J. Biochem, 1997, Vol. 122, No. 3 498-505
© 1997 Japanese Biochemical Society
research-article |
2APB, 2-Aminoethoxydiphenyl Borate, a Membrane-Penetrable Modulator of Ins(1,4,5)P3-Induced Ca2+ Release
,
*Minase Research Institute, Ono Pharmaceutical Company Mishima, Osaka 618
Department of Biomedical Science, Graduate School of Veterinary Medicine, Hokkaido University Sapporo 060
Department of Molecular Neurobiology, Institute of Medical Science, Tokyo University Shiroganedai, Minato-ku, Tokyo 108
Molecular Neurobiology Laboratory, Tsukuba Life Science Center, Institute of Physical and Chemical Research (RIKEN) 3-1-1 Koyadai, Tsukuba, Ibaraki 305
1To whom correspondence should be addressed. Tel: + 81-75-961-1151, Fax: +81-962-9314
The effects of a novel membrane-penetrable modulator, 2APB (2-aminoethoxy diphenyl borate), on Ins(1,4,5)P3-induced Ca2+ release were examined. 2APB inhibited Ins(1,4,5)-P3-induced Ca2+ release from rat cerebellar microsomal preparations without affecting [3H]Ins(1,4,5)P3 binding to its receptor. The IC50 value (concentration producing 50% inhibition) of 2APB for inhibition of Ins(1,4,5)P3 (100 nM) induced Ca2+ release was 42 µM. Further increase in the concentration of 2APB (more than 90 µM) caused a gradual release of Ca2+ from cerebellar microsomal preparations. Addition of 2APB to the extracellular environment inhibited the cytosolic Ca2+ ([Ca2+]c) rise in intact cells such as human platelets and neutrophils stimulated by thromboxane-mimetic STA2, or thrombin, and leukotriene B4 (LTB4) or formyl-methionine-leucine-phenylalanine (FMLP), respectively. 2APB inhibited the contraction of thoracic aorta isolated from rabbits induced by angioten-sin II (AII), STA2, and norepinephrine in a non-competitive manner, but showed no effect on the contraction of potassium-depolarized muscle. 2APB had no effect on the Ca2+ release from the ryanodine-sensitive Ca2+ store prepared from rat leg skeletal muscle and heart. Although the specificity of 2APB with respect to the intracellular signaling system was not fully established, 2APB is the first candidate for a membrane-penetrable modulator of Ins(1,4,5)P3 receptor, and it should be a useful tool to investigate the physiological role of the Ins(1,4,5)P3 receptor in various cells.
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M.-K. Chung, A. D. Guler, and M. J. Caterina Biphasic Currents Evoked by Chemical or Thermal Activation of the Heat-gated Ion Channel, TRPV3 J. Biol. Chem., April 22, 2005; 280(16): 15928 - 15941. [Abstract] [Full Text] [PDF]
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P. K. Aley, K. E. Porter, J. P. Boyle, P. J. Kemp, and C. Peers Hypoxic Modulation of Ca2+ Signaling in Human Venous Endothelial Cells: MULTIPLE ROLES FOR REACTIVE OXYGEN SPECIES J. Biol. Chem., April 8, 2005; 280(14): 13349 - 13354. [Abstract] [Full Text] [PDF]
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C. Hisatsune, K. Nakamura, Y. Kuroda, T. Nakamura, and K. Mikoshiba Amplification of Ca2+ Signaling by Diacylglycerol-mediated Inositol 1,4,5-Trisphosphate Production J. Biol. Chem., March 25, 2005; 280(12): 11723 - 11730. [Abstract] [Full Text] [PDF]
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T.-S. Tang, E. Slow, V. Lupu, I. G. Stavrovskaya, M. Sugimori, R. Llinas, B. S. Kristal, M. R. Hayden, and I. Bezprozvanny Disturbed Ca2+ signaling and apoptosis of medium spiny neurons in Huntington's disease PNAS, February 15, 2005; 102(7): 2602 - 2607. [Abstract] [Full Text] [PDF]
