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Chemical Compound Review

Calcimycin     5-methylamino-2- [[(2S,3R,5R,8S,9S)-3,5,9...

Synonyms: UPCMLD-DP093, SureCN258988, BSPBio_001576, KBioGR_000296, KBioSS_000296, ...
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Disease relevance of A 23187

  • Osteosarcoma cells transfected with 5-LO express active enzyme in broken cell preparations, but no leukotriene metabolites are produced by these cells when stimulated with the calcium ionophore A23187, indicating that an additional component is necessary for cellular 5-LO activity [1].
  • Endocytotic sucrose uptake in Amoeba proteus induced with the calcium ionophore A23187 [2].
  • Chemotactic migration and lysosomal enzyme release elicited by chemotactic factors were inhibited by pertussis toxin with a concentration-dependence similar to that for inhibition of the increase in [Ca2+]in, without an effect on lysosomal enzyme release induced by the ionophore A23187 and phorbol myristate acetate [3].
  • Isolated dog mastocytoma cells sensitized with dog anti-ragweed IgE and challenged with ragweed antigen or incubated with ionophore A23187 or the carboxy-terminal dodecapeptide of platelet factor 4, PF4(59-70), release histamine and concurrently generate leukotrienes B4, C4, and D4 [4].
  • We conclude that the ionophores A23187 or X537A do not stimulate bone resorption nor potentiate the effects of stimulators of bone resorption; instead they are inhibitors of bone resorption stimulated by a wide variety of compounds [5].

Psychiatry related information on A 23187

  • The degranulation response of human neutrophils to the calcium ionophore A23187, serum opsonized zymosan (ZC), aggregated gamma-globulin (A gamma G), C5a, formyl-methionyl-leucyl-phenylalanine (FMLP), and PMA has been studied as a reaction time course in order to compare the release kinetics of the separate granule types [6].
  • Application of calcium ionophore A-23187 significantly shortened the time required for reappearance of the startle reaction to a bright light [7].
  • Adult male rats were tested for the effects of A23187 on operant performance and general motor activity [8].

High impact information on A 23187

  • The completeness of 5-lipoxygenase inhibition was confirmed by examining the profile of eicosanoids produced in whole blood ex vivo after activation with the calcium ionophore A-23187 [9].
  • Finally, transcription of c-fos in A431 cells is markedly induced by the tumor promoter TPA and the calcium ionophore A23187, yet neither induced an increased level of the enhancer-binding activity [10].
  • In contrast, the vWf released by the calcium ionophore A23187 or thrombin consisted of only very large multimers of mature subunits [11].
  • The serine esterase activity is secreted by lymphocytes that have been stimulated with the calcium ionophore A23187 [12].
  • Rabbit alveolar macrophages did not respond to PMA but did respond to A23187 by increasing cell spreading, which was accompanied by increases on the cell surface of four different receptors [13].

Chemical compound and disease context of A 23187


Biological context of A 23187


Anatomical context of A 23187


Associations of A 23187 with other chemical compounds

  • Here we show in rat striatal slices that, although 3H-dopamine release evoked by depolarization with 40 mM K+ is inhibited by 50 mM ethanol, the release evoked by A23187 is enhanced by the presence of ethanol in vitro [28].
  • Two divalent cation ionophores, A23187 and Ionomycin, which are selective for calcium, stimulated the resorption of fetal rat long bones in organ culture at 0.1 to 1 micromolar but not at higher concentrations [29].
  • Purified human monocytes release and metabolize endogenous arachidonic acid (20:4) from phospholipid stores when challenged with particulate inflammatory stimuli or the calcium ionophore A23187 [30].
  • The Ca2+ ionophore A23187 caused cells in Na+-free medium to release and metabolize 20:4 to prostacyclin, PGE2, leukotriene C, and hydroxyeicosatetraenoic acids, suggesting that the phospholipase(s), cyclooxygenase, and lipoxygenase enzymes do not have a requirement for extracellular Na+ [31].
  • IL-8 was retained in these storage organelles for several days after the removal of the stimulus and could be released by EC secretagogues such as phorbol myristate acetate, the calcium ionophore A23187, and histamine [32].

Gene context of A 23187

  • However, A23187 and mAb T3-II further elevated TNF and LT mRNA accumulations in PMA-treated T cell lines [33].
  • Maximal accumulation of GM-CSF mRNA is observed after PDBu/A23187 stimulation [34].
  • Accumulation of CSF-1 mRNA is observed only in NK cells stimulated with both CD16 ligands and rIL-2, whereas accumulation of IL-3 mRNA is observed only in NK cells stimulated with PDBu/A23187 [34].
  • Biological activity of IL-3 and CSF-1 was demonstrable in supernatant fluids of NK cells stimulated with PDBu/A23187 and CD16 ligands/rIL-2, respectively [34].
  • Activation of T cells by antigen, lectin or a combination of phorbol ester (PMA) and calcium ionophore (A23187) leads to the induction of a set of lymphokine genes [35].

