Fontaine J, Famaey J P, Reuse J
Naunyn Schmiedebergs Arch Pharmacol. 1980 Aug;313(2):165-70. doi: 10.1007/BF00498575.
Amodiaquine (3.5 . 10(-7) mol/l), a 4-amino-quinoline antimalarial, increases the responses of the guinea-pig isolated ileum to direct (acetylcholine, histamine, barium, chloride), partially (5-hydroxytryptamine, PGE1 and F2 alpha) and totally (electrical stimulations, nicotine) indirect agonists. Moreover it reverses inhibitions of the electrical induced contractions by acetylcholine antagonists (atropine), acetylcholine release blocking agents (morphine, tetrodotoxin, procaine, noradrenaline) and prostaglandin synthesis inhibitors (indomethacin, ibuprofen, flufenamine acid, hydrocortisone). From 2.7 . 10(-6) mol/l, it induces dose-related tonic contractions which are totally and reversibly abolished by indomethacin as well as by the prostaglandin antagonist, polyphloretin phosphate, but not by atropine, morphine and tetrodotoxin. This indicates that amodiaquine exerts both a direct muscular non selective ileal sensitization to various agonists and, but at higher concentrations, a contractile effect apparently dependent on prostaglandin synthesis and release. At even higher concentrations (5.4 . 10(-6) mol/l) an effect of amodiaquine on acetylcholine release was demonstrated by the observation of phasic contractions inhibited by atropine, morphine and tetrodotoxin. These effects are different from those found by us with several other antimalarial compounds in the same preparation.
阿莫地喹（3.5×10⁻⁷摩尔/升），一种4-氨基喹啉类抗疟药，可增强豚鼠离体回肠对直接激动剂（乙酰胆碱、组胺、钡、氯化物）、部分间接激动剂（5-羟色胺、前列腺素E1和F2α）以及完全间接激动剂（电刺激、尼古丁）的反应。此外，它可逆转乙酰胆碱拮抗剂（阿托品）、乙酰胆碱释放阻断剂（吗啡、河豚毒素、普鲁卡因、去甲肾上腺素）和前列腺素合成抑制剂（吲哚美辛、布洛芬、氟芬那酸、氢化可的松）对电诱导收缩的抑制作用。从2.7×10⁻⁶摩尔/升起，它可诱导剂量相关的强直性收缩，吲哚美辛以及前列腺素拮抗剂多聚磷酸根皮素可完全且可逆地消除这种收缩，但阿托品、吗啡和河豚毒素则不能。这表明阿莫地喹既对各种激动剂产生直接的、非选择性的回肠肌肉致敏作用，又在较高浓度时产生一种显然依赖于前列腺素合成和释放的收缩作用。在更高浓度（5.4×10⁻⁶摩尔/升）时，通过观察阿托品、吗啡和河豚毒素抑制的相性收缩，证明了阿莫地喹对乙酰胆碱释放的影响。这些作用与我们在同一制剂中使用其他几种抗疟化合物所发现的作用不同。
