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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 337.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.96 mL||14.82 mL||29.64 mL|
|5 mM||0.59 mL||2.96 mL||5.93 mL|
|10 mM||0.3 mL||1.48 mL||2.96 mL|
|50 mM||0.06 mL||0.3 mL||0.59 mL|
References are publications that support the biological activity of the product.
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
Mouchbahani-Constance et al (2018) Lionfish venom elicits pain predominantly through the activation of nonpeptidergic nociceptors. Pain. 159 2255 PMID: 29965829
If you know of a relevant reference for AMG 9810, please let us know.
Keywords: AMG 9810, AMG 9810 supplier, Potent, selective, competitive, antagonists, TRPV1, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, AMG9810, TRPV, 2316, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for AMG 9810 include:
Mouchbahani-Constance et al (2018) Lionfish venom elicits pain predominantly through the actiation of non-peptidergic nociceptors. Pain PMID: 29965829
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
Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Oncotarget 9 457 PMID: 26648844
Pitcher et al (2007) Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia. J Transl Med 3 17 PMID: 17603899
Pearce et al (2019) Combination of a Rapidly Penetrating Agonist and a Slowly Penetrating Antagonist Affords Agonist Action of Limited Duration at the Cellular Level. Biomol Ther (Seoul) 27 435 PMID: 31302951
Chen et al (2019) fMRI indicates cortical activation through TRPV1 modulation during acute gouty attacks. Sci Rep 9 12348 PMID: 31451732
Montrucchio et al (2013) Plant derived aporphinic alkaloid S-(+)-dicentrine induces antinociceptive effect in both acute and chronic inflammatory pain models: evidence for a role of TRPA1 channels. PLoS One 8 e67730 PMID: 23861794
Saloman et al (2013) P2X? and TRPV1 functionally interact and mediate sensitization of trigeminal sensory neurons. Neuroscience 232 226 PMID: 23201260
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
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
David-Pereira (2017) The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex. Neuroscience 349 341 PMID: 28300633
Li et al (2015) The Cancer Chemotherapeutic PacT. Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4. J Neurosci 35 13487 PMID: 26424893
Hakimizadeh et al (2012) Endocannabinoid System and TRPV1 Receptors in the Dorsal Hippocampus of the Rats Modulate Anxiety-like Behaviors. Iran J Basic Med Sci 15 795 PMID: 23493622
Yan et al (2011) Dural afferents express acid-sensing ion channels: a role for decreased meningeal pH in migraine headache. Pain 152 106 PMID: 20971560
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
Jeong et al (2018) Activation of temperature-sensitive TRPV1-like receptors in ARC POMC neurons reduces food intake. PLoS Biol 16 e2004399 PMID: 29689050
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
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We used KN62 for calcium imaging experiments and western blotting work. The data were published in Br. J Pharmacol. 2017
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.