AMG 9810

Cat. No. 2316

AMG 9810 C21H23NO3 [545395-94-6]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Doherty et al (2005) Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J.Med.Chem. 48 71. PMID: 15634002.

Gavva et al (2005) 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. J.Pharmacol.Exp.Ther. 313 474. PMID: 15615864.

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Citations are publications that use Tocris products. Selected citations for AMG 9810 include:

Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Oncotarget 9 457. PMID: 26648844.

Wang et al (2015) 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. Proc Natl Acad Sci U S A 13 284. PMID: 26320055.

Gregus et al (2012) Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors. Proc Natl Acad Sci U S A 109 6721. PMID: 22493235.

Sisignano et al (2012) 5,6-EET is released upon neuronal activity and induces mechanical pain hypersensitivity via TRPA1 on central afferent terminals. J Neurosci 32 6364. PMID: 22553041.

Park et al (2011) 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. Front Cell Neurosci 31 18433. PMID: 22171045.

Patwardhan et al (2009) Activation of TRPV1 in the spinal cord by oxidized linoleic acid metabolites contributes to inflammatory hyperalgesia. J Neurosci 106 18820. PMID: 19843694.

Pitcher et al (2007) Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia. J Transl Med 3 17. PMID: 17603899.

Do you know of a great paper that uses AMG 9810 from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: AMG 9810, supplier, Potent, selective, competitive, antagonists, TRPV1, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, AMG9810, Tocris Bioscience, TRPV Antagonist products

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