Johnson T L, Knowles C O
Gen Pharmacol. 1985;16(4):321-5. doi: 10.1016/0306-3623(85)90190-9.
The formamidine pesticide chlordimeform (CDF) was a strong inhibitor of aggregation of rat platelets induced by collagen and arachidonic acid and was a weak inhibitor of that induced by ADP. With the exception of 4-chloro-o-formotoluidide which was an inhibitor of arachidonic acid-induced aggregation only, the CDF metabolites were without discernible effect on aggregation induced by these agents. Amitraz, another formamidine pesticide, inhibited arachidonic acid-induced aggregation but was without effect on that induced by collagen or ADP. Inhibition of collagen- and/or arachidonic acid-induced aggregation by formamidines was concentration-dependent. Although platelets underwent shape change, primary aggregation was markedly inhibited, and secondary aggregation was abolished in some cases. CDF, its two N-desmethyl metabolites, and octopamine, but not amitraz, caused significantly elevated levels of cyclic AMP in platelet rich plasma as compared to controls; however, this effect did not fully account for the action of formamidines on aggregation.
甲脒类杀虫剂杀虫脒（CDF）是胶原蛋白和花生四烯酸诱导的大鼠血小板聚集的强抑制剂，是ADP诱导的血小板聚集的弱抑制剂。除了仅为花生四烯酸诱导聚集抑制剂的4-氯邻甲酰甲苯胺外，CDF代谢产物对这些试剂诱导的聚集没有明显影响。另一种甲脒类杀虫剂双甲脒抑制花生四烯酸诱导的聚集，但对胶原蛋白或ADP诱导的聚集没有影响。甲脒类对胶原蛋白和/或花生四烯酸诱导的聚集的抑制作用是浓度依赖性的。虽然血小板发生了形态变化，但初级聚集受到明显抑制，在某些情况下二级聚集被消除。与对照组相比，CDF及其两种N-去甲基代谢产物以及去甲肾上腺素能使富含血小板血浆中的环磷酸腺苷水平显著升高；然而，这种作用并不能完全解释甲脒类对聚集的作用。
