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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

AmbotzLS-1001     6-bromo-5-methylamino-2- [[(2S,3R,5R,8R,9R)...

Synonyms: CTK8D9434, AR-1H1093, AC1L3GY5, 4-Br-A23187, 4-Bra23187, ...
 
 
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High impact information on 4-Br-A23187

  • We now demonstrate that transforming growth factor type beta (TGF-beta) prevents neuronal Ca2+ overloading of rat hippocampal neurons in response to the glutamatergic agonist N-methyl-D-aspartate or the Ca2+ ionophore 4-Br-A23187 and, in addition, leads to a substantial increase in neuronal Bcl2 protein expression [1].
  • We observed that the supernatants of cultures treated with calcium and ionophore 4-Br-A23187 contained more TF activity than those of control cultures [2].
  • A23187, 4-BrA23187, and ionomycin transport several lanthanide series trivalent cations at efficiencies similar to Ca2+, when compared at cation concentrations of approximately 10(-5) M, ionophore concentrations of approximately 10(-6) M, and a pH of 7.00 [3].
  • Dibutyryl cyclic AMP (db-cAMP) (10(-3) M) was used to stimulate PKA and the calcium ionophore 4-Br-A23187 (10(-5) M) was used to stimulate calmodulin-dependent phosphorylation [4].
  • Effects of pH conditions on Ca2+ transport catalyzed by ionophores A23187, 4-BrA23187, and ionomycin suggest problems with common applications of these compounds in biological systems [5].
 

Biological context of 4-Br-A23187

  • Incubation of the cells with the calcium ionophore, 4-bromo A-23187, leads to increased amounts of intracellular calcium and reductions in ATP levels, but has no effect on oxygen consumption [6].
 

Anatomical context of 4-Br-A23187

  • These combined results show that 4-Br-A23187, with extracellular calcium, increases TF activity concomitant with dramatic changes in cell morphology and the plasma membrane [2].
  • In cells exposed to 4-Br-A23187, the presence of CaBP significantly reduced the rate of rise of [Ca(2+)](i), reduced the peak response, slowed the rate of recovery, and reduced the depolarization of mitochondria [7].
  • To examine the possible inhibitory role of Ca2+ on gap junctions, the Ca2+ ionophore 4-br-A23187 was used [8].
  • Segments of sciatic nerve, with their epineuria punctured, were incubated with or without 4-Br-A23187 [9].
 

Associations of 4-Br-A23187 with other chemical compounds

  • To investigate the activity of PDGF-beta receptors in HPMC, the authors examined intracellular calcium (Ca2+(i)) mobilization in HPMC in response to PDGF-BB (100 ng/ml), histamine (1.0 mmol/L), and 4-brA23187 (1.0 micromol/L) using the calcium indicator, fura-2 [10].
 

Analytical, diagnostic and therapeutic context of 4-Br-A23187

  • Reversing the sequence of perfusions, cells pre-incubated with db-cAMP showed no further rise in response to stimulation with 4-Br-A23187 [4].

References

  1. Regulation of neuronal Bcl2 protein expression and calcium homeostasis by transforming growth factor type beta confers wide-ranging protection on rat hippocampal neurons. Prehn, J.H., Bindokas, V.P., Marcuccilli, C.J., Krajewski, S., Reed, J.C., Miller, R.J. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  2. Fibroblast tissue factor: calcium and ionophore induce shape changes, release of membrane vesicles, and redistribution of tissue factor antigen in addition to increased procoagulant activity. Carson, S.D., Perry, G.A., Pirruccello, S.J. Blood (1994) [Pubmed]
  3. Mechanism and specificity of lanthanide series cation transport by ionophores A23187, 4-BrA23187, and ionomycin. Wang, E., Taylor, R.W., Pfeiffer, D.R. Biophys. J. (1998) [Pubmed]
  4. Asymmetric interactions between phosphorylation pathways regulating ciliary beat frequency in human nasal respiratory epithelium in vitro. Smith, R.P., Shellard, R., Dhillon, D.P., Winter, J., Mehta, A. J. Physiol. (Lond.) (1996) [Pubmed]
  5. Effects of pH conditions on Ca2+ transport catalyzed by ionophores A23187, 4-BrA23187, and ionomycin suggest problems with common applications of these compounds in biological systems. Erdahl, W.L., Chapman, C.J., Taylor, R.W., Pfeiffer, D.R. Biophys. J. (1995) [Pubmed]
  6. Alterations in alveolar type II cell metabolism induced by tetrandrine and other alkaloids. Miles, P.R., Bowman, L., Ma, J.K., Ma, J.Y. Toxicol. Appl. Pharmacol. (1993) [Pubmed]
  7. Calcium buffering and protection from excitotoxic cell death by exogenous calbindin-D28k in HEK 293 cells. Rintoul, G.L., Raymond, L.A., Baimbridge, K.G. Cell Calcium (2001) [Pubmed]
  8. Lindane inhibition of gap junctional communication in myometrial myocytes is partially dependent on phosphoinositide-generated second messengers. Criswell, K.A., Loch-Caruso, R., Stuenkel, E.L. Toxicol. Appl. Pharmacol. (1995) [Pubmed]
  9. Prostacyclin release in experimental diabetes: effects of evening primrose oil. Stevens, E.J., Carrington, A.L., Tomlinson, D.R. Prostaglandins Leukot. Essent. Fatty Acids (1993) [Pubmed]
  10. Platelet derived growth factor-BB induced calcium transients in cultured human peritoneal mesothelial cells. Bird, S.D., Hasan, Q., Davis, P.F., Walker, R.J. ASAIO journal (American Society for Artificial Internal Organs : 1992) (1998) [Pubmed]
 
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