Chemical Name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide
Biological ActivityPotent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.
Doherty et al.
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.
Lionfish venom elicits pain predominantly through the activation of nonpeptidergic nociceptors.
Mouchbahani-Constance et al.
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
fMRI indicates cortical activation through TRPV1 modulation during acute gouty attacks.
Authors: Chen Et al.
Sci Rep 2019;9:12348
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
Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake.
Authors: Jeong Et al.
PLoS Biol 2018;16:e2004399
Lionfish venom elicits pain predominantly through the actiation of non-peptidergic nociceptors.
Authors: Mouchbahani-Constance Et al.
The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex.
Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex.
Authors: Martin Et al.
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
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
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
P2X? and TRPV1 functionally interact and mediate sensitization of trigeminal sensory neurons.
Authors: Saloman Et al.
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
Endocannabinoid System and TRPV1 Receptors in the Dorsal Hippocampus of the Rats Modulate Anxiety-like Behaviors.
Authors: Hakimizadeh Et al.
Iran J Basic Med Sci 2012;15:795
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
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
Dural afferents express acid-sensing ion channels: a role for decreased meningeal pH in migraine headache.
Authors: Yan Et al.
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
Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia.
Authors: Pitcher Et al.
J Transl Med 2007;3:17
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