Toth L A, Elchisak M A
J Pharmacol Exp Ther. 1987 Feb;240(2):359-63.
Human platelets accumulate dopamine (DA) from the incubation medium in vitro and convert a significant percentage of the accumulated DA to dopamine sulfate (DAS). Platelet content of both DA and DAS increased linearly with incubation time and tissue concentration. Increasing the concentration of DA in the incubation medium also increased platelet content of both DA and DAS. However, after prolonged incubation times or in the presence of high concentrations of DA, the percentage conversion of DA to DAS decreased; this decrease was reversed at least partially by incubation in the presence of sodium sulfate, suggesting that sulfate availability may limit sulfoconjugation under some conditions. Incubation with fluoxetine produced a concentration-dependent decrease in both DA and DAS content of the platelets. In contrast, the agent 2,6-dichloro-4-nitrophenol, an inhibitor of the enzyme phenol sulfotransferase, did not interfere with DA uptake, but did inhibit DAS formation in a concentration-dependent manner. These studies suggest that the human platelet may represent a useful model system for the study of factors regulating DA sulfoconjugation.
人血小板在体外可从孵育培养基中积累多巴胺(DA),并将相当比例的积累的DA转化为硫酸多巴胺(DAS)。DA和DAS的血小板含量均随孵育时间和组织浓度呈线性增加。增加孵育培养基中DA的浓度也会增加血小板中DA和DAS的含量。然而,长时间孵育后或在高浓度DA存在的情况下,DA向DAS的转化百分比降低;在硫酸钠存在下孵育至少可部分逆转这种降低,这表明在某些条件下硫酸根的可用性可能会限制硫酸结合作用。用氟西汀孵育会使血小板的DA和DAS含量呈浓度依赖性降低。相比之下,酚磺基转移酶抑制剂2,6-二氯-4-硝基苯酚不干扰DA摄取,但以浓度依赖性方式抑制DAS的形成。这些研究表明,人血小板可能是研究调节DA硫酸结合作用因素的有用模型系统。