Histamine H2 receptor desensitization in HL-60 human promyelocytic leukemia cells
Sawutz, D.G.; Kalinyak, K.; Whitsett, J.A.; Johnson, C.L.
Journal of Pharmacology and Experimental Therapeutics 231(1): 1-7
1984
ISSN/ISBN: 0022-3565 PMID: 6208354 Document Number: 221205
Recent studies have suggested that cAMP may be involved in regulation of cell growth and differentiation of cancer cells. Incubating HL-60 cells in the presence of the specific H2 agonist dimaprit resulted in 30-fold increases in cAMP levels (EC50 tiotidine binding sites was observed between control and dimaprit-desensitized HL-60 cells. Evidently, H2 receptor agonists caused an agonist-dependent desensitization, presumably due to an uncoupling of receptors from adenylate cyclase. Despite the rapid desensitization of the H2 response, dimaprit did induce the cellular maturation of HL-60, suggesting a possible role for endogenous histamine in the regulation of growth and differentiation of the myelogenous cell.