Corbel S, Traiffort E, Stark H, Schunack W, Dy M
CNRS URA 1461, Hôpital Necker, Paris, France.
FEBS Lett. 1997 Mar 10;404(2-3):289-93. doi: 10.1016/s0014-5793(97)00142-7.
Hematopoietic progenitor cells can take up histamine or release IL-3-induced histamine through a bi-directional transport system that is blocked by H3-receptor antagonists. In the present study we demonstrate a correlation between the affinity of various H3-receptor antagonists and their potency as inhibitors of histamine uptake. All compounds that blocked histamine uptake also inhibited IL-3-induced histamine release. Yet, classical H3 receptors are not involved in this biological activity, since highly specific histamine H3-receptor agonists neither alter histamine uptake nor affect the release of endogenous histamine synthesized in response to IL-3. Furthermore, the inhibitory effect of H3-receptor antagonists on histamine uptake was not reversed by the agonists. Unlike H3-receptor antagonists, the agonists did not displace the binding of the labeled antagonist iodoproxyfan.
造血祖细胞可通过一种被H3受体拮抗剂阻断的双向转运系统摄取组胺或释放白细胞介素-3诱导的组胺。在本研究中，我们证明了各种H3受体拮抗剂的亲和力与其作为组胺摄取抑制剂的效力之间存在相关性。所有阻断组胺摄取的化合物也抑制白细胞介素-3诱导的组胺释放。然而，经典的H3受体并不参与这种生物学活性，因为高度特异性的组胺H3受体激动剂既不改变组胺摄取，也不影响响应白细胞介素-3合成的内源性组胺的释放。此外，H3受体拮抗剂对组胺摄取的抑制作用不会被激动剂逆转。与H3受体拮抗剂不同，激动剂不会取代标记拮抗剂碘普罗芬的结合。
