The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

SureCN676619     1-[6-[[(8S,9S,13S,14S,17S)-3- methoxy-13...

Synonyms: CHEMBL1256678, BSPBio_001222, MolMap_000051, U6756_SIGMA, AC1L2XIB, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of U 73122


Psychiatry related information on U 73122

  • Furthermore, administration of the phospholipase C (PLC) inhibitor U-73122, as well as the injection of an aODN complementary to the sequence of PLCbeta(1), antagonized the increase of the pain threshold induced by both cholinomimetic drugs [6].

High impact information on U 73122

  • Recombinant Nt PLC3 displayed Ca(2+)-dependent PI 4,5-P(2)-hydrolyzing activity sensitive to U-73122 and to mutations in the active site [7].
  • U-73122 at low micromolar concentrations inhibited and partially depolarized pollen tube growth, caused PI 4,5-P(2) spreading at the apex, and abolished DAG membrane accumulation [7].
  • Furthermore, PACAP promitogenic effects required PLC pathway function indicated by antagonist U-73122 studies in hop-transfected cortical cells and native sympathetic neuroblasts [8].
  • Superfusing cells with U-73122, an inhibitor of phospholipase C, ablated the NSP4 response [9].
  • However, ET-1-induced 6-keto-PGF1 alpha production was not altered by U-73122 [10].

Chemical compound and disease context of U 73122

  • It is not affected by the AR blockers cyproterone and flutamide, whereas it is completely inhibited by the phospholipase C inhibitor U-73122 and pertussis toxin [11].
  • The effect of PACAP38 on inositol phosphate formation was significantly reduced by U-73122 and by pertussis toxin, indicating that activation of PACAP receptors causes stimulation of a phospholipase C through a pertussis toxin-sensitive G protein [12].
  • 6. ATP- and UTP-induced [Ca2+]i rises were insensitive to pertussis toxin, caffeine (5 mM) and ryanodine (10 microM) but were significantly reduced by U-73122, a phospholipase C (PLC) inhibitor [13].
  • I.c.v. administration of the phospholipase C (PLC) inhibitors U-73122 and neomycin antagonized the hyperalgesia induced by the selective H(1) agonist FMPH [14].
  • The response is partially pertussis toxin (PTX) insensitive, abolished by the phospholipase C inhibitor U-73122, and diminished by the inositol 1,4,5-trisphosphate receptor antagonist 2-aminoethoxydiphenyl borate [15].

Biological context of U 73122

  • Pretreatment of T leukemic Molt-4 cells with PLC inhibitors such as U-73122 or ET-18-OCH(3) potentiated etoposide-induced apoptosis in these cells [16].
  • Addition of U-73122 to intact cells also inhibited the agonist-induced sequestration of cell surface muscarinic receptors and their subsequent down-regulation with an IC50 value (4.1 microM) similar to that observed for inhibition of inositol phosphate release (3.7 microM) [3].
  • Consistent with the signaling model for PDGF-mediated chemotaxis, activation of phospholipase C played a critical role in [Ca2+]o-initiated chemotaxis: U-73122, an inhibitor of the activation of phospholipase C, blocked approximately 50% of PDGF-stimulated chemotaxis but blocked nearly all of the [Ca2+]o-stimulated chemotaxis [17].
  • The effects of ATP, U-73122, apyrase, and saline shear stress on [Ca2+]i homeostasis were studied in fura-2 loaded, mouse fibroblast cells (L929), both in suspension and plated on glass [18].
  • Pretreatment of cells with BAPTA-AM, thapsigargin +NiCl(2), or U-73122 (a phospholipase C inhibitor) inhibited cell adhesion induced by vortex-mediated mechanical stress [19].

Anatomical context of U 73122


Associations of U 73122 with other chemical compounds


Gene context of U 73122

  • Furthermore, U-73122, a phospholipase C-betas (PLC) inhibitor or xestospongin C, an inositol triphosphate receptor (InsP3-R) blocker, have partially prevented the effect of NPY on CRF synthesis and secretion [28].
  • U-73122 also inhibited PMN adherence to and transmigration through TNF-alpha-activated endothelium (IC50 < 50 nM) [29].
  • U-73122, a phospholipase C (PLC) inhibitor, suppressed BK-induced IL-6 and PGE(2) synthesis in SaM-1 cells [30].
  • Addition of the mitogen-activated protein kinase (MAPK)-inhibitor PD 98059 (50 microM), phospholipase C-inhibitor U-73122 (10 microM), p21(ras)-inhibitor lovastatine (250 microM), and the src-like kinase inhibitor PP2 (20 microg/ml) inhibited FF-MAS-induced GVBD, but not spontaneous GVBD [31].
  • In addition, we show that NaCl increases diacylglycerol (DAG) levels and that a phospholipase C (PLC) inhibitor, U-73122, inhibits NaCl-induced ERK1/2 phosphorylation [32].

