1967 年 87 巻 4 号 p. 370-375
Antispasmodic action was examined in 67 kinds of basic amides and alkamine esters of alkoxybenzoic acid, using the excised intestine of male mice and by the Magnus method. In general, these compounds had a strong papaverine-like action and some of the basic amides showed atropine-like activity. The compound with a strong antispasmodic activity, 3-bromo4-butoxybenzoic acid dibutylaminoethylamide (PA-1), was examined by the Magnus method, using mouse intestine and it was found that the anti-barium chloride action of PA-1 was 3.94 times that of papaverine and that its anti-acetylcholine action was 0.0071 times that of atropine. PA-1 has a marked inhibitory action on rabbit intestine in vivo and also has a surface anesthetic activity. In the circulating system, PA-1 acted inhibitorily against isolated heart of a toad but had no effect on the vascular system of a toad hind leg. PA-1 showed transitory fall of blood pressure in the dog. Acute toxicity of PA-1 was 218.5 mg./kg. by subcutaneous injection in mice.