Fontaine J, Reuse J J
Arch Int Pharmacodyn Ther. 1975 Feb;213(2):322-7.
Metoclopramide [(Mcp)-N-diethylaminoethyl-2-methoxy-4-amino-5-chloro-benzamide] was shown by the authors (This Journal 1973, 204, 239) to stimulate the isolated guinea-pig ileum, mainly by an indirecr cholinergic mechanism, to increase responses to acetylcholine (Ac) and transmural stimulation, and to inhibit responses to serotonin (5 HT) and histamine (H). Four structuraly related benzamide derivative (1211, 1265, 1308 and 1347) also stimutated the ileum, 1211 being the most active, and 1347 the least active, and resembled Mcp with regard to the responses to Ac, transmural stimulation and histamine. However, serotonin contractions were enhance by 1265 and 1347, while 1308 and 1211 were inhibitory. These observations suggest that a 4-amino group does not seem to be essential for the stimulant effect or the interference with Ac responses (1211, 1265, 1347), whereas a methylsulfonyl group (1347) and, to a lesser degree, a flour in 5 position (1265) sensitize the ileum towards 5 HT contractions.
作者（《本杂志》1973年，204卷，239页）发现，甲氧氯普胺[（Mcp）-N-二乙氨基乙基-2-甲氧基-4-氨基-5-氯苯甲酰胺]主要通过间接胆碱能机制刺激离体豚鼠回肠，增加对乙酰胆碱（Ac）和透壁刺激的反应，并抑制对5-羟色胺（5-HT）和组胺（H）的反应。四种结构相关的苯甲酰胺衍生物（1211、1265、1308和1347）也刺激回肠，其中1211活性最高，1347活性最低，在对Ac、透壁刺激和组胺的反应方面与甲氧氯普胺相似。然而，1265和1347增强了5-羟色胺收缩，而1308和1211则起抑制作用。这些观察结果表明，4-氨基对于刺激作用或对Ac反应的干扰（1211、1265、1347）似乎不是必需的，而甲磺酰基（1347）以及程度较轻的5位氟（1265）使回肠对5-HT收缩敏感。