Analytical, diagnostic and therapeutic context of U 73122

  • In calcium-free perfusion medium a substantial calcium signal remained which disappeared after loading of cortical neurons with 5 microM U-73122 [33].
  • Flow cytometry assays demonstrated that MCH induces a slow and long-lasting rise in intracellular calcium, which can be blocked by U-73122 [34].


  1. Arrhythmogenic action of thrombin during myocardial reperfusion via release of inositol 1,4,5-triphosphate. Jacobsen, A.N., Du, X.J., Lambert, K.A., Dart, A.M., Woodcock, E.A. Circulation (1996) [Pubmed]
  2. Activation of p38 mitogen-activated protein kinase by oxidized LDL in vascular smooth muscle cells: mediation via pertussis toxin-sensitive G proteins and association with oxidized LDL-induced cytotoxicity. Jing, Q., Xin, S.M., Cheng, Z.J., Zhang, W.B., Zhang, R., Qin, Y.W., Pei, G. Circ. Res. (1999) [Pubmed]
  3. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. Thompson, A.K., Mostafapour, S.P., Denlinger, L.C., Bleasdale, J.E., Fisher, S.K. J. Biol. Chem. (1991) [Pubmed]
  4. Pharmacological analysis of nod factor-induced calcium spiking in Medicago truncatula. Evidence for the requirement of type IIA calcium pumps and phosphoinositide signaling. Engstrom, E.M., Ehrhardt, D.W., Mitra, R.M., Long, S.R. Plant Physiol. (2002) [Pubmed]
  5. Angiotensin II provokes cesium-induced ventricular tachyarrhythmias. Gondo, N., Kumagai, K., Nakashima, H., Saku, K. Cardiovasc. Res. (2001) [Pubmed]
  6. The phospholipase C-IP3 pathway is involved in muscarinic antinociception. Galeotti, N., Bartolini, A., Ghelardini, C. Neuropsychopharmacology (2003) [Pubmed]
  7. Pollen Tube Tip Growth Depends on Plasma Membrane Polarization Mediated by Tobacco PLC3 Activity and Endocytic Membrane Recycling. Helling, D., Possart, A., Cottier, S., Klahre, U., Kost, B. Plant Cell (2006) [Pubmed]
  8. Regulation of neuroblast mitosis is determined by PACAP receptor isoform expression. Nicot, A., DiCicco-Bloom, E. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  9. The rotavirus enterotoxin NSP4 mobilizes intracellular calcium in human intestinal cells by stimulating phospholipase C-mediated inositol 1,4,5-trisphosphate production. Dong, Y., Zeng, C.Q., Ball, J.M., Estes, M.K., Morris, A.P. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  10. Prostacyclin formation elicited by endothelin-1 in rat aorta is mediated via phospholipase D activation and not phospholipase C or A2. Wright, H.M., Malik, K.U. Circ. Res. (1996) [Pubmed]
  11. Testosterone signaling through internalizable surface receptors in androgen receptor-free macrophages. Benten, W.P., Lieberherr, M., Stamm, O., Wrehlke, C., Guo, Z., Wunderlich, F. Mol. Biol. Cell (1999) [Pubmed]
  12. Pituitary adenylate cyclase-activating polypeptide (PACAP) stimulates adenylyl cyclase and phospholipase C activity in rat cerebellar neuroblasts. Basille, M., Gonzalez, B.J., Desrues, L., Demas, M., Fournier, A., Vaudry, H. J. Neurochem. (1995) [Pubmed]
  13. P2Y purinoceptor activation mobilizes intracellular Ca2+ and induces a membrane current in rat intracardiac neurones. Liu, D.M., Katnik, C., Stafford, M., Adams, D.J. J. Physiol. (Lond.) (2000) [Pubmed]
  14. H1-receptor stimulation induces hyperalgesia through activation of the phospholipase C-PKC pathway. Galeotti, N., Malmberg-Aiello, P., Bartolini, A., Schunack, W., Ghelardini, C. Neuropharmacology (2004) [Pubmed]
  15. Human bronchial epithelial cells express PAR-2 with different sensitivity to thermolysin. Ubl, J.J., Grishina, Z.V., Sukhomlin, T.K., Welte, T., Sedehizade, F., Reiser, G. Am. J. Physiol. Lung Cell Mol. Physiol. (2002) [Pubmed]
  16. Proteolytic cleavage of phospholipase C-gamma1 during apoptosis in Molt-4 cells. Bae, S.S., Perry, D.K., Oh, Y.S., Choi, J.H., Galadari, S.H., Ghayur, T., Ryu, S.H., Hannun, Y.A., Suh, P.G. FASEB J. (2000) [Pubmed]
