Home / TRPV Antagonists / AMG 9810

AMG 9810

Catalog #: 2316
17 Citations Datasheet / COA / SDS
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2316/10
2316/50
AMG 9810 | CAS No. 545395-94-6 | TRPV Antagonists
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Description: Potent and selective TRPV1 competitive antagonist

Chemical Name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide

Purity: ≥98%

Product Details
Citations (17)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

AMG 9810 is a 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:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. IL-33/ST2 signaling excites sensory neurons and mediates itch response in a mouse model of poison ivy contact allergy

    Proc. Natl. Acad. Sci. U.S.A., 2016;0(0):.
  2. Epiregulin and EGFR interactions are involved in pain processing
    LJ Martin, SB Smith, A Khoutorsky, CA Magnussen, A Samoshkin, RE Sorge, C Cho, N Yosefpour, S Sivaselvac, S Tohyama, T Cole, TM Khuong, E Mir, DG Gibson, JS Wieskopf, SG Sotocinal, JS Austin, CB Meloto, JH Gitt, C Gkogkas, N Sonenberg, JD Greenspan, RB Fillingim, R Ohrbach, GD Slade, C Knott, R Dubner, AG Nackley, A Ribeiro-da, GG Neely, W Maixner, DV Zaykin, JS Mogil, L Diatchenko
    J. Clin. Invest., 2017;0(0):.
  3. The Complement System Component C5a Produces Thermal Hyperalgesia via Macrophage-to-Nociceptor Signaling That Requires NGF and TRPV1

    J Neurosci, 2016;36(18):5055-70.
  4. The endocannabinoid/endovanilloid N-arachidonoyl dopamine (NADA) and synthetic cannabinoid WIN55,212-2 abate the inflammatory activation of human endothelial cells.
    Wilhelmsen K, Khakpour S, Tran A, Sheehan K, Schumacher M, Xu F, Hellman J
    J Biol Chem, 2014;289(19):13079-100.
  5. 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
  6. 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
  7. Lionfish venom elicits pain predominantly through the activation of nonpeptidergic nociceptors.
    Mouchbahani-Constance et al.
    Pain., 2018;159:2255

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Citations for AMG 9810

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

17 Citations: Showing 1 - 10

  1. fMRI indicates cortical activation through TRPV1 modulation during acute gouty attacks.
    Authors: Chen Et al.
    Sci Rep  2019;9:12348
  2. Combination of a Rapidly Penetrating Agonist and a Slowly Penetrating Antagonist Affords Agonist Action of Limited Duration at the Cellular Level.
    Authors: Pearce Et al.
    Biomol Ther (Seoul)  2019;27:435
  3. Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake.
    Authors: Jeong Et al.
    PLoS Biol  2018;16:e2004399
  4. Lionfish venom elicits pain predominantly through the actiation of non-peptidergic nociceptors.
    Authors: Mouchbahani-Constance Et al.
    Pain  2018;
  5. 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
  6. Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex.
    Authors: Martin Et al.
    Oncotarget  2015;9:457
  7. The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4.
    Authors: Li Et al.
    J Neurosci  2015;35:13487
  8. 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
  9. Plant derived aporphinic alkaloid S-(+)-dicentrine induces antinociceptive effect in both acute and chronic inflammatory pain models: evidence for a role of TRPA1 channels.
    Authors: Montrucchio Et al.
    PLoS One  2013;8:e67730
  10. P2X? and TRPV1 functionally interact and mediate sensitization of trigeminal sensory neurons.
    Authors: Saloman Et al.
    Neuroscience  2013;232:226

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