Johnson T L, Knowles C O
Toxicol Lett. 1981 Sep;9(1):1-4. doi: 10.1016/0378-4274(81)90166-1.
Chlordimeform, a formamidine insecticide and acaricide, and two of its toxic N-demethyl metabolites inhibited rat blood platelet 5-hydroxytryptamine (5-HT) uptake. A direct relationship existed between formamidine uptake inhibitory potency and N-demethylation. Didemethylchlordimeform, the most potent formamidine inhibitor of 5-HT uptake examined, had a pI50 of 4.2. However, it was appreciably less active than the classical inhibitor imipramine, which yielded 86.4% inhibition of 5-HT uptake at a concentration of 1.10(-5) M.
杀虫脒，一种脒类杀虫剂和杀螨剂，及其两种有毒的N-去甲基代谢物抑制大鼠血小板对5-羟色胺（5-HT）的摄取。脒类摄取抑制效力与N-去甲基化之间存在直接关系。双去甲基杀虫脒，在所检测的5-HT摄取的最有效的脒类抑制剂，其半数抑制浓度（pI50）为4.2。然而，它的活性明显低于经典抑制剂丙咪嗪，丙咪嗪在浓度为1.10(-5) M时对5-HT摄取的抑制率为86.4%。