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 H.-N. Liu, S. Ohya, S. Furuzono, J. Wang, Y. Imaizumi, and S. Nakayama Co-contribution of IP3R and Ca{superscript 2}+ Influx Pathways to Pacemaker Ca{superscript 2}+ Activity in Stomach ICC J Biol Rhythms, February 1, 2005; 20(1): 15 - 26. [Abstract] [PDF]
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G. St. J Bird and J. W Putney Jr Capacitative calcium entry supports calcium oscillations in human embryonic kidney cells J. Physiol., February 1, 2005; 562(3): 697 - 706. [Abstract] [Full Text] [PDF]
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S. Bollimuntha, B. B. Singh, S. Shavali, S. K. Sharma, and M. Ebadi TRPC1-mediated Inhibition of 1-Methyl-4-phenylpyridinium Ion Neurotoxicity in Human SH-SY5Y Neuroblastoma Cells J. Biol. Chem., January 21, 2005; 280(3): 2132 - 2140. [Abstract] [Full Text] [PDF]
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S. N. Saleh and I. A. Greenwood Activation of chloride currents in murine portal vein smooth muscle cells by membrane depolarization involves intracellular calcium release Am J Physiol Cell Physiol, January 1, 2005; 288(1): C122 - C131. [Abstract] [Full Text] [PDF]
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N. Gamper, V. Reznikov, Y. Yamada, J. Yang, and M. S. Shapiro Phosphotidylinositol 4,5-Bisphosphate Signals Underlie Receptor-Specific Gq/11-Mediated Modulation of N-Type Ca2+ Channels J. Neurosci., December 1, 2004; 24(48): 10980 - 10992. [Abstract] [Full Text] [PDF]
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O. Basset, F.-X. Boittin, O. M. Dorchies, J.-Y. Chatton, C. van Breemen, and U. T. Ruegg Involvement of Inositol 1,4,5-Trisphosphate in Nicotinic Calcium Responses in Dystrophic Myotubes Assessed by Near-plasma Membrane Calcium Measurement J. Biol. Chem., November 5, 2004; 279(45): 47092 - 47100. [Abstract] [Full Text] [PDF]
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O. Dyachok and E. Gylfe Ca2+-induced Ca2+ Release via Inositol 1,4,5-trisphosphate Receptors Is Amplified by Protein Kinase A and Triggers Exocytosis in Pancreatic {beta}-Cells J. Biol. Chem., October 29, 2004; 279(44): 45455 - 45461. [Abstract] [Full Text] [PDF]
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V. K. Unni, S. S. Zakharenko, L. Zablow, A. J. DeCostanzo, and S. A. Siegelbaum Calcium Release from Presynaptic Ryanodine-Sensitive Stores Is Required for Long-Term Depression at Hippocampal CA3-CA3 Pyramidal Neuron Synapses J. Neurosci., October 27, 2004; 24(43): 9612 - 9622. [Abstract] [Full Text] [PDF]
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W. Guo, F. Wei, S. Zou, M. T. Robbins, S. Sugiyo, T. Ikeda, J.-C. Tu, P. F. Worley, R. Dubner, and K. Ren Group I Metabotropic Glutamate Receptor NMDA Receptor Coupling and Signaling Cascade Mediate Spinal Dorsal Horn NMDA Receptor 2B Tyrosine Phosphorylation Associated with Inflammatory Hyperalgesia J. Neurosci., October 13, 2004; 24(41): 9161 - 9173. [Abstract] [Full Text] [PDF]
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K. D. Garcia, T. Shah, and J. Garcia Immunolocalization of type 2 inositol 1,4,5-trisphosphate receptors in cardiac myocytes from newborn mice Am J Physiol Cell Physiol, October 1, 2004; 287(4): C1048 - C1057. [Abstract] [Full Text] [PDF]
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W. I. DeHaven and J. Cuevas VPAC Receptor Modulation of Neuroexcitability in Intracardiac Neurons: DEPENDENCE ON INTRACELLULAR CALCIUM MOBILIZATION AND SYNERGISTIC ENHANCEMENT BY PAC1 RECEPTOR ACTIVATION J. Biol. Chem., September 24, 2004; 279(39): 40609 - 40621. [Abstract] [Full Text] [PDF]
