It has a melting point of 71.5-74.5 °C. Zucapsaicin mediates an antinociceptive action via acting as an agonist at TRPV1. (wikipedia.org)
Zucapsaicin mediates an antinociceptive action via acting as an agonist at TRPV1. (wikipedia.org)
Zucapsaicin excites and desensitizes C-fibers via agonist at TRPV1 on nociceptive neurons. (wikipedia.org)
It is suggested that this compound, similarly to its trans isomer, is an agonist of the vanilloid receptor VR1 (TRPV1) and a neuronal calcium channel blocker. (wikipedia.org)
It was shown that desensitization and tachyphylaxis of TRPV1 channels contribute to capsaicin-induced pain relief. (wikipedia.org)
Background Transient receptor potential cation channel subfamily V member 1 (TRPV1) are sensitive to heat, capsaicin, pungent chemicals and other noxious stimuli. (researchgate.net)
Methods A next-generation sequencing (NGS) panel was created for the human TRPV1 gene and in addition, for the leukotriene receptors BLT1 and BLT2 recently described to modulate TRPV1 mediated sensitisation processes rendering the coding genes LTB4R and LTB4R2 important co-players in pharmacogenetic approaches involving TRPV1. (researchgate.net)
The method adds a large amount of genetic information as a basis for complete analysis of TRPV1 ion channel genetics and its functional consequences. (researchgate.net)
This study focused on the expression and functionality of TRPV1, a nonselective cation channel that was found to be expressed in different carcinoma tissues. (dovepress.com)
In this study, stimulation by the TRPV1 agonist, capsaicin, of SUM149PT cells, a model system for the most aggressive breast cancer subtype, triple-negative breast cancer, led to intracellular calcium signals that were diminished by the specific TRPV1 antagonist, capsazepin. (dovepress.com)
In conclusion, the current study revealed the expression profiles of human TRP channels in 60 different breast cancer tissues and cell lines and furthermore validated the antitumor activity of TRPV1 against SUM149PT breast cancer cells, indicating that activation of TRPV1 could be used as a therapeutic target, even in the most aggressive breast cancer types. (dovepress.com)
9 TRP channels play an important role in the development of several diseases, and one of the most investigated and described TRP channel is TRPV1. (dovepress.com)
10 TRPV1 agonist, capsaicin, is capable of inducing apoptosis 11 , 12 and inhibiting cancer cell growth by cell cycle arrest in many different types of cancer, for example, osteosarcoma, colon, and pancreatic cancer cells, while normal cells remained unharmed. (dovepress.com)
Calcium entry through transient receptor potential vanilloid 1 (TRPV1) ion channels modulates the delicate balance between proliferation and apoptosis. (encyclopedia.pub)
The opening of transient receptor potential vanilloid 1 (TRPV1) ligand-gated ion channels facilitates transmembrane Ca 2+ and Na + entry, which modifies the delicate balance between apoptotic and proliferative signaling pathways. (encyclopedia.pub)
Transient receptor potential vanilloid member 1 (TRPV1) is a heat and capsaicin receptor that allows cations to permeate and cause pain. (bvsalud.org)
In this study, we directly visualized single-molecule structural fluctuations of the TRPV1 channels in a lipid bilayer with the ligands resiniferatoxin (agonist, 1,000 times hotter than capsaicin) and capsazepine (antagonist) by high-speed atomic force microscopy. (bvsalud.org)
Expression of the GFRα3 receptor is primarily restricted to the peripheral nervous system and is found in a subpopulation of nociceptive sensory neurons of the dorsal root ganglia (DRGs) that coexpress the Ret and TrkA receptor tyrosine kinases and the thermosensitive channel TRPV1. (jneurosci.org)
Expression of artemin caused a 20.5% increase in DRG neuron number and increased the level of mRNA encoding GFRα3, TrkA, TRPV1, and the putative noxious cold-detecting channel TRPA1. (jneurosci.org)
Here, we investigated the antinociceptive effect of PCW in complete freund's adjuvant (CFA)-induced mice and its possible mechanisms associated with opioid system and TRPV1 ion channel. (biomedcentral.com)
This effect may result from the activation of κ-opioid receptor via dynorphin release and the inhibition of TRPV1. (biomedcentral.com)
