Corbel S, Dy M
CNRS URA 1461, Hôpital Necker, Paris, France.
FEBS Lett. 1996 Aug 12;391(3):279-81. doi: 10.1016/0014-5793(96)00741-7.
Murine hematopoietic progenitor cells synthesize substantial amounts of histamine in response to IL-3 or calcium ionophore. They also take up extracellular histamine by an active transport system. In the present study we demonstrate that this system mediates both influx and efflux of histamine. Indeed, MR16155 and thioperamide, the two H3 antagonists which are most effective in inhibiting histamine uptake, likewise diminish the release of preloaded histamine from bone marrow cells. These compounds also inhibit the release of histamine which has been newly synthesized by hematopoietic progenitors in response to IL-3 or calcium ionophore, as assessed by the accumulation of the mediator inside the cells in the presence of the antagonists. The potency of different histamine receptor antagonists as inhibitors of histamine release increases with their capacity to block histamine uptake.
小鼠造血祖细胞在受到白细胞介素-3或钙离子载体刺激时会合成大量组胺。它们还通过主动转运系统摄取细胞外组胺。在本研究中，我们证明该系统介导组胺的流入和流出。事实上，MR16155和硫代哌酰胺这两种在抑制组胺摄取方面最有效的H3拮抗剂，同样会减少骨髓细胞中预加载组胺的释放。这些化合物还抑制造血祖细胞响应白细胞介素-3或钙离子载体新合成的组胺的释放，这通过在拮抗剂存在的情况下细胞内介质的积累来评估。不同组胺受体拮抗剂作为组胺释放抑制剂的效力随着它们阻断组胺摄取的能力而增加。
