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 U 73343 (Cat. No. 4133) 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

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

Showing Results 1 - 10 of 47

  1. Detachment of surface membrane invagination systems by cationic amphiphilic drugs.
    Authors: Osman Et al.
    ASN Neuro
  2. Divergence in endothelin-1- and bradykinin-activated store-operated calcium entry in afferent sensory neurons.
    Authors: Szteyn Et al.
    PLoS One
  3. Intercellular Odontoblast Communication via ATP Mediated by Pannexin-1 Channel and Phospholipase C-coupled Receptor Activation.
    Authors: Sato Et al.
    PLoS One
  4. 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
  5. The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes.
    Authors: Ang Et al.
  6. GABAB receptor upregulates fragile X mental retardation protein expression in neurons.
    Authors: Zhang Et al.
    Mediators Inflamm
  7. Allantoin ameliorates chemically-induced pancreatic β-cell damage through activation of the imidazoline I3 receptors.
    Authors: Amitani Et al.
  8. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci
  9. 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.
  10. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci
  11. Oxidized LDL activates blood platelets through CD36/NOX2-mediated inhibition of the cGMP/protein kinase G signaling cascade.
    Authors: Magwenzi Et al.
    PLoS One
  12. 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
  13. 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
  14. Dopamine Promotes Motor Cortex Plasticity and Motor Skill Learning via PLC Activation.
    Authors: Rioult-Pedotti Et al.
    PLoS One
  15. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils.
    Authors: Manosalva Et al.
    Sci Rep
  16. 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
  17. Lactate-mediated glia-neuronal signalling in the mammalian brain.
    Authors: Tang Et al.
    Nat Commun
  18. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
  19. 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
  20. A polarized Ca2+, diacylglycerol and STIM1 signalling system regulates directed cell migration.
    Authors: Tsai Et al.
    Nat Cell Biol
  21. Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
    Authors: Morelli Et al.
    BMC Cancer
  22. TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis.
    Authors: Pandya and Pillai
    J Neurophysiol
  23. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
  24. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons.
    Authors: Mariqueo Et al.
    Mol Med Rep
  25. 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)
  26. In vivo epithelial wound repair requires mobilization of endogenous intracellular and extracellular calcium.
    Authors: Aihara Et al.
    Proc Natl Acad Sci U S A
  27. Divergent β-arrestin-dependent signaling events are dependent upon sequences within G-protein-coupled receptor C termini.
    Authors: Pal Et al.
    J Biol Chem
  28. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci
  29. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res
  30. 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.
  31. Reproducible and sustained regulation of Gαs signalling using a metazoan opsin as an optogenetic tool.
    Authors: Bailes Et al.
  32. 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
  33. The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
    Authors: Lee Et al.
  34. Gαq/11-mediated intracellular calcium responses to retrograde flow in endothelial cells.
    Authors: Melchior and Frangos
    J Pharmacol Exp Ther
  35. Apical and basolateral pools of proteinase-activated receptor-2 direct distinct signaling events in the intestinal epithelium.
    Authors: Lau Et al.
  36. 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
  37. The maturation of GABAergic transmission in visual cortex requires endocannabinoid-mediated LTD of inhibitory inputs during a critical period.
    Authors: Jiang Et al.
  38. Rat hypocretin/orexin neurons are maintained in a depolarized state by TRPC channels.
    Authors: Cvetkovic-Lopes Et al.
    PLoS One
  39. Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate.
    Authors: Sowa Et al.
    J Neurosci
  40. Plasticity of burst firing induced by synergistic activation of metabotropic glutamate and acetylcholine receptors.
    Authors: Moore Et al.
  41. Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling.
    Authors: Yin Et al.
  42. 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
  43. Endocannabinoids mediate muscarine-induced synaptic depression at the vertebrate neuromuscular junction.
    Authors: Newman Et al.
    Eur J Neurosci
  44. Mechanism of the vascular angiotensin II/α2-adrenoceptor interaction.
    Authors: Jackson Et al.
    Am J Physiol Cell Physiol
  45. PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate.
    Authors: Pierre Et al.
    EMBO J
  46. Phospholipase C activator m-3M3FBS affects Ca2+ homeostasis independently of phospholipase C activation.
    Authors: Krjukova Et al.
    Br J Pharmacol
  47. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    Am J Physiol Cell Physiol
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U 73343

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