pathway, such as 5-hydroxyeicosatetraenoic acid (5-HETE), leukotriene C4, D4 and E4, reversed the inhibitory effect of AA861. Among them, leukotriene D4 was the most potent, having an EC50 value of about 3 nM. The present study shows for the first time that 5-lipoxygenase metabolites may have a modulatory effect on acetylcholine release in the myenteric plexus of guinea-pig ileum.
二十碳四烯酸，一种5-和12-脂氧合酶的抑制剂，以及AA861，一种5-脂氧合酶的选择性抑制剂，呈剂量依赖性地抑制电场刺激诱导的豚鼠回肠肌间神经丛中乙酰胆碱的释放。由5-脂氧合酶途径产生的花生四烯酸代谢产物，如5-羟基二十碳四烯酸（5-HETE）、白三烯C4、D4和E4，可逆转AA861的抑制作用。其中，白三烯D4的作用最强，其EC50值约为3 nM。本研究首次表明，5-脂氧合酶代谢产物可能对豚鼠回肠肌间神经丛中乙酰胆碱的释放具有调节作用。
