Malmgren R
Psychopharmacology (Berl). 1984;84(4):480-5. doi: 10.1007/BF00431453.
The uptake of 14C-dopamine (DA) by human platelets at 10(-7) -2.5 X 10(-4) M of labelled amine concentration was studied in human platelet-rich plasma. The total uptake could be resolved into two components, one of which was saturable and completely inhibited by 10(-5) imipramine and another which was unsaturable but temperature-dependent. The saturable uptake of DA had an apparent Km of 75 X 10(-6) M and Vmax of 1.34 pmol/10(6) platelets/min. The uptake of unsaturable DA was 1.33 pmol/10(6) platelets/min at 10(-4) M DA. Dopamine exerted a mixed non-competitive inhibition of the saturable 5-HT transport and vice versa. Thus the increase in Km was paralleled by a decrease in Vmax. The low-affinity transport of DA by the human platelets does not share any of the dopamine uptake characteristics found in neuronal tissue. The platelet therefore seems to be a poor model for the presynaptic function of the dopamine neurons.
在富含人血小板的血浆中,研究了在10^(-7)-2.5×10^(-4)M标记胺浓度下,人血小板对14C-多巴胺(DA)的摄取情况。总摄取可分为两个部分,其中一个部分可饱和,且被10^(-5)丙咪嗪完全抑制,另一个部分不饱和但依赖温度。DA的可饱和摄取的表观Km为75×10^(-6)M,Vmax为1.34 pmol/10^6个血小板/分钟。在10^(-4)M DA时,不饱和DA的摄取为1.33 pmol/10^6个血小板/分钟。多巴胺对可饱和的5-羟色胺转运产生混合非竞争性抑制,反之亦然。因此,Km的增加与Vmax的降低平行。人血小板对DA的低亲和力转运不具有在神经组织中发现的任何多巴胺摄取特征。因此,血小板似乎不是多巴胺神经元突触前功能的良好模型。