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S. I. Zakharov, T. Smani, Y. Dobrydneva, F. Monje, C. Fichandler, P. F. Blackmore, and V. M. Bolotina Diethylstilbestrol Is a Potent Inhibitor of Store-Operated Channels and Capacitative Ca2+ Influx Mol. Pharmacol., September 1, 2004; 66(3): 702 - 707. [Abstract] [Full Text] [PDF]
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 S. K. Fellner and L. A. Parker Endothelin B receptor Ca2+ signaling in shark vascular smooth muscle: participation of inositol trisphosphate and ryanodine receptors J. Exp. Biol., September 1, 2004; 207(19): 3411 - 3417. [Abstract] [Full Text] [PDF]
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C. D. Knox, A. E. Belous, J. M. Pierce, A. Wakata, I. B. Nicoud, C. D. Anderson, C. W. Pinson, and R. S. Chari Novel role of phospholipase C-{delta}1: regulation of liver mitochondrial Ca2+ uptake Am J Physiol Gastrointest Liver Physiol, September 1, 2004; 287(3): G533 - G540. [Abstract] [Full Text] [PDF]
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C. L. Kerr, W. F. Hanna, J. H. Shaper, and W. W. Wright Lewis X-Containing Glycans are Specific and Potent Competitive Inhibitors of the Binding of ZP3 to Complementary Sites on Capacitated, Acrosome-Intact Mouse Sperm Biol Reprod, September 1, 2004; 71(3): 770 - 777. [Abstract] [Full Text] [PDF]
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H.-Z. Hu, Q. Gu, C. Wang, C. K. Colton, J. Tang, M. Kinoshita-Kawada, L.-Y. Lee, J. D. Wood, and M. X. Zhu 2-Aminoethoxydiphenyl Borate Is a Common Activator of TRPV1, TRPV2, and TRPV3 J. Biol. Chem., August 20, 2004; 279(34): 35741 - 35748. [Abstract] [Full Text] [PDF]
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M. C. Beauvois, A. Arredouani, J.-C. Jonas, J.-F. Rolland, F. Schuit, J.-C. Henquin, and P. Gilon Atypical Ca2+-induced Ca2+ release from a sarco-endoplasmic reticulum Ca2+-ATPase 3-dependent Ca2+ pool in mouse pancreatic {beta}-cells J. Physiol., August 15, 2004; 559(1): 141 - 156. [Abstract] [Full Text] [PDF]
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C. Lamont and W. G. Wier Different roles of ryanodine receptors and inositol (1,4,5)-trisphosphate receptors in adrenergically stimulated contractions of small arteries Am J Physiol Heart Circ Physiol, August 1, 2004; 287(2): H617 - H625. [Abstract] [Full Text] [PDF]
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M.-K. Chung, H. Lee, A. Mizuno, M. Suzuki, and M. J. Caterina 2-Aminoethoxydiphenyl Borate Activates and Sensitizes the Heat-Gated Ion Channel TRPV3 J. Neurosci., June 2, 2004; 24(22): 5177 - 5182. [Abstract] [Full Text] [PDF]
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M. Aoyama, A. Yamada, J. Wang, S. Ohya, S. Furuzono, T. Goto, S. Hotta, Y. Ito, T. Matsubara, K. Shimokata, et al. Requirement of ryanodine receptors for pacemaker Ca2+ activity in ICC and HEK293 cells J. Cell Sci., June 1, 2004; 117(13): 2813 - 2825. [Abstract] [Full Text] [PDF]
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S. Morales, P. J. Camello, S. Alcon, G. M. Salido, G. Mawe, and M. J. Pozo Coactivation of capacitative calcium entry and L-type calcium channels in guinea pig gallbladder Am J Physiol Gastrointest Liver Physiol, June 1, 2004; 286(6): G1090 - G1100. [Abstract] [Full Text] [PDF]
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J. H. Nam, J.-E. Woo, D.-Y. Uhm, and S. J. Kim Membrane-delimited Regulation of Novel Background K+ Channels by MgATP in Murine Immature B Cells J. Biol. Chem., May 14, 2004; 279(20): 20643 - 20654. [Abstract] [Full Text] [PDF]
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