Analytical, diagnostic and therapeutic context of A 23187


  1. Identification and isolation of a membrane protein necessary for leukotriene production. Miller, D.K., Gillard, J.W., Vickers, P.J., Sadowski, S., Léveillé, C., Mancini, J.A., Charleson, P., Dixon, R.A., Ford-Hutchinson, A.W., Fortin, R. Nature (1990) [Pubmed]
  2. Endocytotic sucrose uptake in Amoeba proteus induced with the calcium ionophore A23187. Prusch, R.D. Science (1980) [Pubmed]
  3. Pertussis toxin inhibition of chemotactic factor-induced calcium mobilization and function in human polymorphonuclear leukocytes. Goldman, D.W., Chang, F.H., Gifford, L.A., Goetzl, E.J., Bourne, H.R. J. Exp. Med. (1985) [Pubmed]
  4. Stimulus specificity of the generation of leukotrienes by dog mastocytoma cells. Goetzl, E.J., Phillips, M.J., Gold, W.M. J. Exp. Med. (1983) [Pubmed]
  5. Bone resorption in organ culture: inhibition by the divalent cation ionophores A23187 and X-537A. Ivey, J.L., Wright, D.R., Tashjian, A.H. J. Clin. Invest. (1976) [Pubmed]
  6. The sequential release of granule constitutents from human neutrophils. Bentwood, B.J., Henson, P.M. J. Immunol. (1980) [Pubmed]
  7. Local application of calcium-modulating agents to a crushed goldfish optic nerve modifies visual recovery. Meiri, H., Grafstein, B. Exp. Neurol. (1984) [Pubmed]
  8. Further characterization of the neurofunctional effects of the calcium ionophore A23187. Sobotka, T., Brodie, R., Quander, Y., O'Donnell, M., West, G. Drug and chemical toxicology. (1989) [Pubmed]
  9. The effects of a 5-lipoxygenase inhibitor on asthma induced by cold, dry air. Israel, E., Dermarkarian, R., Rosenberg, M., Sperling, R., Taylor, G., Rubin, P., Drazen, J.M. N. Engl. J. Med. (1990) [Pubmed]
  10. Inducible binding of a factor to the c-fos enhancer. Prywes, R., Roeder, R.G. Cell (1986) [Pubmed]
  11. Inducible secretion of large, biologically potent von Willebrand factor multimers. Sporn, L.A., Marder, V.J., Wagner, D.D. Cell (1986) [Pubmed]
  12. Isolation and characterization of a serine esterase from cytolytic T cell granules. Young, J.D., Leong, L.G., Liu, C.C., Damiano, A., Wall, D.A., Cohn, Z.A. Cell (1986) [Pubmed]
  13. Fusion of intracellular membrane pools with cell surfaces of macrophages stimulated by phorbol esters and calcium ionophores. Buys, S.S., Keogh, E.A., Kaplan, J. Cell (1984) [Pubmed]
  14. Angiotensin II-mediated hypertension in the rat increases vascular superoxide production via membrane NADH/NADPH oxidase activation. Contribution to alterations of vasomotor tone. Rajagopalan, S., Kurz, S., Münzel, T., Tarpey, M., Freeman, B.A., Griendling, K.K., Harrison, D.G. J. Clin. Invest. (1996) [Pubmed]
  15. Inhibition of Ca(2+)-dependent K+ transport and cell dehydration in sickle erythrocytes by clotrimazole and other imidazole derivatives. Brugnara, C., de Franceschi, L., Alper, S.L. J. Clin. Invest. (1993) [Pubmed]
  16. Dog mastocytoma cells secrete a 92-kD gelatinase activated extracellularly by mast cell chymase. Fang, K.C., Raymond, W.W., Lazarus, S.C., Caughey, G.H. J. Clin. Invest. (1996) [Pubmed]
  17. Radioimmunoassay of the leukotrienes of slow reacting substance of anaphylaxis. Levine, L., Morgan, R.A., Lewis, R.A., Austen, K.F., Clark, D.A., Marfat, A., Corey, E.J. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  18. Mitogens increase phosphorylation of phosphoinositides in thymocytes. Taylor, M.V., Metcalfe, J.C., Hesketh, T.R., Smith, G.A., Moore, J.P. Nature (1984) [Pubmed]
  19. Release of eosinophil chemotactic factor from human polymorphonuclear neutrophils by calcium ionophore A23187 and phagocytosis. Gzarnetzki, B.M., Konig, W., Lichtenstein, L.M. Nature (1975) [Pubmed]
