Costa J L, Murphy D L, Reveille J
Br J Pharmacol. 1977 Oct;61(2):223-8. doi: 10.1111/j.1476-5381.1977.tb08408.x.
1 The uptake of various 3H-labelled amines into a thrombin-releasable compartment of human platelets, thought to represent the platelet vesicular storage pool, has been evaluated. Measurable amounts of 5-hydroxytryptamine (5-HT), dopamine, tyramine, octopamine, and tryptamine accumulate in this pool, and also in a non-thrombin-releasable (cytoplasmic) pool during a 30 min incubation period with 10(-5) M extracellular amine concentrations. 2 No differences in the accumulation of vesicular or cytoplasmic 5-HT, dopamine, and tyramine are found in platelets treated with deprenyl to inhibit platelet monoamine oxidase as compared to controls. 3 Extracellular tyramine or dopamine in concentrations as high as 10(-5) M does not alter the initial rate of 5-HT uptake across the platelet plasma membrane. Similarly, sizable cytoplasmic pools of either amine do not alter the initial rate at which small amounts of 5-HT enter platelet cytoplasm or storage vesicles. 5-HT thus appears to be the preferred substrate for uptake into platelets and for movement from cytoplasm to vesicles.
已对各种³H标记胺类进入人血小板中可被凝血酶释放的区室(被认为代表血小板囊泡储存池)的摄取情况进行了评估。在细胞外胺浓度为10⁻⁵ M的30分钟孵育期内,可测量量的5-羟色胺(5-HT)、多巴胺、酪胺、章鱼胺和色胺积聚在这个池中,也积聚在不可被凝血酶释放的(细胞质)池中。
与对照组相比,用司来吉兰处理以抑制血小板单胺氧化酶的血小板中,囊泡或细胞质中的5-HT、多巴胺和酪胺的积聚没有差异。
浓度高达10⁻⁵ M的细胞外酪胺或多巴胺不会改变5-HT跨血小板质膜摄取的初始速率。同样,这两种胺类相当大的细胞质池也不会改变少量5-HT进入血小板细胞质或储存囊泡的初始速率。因此,5-HT似乎是进入血小板以及从细胞质转运到囊泡的首选底物。