Capsaicin receptor1
It is a modulator of transient receptor potential cation channel subfamily V member 1 (TRPV-1), also known as the vanilloid or capsaicin receptor 1 that reduces pain, and improves articular functions. (wikipedia.org)
Epidermal growth f2
whereas human epidermal growth factor receptor 2 (HER2)-positive breast cancers can be targeted by specific drugs, the triple-negative breast cancer phenotype is defined by chromosomal instability and low expression levels of estrogen receptor (ER) alpha, progesterone receptor (PR), and HER2, rendering treatment rather difficult. (dovepress.com)
Proliferation is upregulated through two mechanisms: (1) ATP binding to the G-protein-coupled receptor P2Y2, commencing a kinase signaling cascade that activates the serine-threonine kinase Akt, and (2) the transactivation of the epidermal growth factor receptor (EGFR), leading to a series of protein signals that activate the extracellular signal-regulated kinases (ERK) 1/2. (encyclopedia.pub)
TRPV45
Among these is the vanilloid TRP (TRPV) comprised of 6 members including TRPV4 which is found to be expressed in the vasculature, endothelial cells (ECs) and vascular smooth muscle cells (VSMCs) according to western blotting, RT-PCR and immunohistochemistry studies (3, 4). (herts.ac.uk)
As a cation channel, TRPV4 mediates Ca+2 influx that plays a major role in endothelium-dependent vasodilation (VD) and VSMCs hyperpolarization and hence VD (5, 6). (herts.ac.uk)
Arterial rings were pre-contracted with noradrenaline (300nM) followed by TRPV4-agonist, RN-1747 (3nM-3µM) to evoke relaxation dose response curves. (herts.ac.uk)
These results showed the TRPV4 function is compromised in both endothelial and VSMC and is in part due to reduction in channel number. (herts.ac.uk)
Diabetes-induced lipolysis might accelerate the degradation of caveolae, a cone shaped pocket of proteins and lipids serves as a docking site for channels and receptors in endothelium and hence reduce levels of caveolin-associated TRPV4 so compromising vascular function (7). (herts.ac.uk)
Inhibition4
Conversely, inhibition of PVA neuronal activity using DREADDs (designer receptors exclusively activated by designer drugs) or inactivation of PVA extracellular signal-regulated kinase at the critical time window blunted mechanical hyperalgesia in chronic pain models. (iasp-pain.org)
these were abrogated by pharmacological inhibition of TRPA1 channel activity, disruption of TRPA1 channel function or removal of extracellular Ca 2+ . (biomedcentral.com)
Inhibition of TRPA1 channel activity exacerbated Aβ 1-42 -induced astrogliosis but inhibited Aβ 1-42 -increased PP2B activation, the production of pro-inflammatory cytokines and activities of transcriptional factors NF-κB and NFAT in astrocytes and in APP/PS1 Tg mice. (biomedcentral.com)
It is well-known that activation of opioid receptors result in the inhibition of chronic inflammatory pain [ 3 ]. (biomedcentral.com)
Neuronal1
Artemin, a neuronal survival factor in the glial cell line-derived neurotrophic factor family, binds the glycosylphosphatidylinositol-anchored protein GFRα3 and the receptor tyrosine kinase Ret. (jneurosci.org)
Transmembrane1
Transient receptor potential ankyrin 1 (TRPA1) channel is a type of nonselective transmembrane cation channel with multiple ankyrin repeats on its N-terminal [ 17 - 20 ]. (biomedcentral.com)
Ligands1
GDNF family ligands (GFLs) activate the Ret receptor tyrosine kinase through binding of glycosylphosphatidylinositol-anchored GDNF family receptor α coreceptors (GFRα1-4) ( Sariola and Saarma, 2003 ). (jneurosci.org)
Calcium3
ii) activation of phospholipase C with the subsequent phosphatidylinositol 4,5-biphosphate hydrolysis (rather controversial) and iii) activation of calcium-dependent protein kinase C isoforms and subsequent channel phosphorylation. (wikipedia.org)
Transient receptor potential (TRP) channels contribute to the regulation of intracellular calcium, which can promote cancer hallmarks in cases of dysregulation of gene transcription and calcium-dependent pro-proliferative or anti-apoptotic mechanisms. (dovepress.com)