  20. Metarhodopsin I/metarhodopsin II transition triggers light-induced change in calcium binding at rod disk membranes. Kaupp, U.B., Schnetkamp, P.P., Junge, W. Nature (1980) [Pubmed]
  21. Paramecium fusion rosettes: possible function as Ca2+ gates. Satir, B.H., Oberg, S.G. Science (1978) [Pubmed]
  22. Platelet coagulation factor XIa-inhibitor, a form of Alzheimer amyloid precursor protein. Smith, R.P., Higuchi, D.A., Broze, G.J. Science (1990) [Pubmed]
  23. Leukotriene B, a potent chemokinetic and aggregating substance released from polymorphonuclear leukocytes. Ford-Hutchinson, A.W., Bray, M.A., Doig, M.V., Shipley, M.E., Smith, M.J. Nature (1980) [Pubmed]
  24. Protein kinase C regulation of the receptor-coupled calcium signal in histamine-secreting rat basophilic leukaemia cells. Sagi-Eisenberg, R., Lieman, H., Pecht, I. Nature (1985) [Pubmed]
  25. Vascular endothelial cells synthesize nitric oxide from L-arginine. Palmer, R.M., Ashton, D.S., Moncada, S. Nature (1988) [Pubmed]
  26. Activated human eosinophils generate SRS-A leukotrienes following IgG-dependent stimulation. Shaw, R.J., Walsh, G.M., Cromwell, O., Moqbel, R., Spry, C.J., Kay, A.B. Nature (1985) [Pubmed]
  27. Effects of catecholamines, ATP and ionophore A23187 on potassium and calcium movements in isolated hepatocytes. Burgess, G.M., Claret, M., Jenkinson, D.H. Nature (1979) [Pubmed]
  28. Possible association of alcohol tolerance with increased synaptic Ca2+ sensitivity. Lynch, M.A., Littleton, J.M. Nature (1983) [Pubmed]
  29. Divalent cation ionophores stimulate resorption and inhibit DNA synthesis in cultured fetal rat bone. Lorenzo, J.A., Raisz, L.G. Science (1981) [Pubmed]
  30. Arachidonic acid metabolism by human monocytes. Studies with platelet-depleted cultures. Pawlowski, N.A., Kaplan, G., Hamill, A.L., Cohn, Z.A., Scott, W.A. J. Exp. Med. (1983) [Pubmed]
  31. Evidence for sequential signals in the induction of the arachidonic acid cascade in macrophages. Aderem, A.A., Scott, W.A., Cohn, Z.A. J. Exp. Med. (1986) [Pubmed]
  32. Endothelial cell "memory" of inflammatory stimulation: human venular endothelial cells store interleukin 8 in Weibel-Palade bodies. Wolff, B., Burns, A.R., Middleton, J., Rot, A. J. Exp. Med. (1998) [Pubmed]
  33. Production of tumor necrosis factor/cachectin by human T cell lines and peripheral blood T lymphocytes stimulated by phorbol myristate acetate and anti-CD3 antibody. Sung, S.S., Bjorndahl, J.M., Wang, C.Y., Kao, H.T., Fu, S.M. J. Exp. Med. (1988) [Pubmed]
  34. Production of hematopoietic colony-stimulating factors by human natural killer cells. Cuturi, M.C., Anegón, I., Sherman, F., Loudon, R., Clark, S.C., Perussia, B., Trinchieri, G. J. Exp. Med. (1989) [Pubmed]
  35. Bovine papilloma virus encoded E2 protein activates lymphokine genes through DNA elements, distinct from the consensus motif, in the long control region of its own genome. Heike, T., Miyatake, S., Yoshida, M., Arai, K., Arai, N. EMBO J. (1989) [Pubmed]
  36. Ionophore-mediated calcium entry induces mussel gill ciliary arrest. Satir, P. Science (1975) [Pubmed]
  37. Leukocyte common antigen (CD45) is required for immunoglobulin E-mediated degranulation of mast cells. Berger, S.A., Mak, T.W., Paige, C.J. J. Exp. Med. (1994) [Pubmed]
  38. Selective suppression of interleukin-12 induction after macrophage receptor ligation. Sutterwala, F.S., Noel, G.J., Clynes, R., Mosser, D.M. J. Exp. Med. (1997) [Pubmed]
  39. Relative contribution of leukotriene B4 to the neutrophil chemotactic activity produced by the resident human alveolar macrophage. Martin, T.R., Raugi, G., Merritt, T.L., Henderson, W.R. J. Clin. Invest. (1987) [Pubmed]
  40. Regulation of calreticulin gene expression by calcium. Waser, M., Mesaeli, N., Spencer, C., Michalak, M. J. Cell Biol. (1997) [Pubmed]
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