U 73122 (CAS 112648-68-7): R&D Systems
Catalog Number: 1268
Chemical Name: 1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione
Biological Activity

Phospholipase C inhibitor. Inhibits agonist-induced platelet aggregation with IC50 values of 1-5 μM. Potently inhibits human polymorphonuclear neutrophil adhesion on biological surfaces (IC50 < 50 nM) and exhibits antinociceptive activity in vivo. Also activates TRPM4 and inhibits TRPM3 channels.

Negative Control also available.
Technical Data
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of Pharmacia
Other Product-Specific Information:
Background References
  1. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils.
    Bleasdale et al.
    J.Pharmacol.Exp.Ther., 1990;255:756
  2. U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions.
    Smith et al.
    J.Pharmacol.Exp.Ther., 1996;278:320
  3. Phospholipase Cβ3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain.
    Shi et al.
    Proc.Natl.Acad.Sci.U.S.A., 2008;105:20004
  4. Direct modulation of TRPM4 and TRPM3 channels by the phospholipase C inhibitor U73122.
    Leitner et al.
    Br.J.Pharmacol., 2016;173:2555
Citations:

The citations listed below are publications that use Tocris products. Selected citations for U 73122 include:

50 Citations: Showing 1 - 10
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  1. The novel cannabinoid receptor GPR55 mediates anxiolytic-like effects in the medial orbital cortex of mice with acute stress.
    Authors: Shi?
    Mol Brain 2017;10(1):38
  2. The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
    Authors: Olianas Et al.
    European Journal of Pharmacology 2016;794:135
  3. Detachment of surface membrane invagination systems by cationic amphiphilic drugs.
    Authors: Osman Et al.
    ASN Neuro 2016;6:18536
  4. The prostaglandin E2-EP3 receptor axis regulates Anaplasma phagocytophilum-mediated NLRC4 inflammasome activation.
    Authors: Wang Et al.
    PLoS Pathog. 2016;12:e1005803
  5. Divergence in endothelin-1- and bradykinin-activated store-operated calcium entry in afferent sensory neurons.
    Authors: Szteyn Et al.
    PLoS One 2015;7
  6. Intercellular Odontoblast Communication via ATP Mediated by Pannexin-1 Channel and Phospholipase C-coupled Receptor Activation.
    Authors: Sato Et al.
    PLoS One 2015;6:326
  7. Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane.
    Authors: Azab Et al.
    Sci Rep 2015;6
  8. The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes.
    Authors: Ang Et al.
    MBio 2015;5:8134
  9. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Mediators Inflamm 2015;5:10468
  10. Allantoin ameliorates chemically-induced pancreatic β-cell damage through activation of the imidazoline I3 receptors.
    Authors: Amitani Et al.
    PeerJ 2015;3:e1105
  11. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci 2015;35:11252
  12. The Effect of Therapeutic Blockades of Dust Particles-Induced Ca2+ Signaling and Proinflammatory Cytokine IL-8 in Human Bronchial Epithelial Cells.
    Authors: Yoon Et al.
    Blood 2015;2015:843024
  13. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci 2015;18:545
  14. Oxidized LDL activates blood platelets through CD36/NOX2-mediated inhibition of the cGMP/protein kinase G signaling cascade.
    Authors: Magwenzi Et al.
    PLoS One 2015;125:2693
  15. A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype-3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells.
    Authors: Liu Et al.
    Sci Rep 2015;11:4121
  16. Activation of Phosphatidylinositol-Linked Dopamine Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex.
    Authors: Glovaci and Chapman
    PLoS One 2015;10:e0131948
  17. Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
    Authors: Rioult-Pedotti Et al.
    PLoS One 2015;10:e0124986
  18. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils.
    Authors: Manosalva Et al.
    Sci Rep 2015;10:e0119715
  19. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One 2014;9:e106316
  20. Lactate-mediated glia-neuronal signalling in the mammalian brain.
    Authors: Tang Et al.
    Nat Commun 2014;5:3284
  21. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    Oncotarget 2014;5:3145
  22. Chemotherapeutic drugs induce ATP release via caspase-gated pannexin-1 channels and a caspase/pannexin-1-independent mechanism.
    Authors: Boyd-Tressler Et al.
    J Biol Chem 2014;289:27246
  23. A polarized Ca2+, diacylglycerol and STIM1 signalling system regulates directed cell migration.
    Authors: Tsai Et al.
    Nat Cell Biol 2014;16:133
  24. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Authors: Morelli Et al.
    BMC Cancer 2014;14:921
  25. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    J Neurophysiol 2014;12:47
  26. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood 2014;123:249
  27. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons.
    Authors: Mariqueo Et al.
    Mol Med Rep 2014;111:1940
  28. Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition.
    Authors: Chang Et al.
    Psychopharmacology (Berl) 2013;34:1096
  29. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Authors: Aihara Et al.
    Proc Natl Acad Sci U S A 2013;288:33585
  30. Divergent β-arrestin-dependent signaling events are dependent upon sequences within G-protein-coupled receptor C termini.
    Authors: Pal Et al.
    J Biol Chem 2013;288:3265
  31. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci 2013;16:874
  32. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res 2013;14:134
  33. SKF83959, an agonist of phosphatidylinositol-linked D(1)-like receptors, promotes ERK1/2 activation and cell migration in cultured rat astrocytes.
    Authors: Huang Et al.
    Oncotarget 2012;7:e49954
  34. Reproducible and sustained regulation of Gαs signalling using a metazoan opsin as an optogenetic tool.
    Authors: Bailes Et al.
    Neuron 2012;7:e30774
  35. γ-protocadherins control cortical dendrite arborization by regulating the activity of a FAK/PKC/MARCKS signaling pathway.
    Authors: Garrett Et al.
    Proc Natl Acad Sci U S A 2012;74:269
  36. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
    Nature 2012;492:123
  37. Gαq/11-mediated intracellular calcium responses to retrograde flow in endothelial cells.
    Authors: Melchior and Frangos
    J Pharmacol Exp Ther 2012;303:C467
  38. Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium.
    Authors: Lau Et al.
    Carcinogenesis 2011;300:C113
  39. Phospholipase C, Ca2+, and calmodulin signaling are required for 5-HT2A receptor-mediated transamidation of Rac1 by transglutaminase.
    Authors: Dai Et al.
    J Biol Chem 2011;213:403
  40. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
    Neuron 2010;66:248
  41. Rat hypocretin/orexin neurons are maintained in a depolarized state by TRPC channels.
    Authors: Cvetkovic-Lopes Et al.
    PLoS One 2010;5:e15673
  42. Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate.
    Authors: Sowa Et al.
    J Neurosci 2010;30:10282
  43. Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.
    Authors: Moore Et al.
    Neuron 2009;61:287
  44. Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling.
    Authors: Yin Et al.
    Neuropharmacology 2008;54:79
  45. Phospholipase C{β}3 in mouse and human dorsal root ganglia and spinal cord is a possible target for treatment of neuropathic pain.
    Authors: Shi Et al.
    Front Physiol 2008;105:20004
  46. Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction.
    Authors: Newman Et al.
    Eur J Neurosci 2007;25:1619
  47. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol 2005;314:1109
  48. PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate.
    Authors: Pierre Et al.
    EMBO J 2004;23:3031
  49. Phospholipase C activator m-3M3FBS affects Ca2+ homeostasis independently of phospholipase C activation.
    Authors: Krjukova Et al.
    Br J Pharmacol 2004;143:3
  50. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Am J Physiol Cell Physiol 2003;100:1322
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U 73343

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