Relationship between 3H-histamine uptake and H2-receptors in the human promyelocytic leukemia cell line HL-60.
Association of 3H-histamine (3H-H) with HL-60 cells was a time- and temperature-dependent process. At 37 degrees C, the association of 3H-H (50 fmole/10(6) cells) was maximal and constant 60 min after the addition of HL-60 cells, while there is no significant radioactivity associated with cells incubated at 4 degrees C during 120 min incubation. Under these conditions, the cell-associated radioactivity remains unchanged, even after a washout period and addition of large excess (10(-3) M) of histamine, indicating an irreversible interaction between histamine and HL-60 cells. The interaction of 3H-H with HL-60 cells depends on cell viability, cell concentration and was reduced by various metabolic inhibitors such as iodacetamide, dinitrophenol, sodium azide and ouabain. Histamine uptake by HL-60 cells was inhibited by a series of H1, H2 histamine agonists (impromidine, histamine, 4-MH, AET, PEA) and antagonists (cimetidine, oxmetidine, ranitidine, diphenhydramine), according to the following order of potencies: 1 greater than H, 4-MH greater than AET greater than PEA and H,C greater than DPH. Among the histamine analogs tested (acid N-acetyl histamine, imidazole, acid imidazole acetic and histidine), only the N-acetyl histamine acid was able to inhibit 3H-H uptake by HL-60 cells. Three antidepressant drugs (amitriptyline, imipramine, clomipramine) also antagonize 3H-H uptake by HL-60 cells, but this effect was only observed at toxic concentrations (10(-5) M and above) and was related to a loss of the cell viability.(ABSTRACT TRUNCATED AT 250 WORDS)
Gespach
C
C
Marrec
N
N
Balitrand
N
N
D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology; D001692:Biological Transport; D002460:Cell Line; D002470:Cell Survival; D006632:Histamine / Q000378:metabolism*; D006634:Histamine H1 Antagonists / Q000494:pharmacology; D006801:Humans; D015470:Leukemia, Myeloid, Acute / Q000378:metabolism*; D011968:Receptors, Histamine / Q000502:physiology*; D011970:Receptors, Histamine H2 / Q000187:drug effects / Q000502:physiology*; D014316:Tritium
D000929:Antidepressive Agents, Tricyclic; D006634:Histamine H1 Antagonists; D011968:Receptors, Histamine; D011970:Receptors, Histamine H2; D014316:Tritium; D006632:Histamine