Effect of a potent selective protein kinase C inhibitor on histamine release from rat mast cells.
3,10-Dihydroxy-10-[(dimethylamino)methyl]-2,3,9,10,11,12-hexahydro-9- methyl-9,12-epoxy-1H-diindolo[1,2,3-fg-3',2',1'-k1]pyrrolo[3,4- l][1,6]benzodiazocin-1-one (UCN-01) strongly and dose-dependently inhibited histamine release from rat peritoneal mast cells that was induced by anti-immunoglobulin E (anti-IgE), calcimycin (A 23187), and 1,2-o-tetradecanoyl-13-acetate (TPA). The concentrations of UCN-01 required for 50% inhibition of histamine release induced by anti-IgE, A23187, and TPA were 1.5, 2.7, and 1.4 nM, respectively; these values are similar to those for 50% inhibition of protein kinase C. These results suggest possible participation cells induced by various secretagogues.
Takei
M
M
La Jolla Institute for Allergy & Immunology, CA 92037.
Endo
K
K
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000001:Calcimycin / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D007073:Immunoglobulin E / Q000276:immunology; D066298:In Vitro Techniques; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D051381:Rats; D019311:Staurosporine / Q000031:analogs & derivatives; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology
D000470:Alkaloids; D007073:Immunoglobulin E; D000001:Calcimycin; C054852:7-hydroxystaurosporine; D011493:Protein Kinase C; D019311:Staurosporine; D013755:Tetradecanoylphorbol Acetate