Catalog Number: 2316
Chemical Name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide
Biological Activity
Potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM). Inhibits capsaicin-, proton-, heat- and endogenous ligand-induced activation of human and rat recombinant TRPV1 receptors. Displays antihyperalgesic properties in a rat model of inflammatory pain.
Technical Data
  • M.Wt:
    337.42
  • Formula:
    C21H23NO3
  • Solubility:
    Soluble to 50 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Desiccate at +4°C
  • CAS No:
    545395-94-6
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.
Background References
  1. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
    Doherty et al.
    J.Med.Chem., 2005;48:71
  2. AMG 9810 [(E)-3-(4-t-Butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties.
    Gavva et al.
    J.Pharmacol.Exp.Ther., 2005;313:474
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AMG 9810 include:

8 Citations: Showing 1 - 8
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  1. The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex.
    Authors: David-Pereira
    Neuroscience 2017;349:341
  2. Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex.
    Authors: Martin Et al.
    Oncotarget 2015;9:457
  3. Mother root of Aconitum carmichaelii Debeaux exerts antinociceptive effect in Complet Freund's Adjuvant-induced mice: roles of dynorpin/κ-opioid system and transient receptor potential vanilloid type-1 ion channel.
    Authors: Wang Et al.
    Proc Natl Acad Sci U S A 2015;13:284
  4. 5,6-EET is released upon neuronal activity and induces mechanical pain hypersensitivity via TRPA1 on central afferent terminals.
    Authors: Sisignano Et al.
    J Neurosci 2012;32:6364
  5. Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors.
    Authors: Gregus Et al.
    Proc Natl Acad Sci U S A 2012;109:6721
  6. Resolvin D2 is a potent endogenous inhibitor for transient receptor potential subtype V1/A1, inflammatory pain, and spinal cord synaptic plasticity in mice: distinct roles of resolvin D1, D2, and E1.
    Authors: Park Et al.
    Front Cell Neurosci 2011;31:18433
  7. Activation of TRPV1 in the spinal cord by oxidized linoleic acid metabolites contributes to inflammatory hyperalgesia.
    Authors: Patwardhan Et al.
    J Neurosci 2009;106:18820
  8. Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia.
    Authors: Pitcher Et al.
    J Transl Med 2007;3:17

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