Knowles C O, Johnson T L
Toxicology. 1984 May 14;31(2):91-8. doi: 10.1016/0300-483x(84)90001-5.
Uptake of radioactive 5-hydroxytryptamine (5-HT) by platelets from rats treated intraperitoneally with the insecticide/acaricide chlordimeform (CDF) at 25 mg/kg was not significantly influenced at 1 h; however, uptake of this amine by platelets from rats treated with its N- monodemethyl metabolite (DMC) at the same dosage was significantly inhibited (37%). Two reversed phase high performance liquid chromatographic systems with electrochemical detection were developed with a capacity to separate 11 biogenic amines and related compounds. Only 5-HT, norepinephrine (NE), dopamine (DA), and 3,4-dihydroxyphenylacetic acid (DOPAC) were consistently detected in platelets and plasma samples. At 1 h and/or 24 h postinjection, CDF effected significant decreases in platelet levels of 5-HT, NE, and DA and plasma levels of 5-HT, whereas platelet and plasma levels of DOPAC were significantly increased. DMC effected significant decreases in both platelet and plasma levels of 5-HT. These in vivo studies confirmed previous in vitro experiments which demonstrated that formamidines inhibited uptake of 5-HT by platelets and released endogenous stores of amines from platelets.
腹腔注射剂量为25mg/kg的杀虫剂/杀螨剂杀虫脒（CDF）后1小时，大鼠血小板对放射性5-羟色胺（5-HT）的摄取未受到显著影响；然而，以相同剂量用其N-单去甲基代谢物（DMC）处理的大鼠血小板对这种胺的摄取受到显著抑制（37%）。开发了两种具有电化学检测功能的反相高效液相色谱系统，能够分离11种生物胺及相关化合物。在血小板和血浆样本中仅持续检测到5-HT、去甲肾上腺素（NE）、多巴胺（DA）和3,4-二羟基苯乙酸（DOPAC）。注射后1小时和/或24小时，CDF使血小板中5-HT、NE和DA的水平以及血浆中5-HT的水平显著降低，而血小板和血浆中DOPAC的水平显著升高。DMC使血小板和血浆中5-HT的水平均显著降低。这些体内研究证实了先前的体外实验，即甲脒类化合物抑制血小板对5-HT的摄取并从血小板中释放内源性胺储备。