  17. Extracellular calcium and platelet-derived growth factor promote receptor-mediated chemotaxis in osteoblasts through different signaling pathways. Godwin, S.L., Soltoff, S.P. J. Biol. Chem. (1997) [Pubmed]
  18. Shear stress-induced [Ca2+]i transients and oscillations in mouse fibroblasts are mediated by endogenously released ATP. Grierson, J.P., Meldolesi, J. J. Biol. Chem. (1995) [Pubmed]
  19. Vortex-mediated mechanical stress induces integrin-dependent cell adhesion mediated by inositol 1,4,5-trisphosphate-sensitive Ca2+ release in THP-1 cells. Ashida, N., Takechi, H., Kita, T., Arai, H. J. Biol. Chem. (2003) [Pubmed]
  20. The aminosteroid phospholipase C antagonist U-73122 (1-[6-[[17-beta-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro. Feisst, C., Albert, D., Steinhilber, D., Werz, O. Mol. Pharmacol. (2005) [Pubmed]
  21. Effect of phospholipase C inhibitor U-73122 on antigen-induced airway smooth muscle contraction in guinea pigs. Salari, H., Bramley, A., Langlands, J., Howard, S., Chan-Yeung, M., Chan, H., Schellenberg, R. Am. J. Respir. Cell Mol. Biol. (1993) [Pubmed]
  22. Dynamic Ca2+ signalling in rat arterial smooth muscle cells under the control of local renin-angiotensin system. Asada, Y., Yamazawa, T., Hirose, K., Takasaka, T., Iino, M. J. Physiol. (Lond.) (1999) [Pubmed]
  23. Inhibition of phospholipase C attenuates liver mitochondrial calcium overload following cold ischemia. Knox, C.D., Pierce, J.M., Nicoud, I.B., Belous, A.E., Jones, C.M., Anderson, C.D., Chari, R.S. Transplantation (2006) [Pubmed]
  24. Stimulation of the intracellular killing of Staphylococcus aureus by human monocytes mediated by Fc gamma receptors I and II. Zheng, L., Nibbering, P.H., van Furth, R. Eur. J. Immunol. (1993) [Pubmed]
  25. PAC1 receptor activation by PACAP-38 mediates Ca2+ release from a cAMP-dependent pool in human fetal adrenal gland chromaffin cells. Payet, M.D., Bilodeau, L., Breault, L., Fournier, A., Yon, L., Vaudry, H., Gallo-Payet, N. J. Biol. Chem. (2003) [Pubmed]
  26. EP1- and EP3-receptors mediate prostaglandin E2-induced constriction of porcine large cerebral arteries. Jadhav, V., Jabre, A., Lin, S.Z., Lee, T.J. J. Cereb. Blood Flow Metab. (2004) [Pubmed]
  27. Calcineurin phosphatase activity: activation by glucocorticoids and role of intracellular calcium. Tong, D.C., Buck, S.M., Roberts, B.R., Klein, J.D., Tumlin, J.A. Transplantation (2004) [Pubmed]
  28. Characterization of neuropeptide Y-mediated corticotropin-releasing factor synthesis and release from human placental trophoblasts. Robidoux, J., Simoneau, L., St-Pierre, S., Masse, A., Lafond, J. Endocrinology (2000) [Pubmed]
  29. U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions. Smith, R.J., Justen, J.M., McNab, A.R., Rosenbloom, C.L., Steele, A.N., Detmers, P.A., Anderson, D.C., Manning, A.M. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  30. Activation of osteoblastic functions by a mediator of pain, bradykinin. Kondo, A., Togari, A. Biochem. Pharmacol. (2004) [Pubmed]
  31. Resumption of meiosis induced by meiosis-activating sterol has a different signal transduction pathway than spontaneous resumption of meiosis in denuded mouse oocytes cultured in vitro. Faerge, I., Terry, B., Kalous, J., Wahl, P., Lessl, M., Ottesen, J.L., Hyttel, P., Grøndahl, C. Biol. Reprod. (2001) [Pubmed]
  32. Hyperosmolality induces activation of cPKC and nPKC, a requirement for ERK1/2 activation in NIH/3T3 cells. Zhuang, S., Hirai, S.I., Ohno, S. Am. J. Physiol., Cell Physiol. (2000) [Pubmed]
  33. BDNF acutely modulates synaptic transmission and calcium signalling in developing cortical neurons. He, J., Gong, H., Luo, Q. Cell. Physiol. Biochem. (2005) [Pubmed]
  34. Mechanisms of action of melanin-concentrating hormone in the teleost fish erythrophoroma cell line (GEM-81). Isoldi, M.C., de Pina Benabou, M.H., Schumacher, R.I., Góis, C.C., Scarparo, A.C., Rebouças, N.A., Visconti, M.A. Gen. Comp. Endocrinol. (2004) [Pubmed]
WikiGenes - Universities