Platelet activating factor-amidophosphonate (PAF-AP), a partial agonist inhibited platelet activating factor-induced calcium mobilization in human monocytic leukemic U-937 cell.
Differentiated human monocytic leukemic U-937 cells express platelet activating factor (PAF) receptor and produce intracellular messengers for this receptor. A structural analog, PAF-AP, functioned as a partial agonist that can activate PAF receptor and receptor mediated signal transduction. This partial agonist inhibited and cross-desensitized full agonist (PAF) induced intracellular calcium mobilization. These observations are further support that phosphoinositide hydrolysis and intracellular calcium mobilization function as the major signal transduction mechanism for PAF receptors in U-937 cells.
Barzaghi
G
G
Department of Immunology, Smith Kline & French Laboratories, King of Prussia, PA 19406-0939.
Mong
S
S
D002118:Calcium / Q000378:metabolism*; D002460:Cell Line; D006801:Humans; D007951:Leukemia, Myeloid; D010716:Phosphatidylinositols / Q000378:metabolism; D010972:Platelet Activating Factor / Q000031:analogs & derivatives* / Q000494:pharmacology; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D043562:Receptors, G-Protein-Coupled; D015398:Signal Transduction
D010716:Phosphatidylinositols; D010972:Platelet Activating Factor; D010980:Platelet Membrane Glycoproteins; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; C039351:platelet activating factor receptor; C047125:platelet activating factor-amidophosphonate; D002118:Calcium