Transient receptor potential (TRP) channels, which are membranous ion channels that conduct calcium and sodium ions, have been shown to influence cancer cell growth. (dovepress.com)
Antagonist1
PCW dose-dependently attenuated mechanical and heat hypersensitivities with no tolerance, which could be partially attenuated by coadministration of κ-opioid receptor antagonist nor-BNI or anti-dynorphin A (1-13) antiserum. (biomedcentral.com)
Neuropathic pain1
They are mainly distributed in C sensory nerve fibers as well as Aẟ fibers to transmit sensory information involving inflammatory and neuropathic pain, and activation of these channels releases somatostatin, calcitonin gene-related peptide (CGRP) and other neuropeptides (neurokinin A, kassinin), leading to neurogenic inflammation [A19720]. (wikipedia.org)
Nociceptor1
Here, we showed that GM-CSF promotes bone cancer-associated pain by enhancing excitability of DRG neurons via the Jak2-Stat3-mediated upregulation of expression of nociceptor-specific voltage-gated sodium channels. (iasp-pain.org)
Nociceptive1
The present study was designed to demonstrate the vasosensory reflex responses evoked by thermal nociceptive stimuli in anaesthetised rat models and to examine the role of perivascular histamine receptors in mediating these responses. (ijpp.com)
Intracellular2
It binds to intracellular sites and initially stimulates the channels, causing burning sensation. (wikipedia.org)
Upon detection of these signals, the TRPA1 channel is activated, which results in increased intracellular Ca 2+ levels and activated downstream signaling cascades [ 17 - 20 ]. (biomedcentral.com)
Temperature2
7 , 8 These channels can be activated by many stimuli, including temperature or pH changes in the extracellular space. (dovepress.com)
Perivascular histamine receptors play a significant role in mediating the temperature-induced vasosensory reflex responses. (ijpp.com)
Neurons2
All these events are primarily regulated by an array of regulatory proteins that are present on the cell surface, such as ion channels, receptors and adhesion molecules which sense the different chemical signaling cues and allow the neurons to respond accordingly [ 8-10 ]. (silverchair.com)
The voltage gated Na channels Nav1.7, Nav1.8 and Nav1.9 were found to be selectively up-regulated in rat DRG neurons treated with GM-CSF, which resulted in enhanced excitability. (iasp-pain.org)
Apoptosis1
Two major mechanisms of apoptosis are an extrinsic, death-receptor mediated mechanism, and an intrinsic, mitochondria-mediated mechanism [ 4 ] . (encyclopedia.pub)
Inflammatory2
Ablation of TRPA1-channel function in APP/PS1 Tg mice alleviated behavioral dysfunction, Aβ plaque deposition and pro-inflammatory cytokine production but increased astrogliosis in brain lesions. (biomedcentral.com)
These findings indicate that PCW might be a potential agent for the management of chronic inflammatory pain. (biomedcentral.com)
Roles1
Potassium (K), the main cation inside cells, plays roles in maintaining cellular osmolarity and acid-base equilibrium, as well as nerve stimulation transmission, and regulation of cardiac and muscle functions. (mdpi.com)
Therapeutic potential2
Cannabidiol or CBD is a non-intoxicating component of the cannabis plant with enormous therapeutic potential. (holisticcanna.com)
our data also highlight the therapeutic potential of targeting GM-CSF. (iasp-pain.org)
Role2
In this work, we explored the role of transient receptor potential vanilloid 2 (TRPV2), a non-selective cation channel in the context of neurite functions. (silverchair.com)
The protein expression of TRPA1 channels was higher in brains, mainly astrocytes of the hippocampus, from APP/PS1 Tg mice than WT mice. (biomedcentral.com)
TRPA11
However, little is known about the significance of the TRPA1 channel in the pathophysiology of Alzheimer's disease (AD). (biomedcentral.com)
Expression1
however, no study has examined the expression profiles of human TRP channels in breast cancer on a large scale. (dovepress.com)
Regulation2
Indeed, changes in the spatiotemporal Ca 2+ -levels and Ca 2+ -oscillation patterns have been correlated with most of these functions [ 2 , 8-10 ], which strongly suggest the importance of different Ca 2+ channels in the regulation of neuritogenesis. (silverchair.com)