Pharmacological characterization of the histamine uptake system in HL-60 human promyelocytic leukemia cells

Serotonin and histamine H1, H2 receptor agonists or antagonists inhibited [3H]histamine uptake by HL-60 cells, according to the following order of potency: impromidine greater than 4-MH greater than histamine greater than AET greater than PEA and: cimetidine, histamine greater than diphenhydramine, serotonin. It is concluded that histamine uptake by HL-60 cells was specifically controlled by the H2 type histamine receptor and that this active process might be involved in pathophysiological regulations in leukemic and normal granulocytic precursors and in the control of histamine levels in peripheral blood and tissues in man.