• We aimed to investigate the contribution of neurons expressing transient receptor potential vanilloid subtype 1 (TRPV1) to alveolar bone homeostasis in periodontitis with diabetes. (physiciansweekly.com)
  • Transient receptor potential vanilloid-1 (TRPV1) is a member of the TRP family of channels that are responsible for nociceptive, thermal and mechanical sensations. (edu.au)
  • Capsaicin (CAP), the active ingredient of hot chilli peppers, is one of a number of related endogenous and plant-derived compounds (broadly termed 'vanilloid-like agents') that have been shown to induce apoptosis and inhibit cell proliferation in some cancer cells, through both TRPV1-dependent and -independent mechanisms. (edu.au)
  • Specific targeting by vanilloid-like agents toward TRPV1 on cancerous cells in patients with haematological malignancies may represent a novel therapeutic approach to treating these diseases. (edu.au)
  • 1) study the effect of TRPV1 agonists and antagonists on the viability of THP-1, U266B1 and U937 haematological malignant cell lines, 2) validate and optimise Western blotting and flow cytometry protocols to detect TRPV1 expression in leukocytes, 3) investigate TRPV1 expression in THP-1, U266B1 and U937 cells, and 4) compare TRPV1 expression in leukocytes obtained from patients with blood cancers to normal subjects. (edu.au)
  • In particular, there is a focus on the role of TRPV1 in cancer, including haematological malignancies (Chapter 1). (edu.au)
  • Knocking out the transient receptor potential vanilloid-1 (TRPV1) gene promotes the development of age-related obesity in mice: an insight into mechanisms. (mtak.hu)
  • The transient receptor potential vanilloid 1 (TRPV1) may play a role in the pathogenesis of ulcerative colitis (UC). (gastrocourse.ru)
  • TRP vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1) were reported to be triggered by mechanical stimuli, which is thought to function during mosquito piercing, as well as unpleasant chemicals or high temperature in HEK293T cells. (medicineinnovates.com)
  • A number of vanilloids, most notably capsaicin, bind to the transient receptor potential vanilloid type 1 (TRPV1) receptor, an ion channel which naturally responds to noxious stimuli such as high temperatures and acidic pH. (wikipedia.org)
  • Fatty acid amide hydrolase (FAAH), is a crucial enzyme for endovanilloid, and the N-acylethanolamines (NAEs), catabolism at TRPV1, and other cannabinoid receptors. (wikipedia.org)
  • Capsaicin receptor: TRPV1 a promiscuous TRP channel. (wikipedia.org)
  • Trpv1 - transient receptor potential cation. (wikigenes.org)
  • Those effects depend on the chronic activation of something called the transient receptor potential vanilloid 1 (TRPV1) channel found in the lining of blood vessels. (medicalnewstoday.com)
  • Transient receptor potential vanilloid 1 (TRPV1) modulates macrophage-mediated responses in sepsis, but its role in other pathogenic diseases has never been addressed. (hindawi.com)
  • Recently, a protective role for transient receptor vanilloid 1 (TRPV1), a nonselective cation channel found on both neuronal and nonneuronal cells, was suggested in bacteria-induced sepsis [ 7 - 10 ]. (hindawi.com)
  • 2015). Co-administration of transient receptor potential vanilloid 4 (TRPV4) and TRPV1 antagonists potentiate the effect of each drug in a rat model of cystitis . (up.pt)
  • It stimulates the 'transient receptor potential vanilloid 1' (TRPV1) receptor which is found in the nerves in the skin that detect pain. (europa.eu)
  • The rapid release of high doses of capsaicin from Qutenza overstimulates the TRPV1 receptors so they become less sensitive to the stimuli that normally cause neuropathic pain. (europa.eu)
  • 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)
  • The capsaicin- and heat-activated transient receptor potential vanilloid 1 (TRPV1) channel contributes to neurogenic inflammation and pain hypersensitivity, in part because of its potentiation downstream of phospholipase C-coupled receptors that regulate phosphoinositide lipid content. (jneurosci.org)
  • The research team developed Metabocin, which can be taken orally, to target receptors called TRPV1 (transient receptor potential vanilloid subfamily 1) that are found in high numbers in fat cells. (asianage.com)
  • Stimulating the TRPV1 receptors causes white fat cells to start burning energy instead of storing it, which, in theory, should cause weight loss. (asianage.com)
  • CGRP release was induced by either 60 mM K + (for depolarization-induced stimulation) or 100 nM capsaicin (for transient receptor potential vanilloid 1 (TRPV1) -induced stimulation) and measured using an enzyme-linked immunosorbent assay. (lu.se)
  • However, when the TRPV1 blocker AMG9810 (1 mM) was coapplied with ACEA, K + -induced CGRP release was significantly attenuated in the TG and dura. (lu.se)
  • Conclusions: Results from the present study indicate that ACEA per se does not exhibit antimigraine potential due to its dual agonistic properties, resulting in activation of both CB1 and TRPV1, and thereby inhibition and stimulation of CGRP release, respectively. (lu.se)
  • In terms of lipolysis, capsaicinoids are an agonist of the transient receptor potential vanilloid subfamily member 1 (TRPV1). (biomedcentral.com)
  • This TRPV1 releases the substance P, which in turn activates the postsynaptic receptor of substance P, neurokinin-1. (biomedcentral.com)
  • Transient receptor potential channel vanilloid subfamily 4 (TRPV4), a member of TRP family, is a mechanosensitive non-selective cation channel. (nih.gov)
  • We used cryo-electron microscopy to capture the epithelial calcium channel TRPV6 (transient receptor potential vanilloid subfamily member 6) inactivated by CaM. (columbia.edu)
  • Ablation of transient receptor potential vanilloid subtype 1-expressing neurons in rat trigeminal ganglia aggravated bone resorption in periodontitis with diabetes. (physiciansweekly.com)
  • Responses were compared with those in mice deficient in the cold/menthol receptor, TRPM8, expressed in trigeminal sensory neurons innervating the oral cavity. (bmj.com)
  • Capsaicin, an active ingredient of chili peppers, is a potent exogenous agonist for transient receptor potential vanilloid 1 receptors. (cabi.org)
  • Capsaicin also activates the transient potential vanilloid 1 receptor of C-type pain sensors in mammals. (cleveland.edu)
  • The aim of the present study was to examine the effect of the synthetic endocannabinoid (eCB) analogue, arachidonyl-2′-chloroethylamide (ACEA), on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to activate G i/o -coupled cannabinoid receptors type 1 (CB1), resulting in neuronal inhibition. (lu.se)
  • coupled cannabinoid receptors type 1 (CB1), resulting in neuronal inhibition. (lu.se)
  • Background: Based on the current understanding of the role of neuropeptide signalling in migraine, we explored the therapeutic potential of a specific cannabinoid agonist. (lu.se)
  • The mechanism of activation of the transient receptor potential vanilloid 4 (TRPV4) channel by 4α-phorbol esters was investigated by combining information from chemical modification of 4α-phorbol-didecanoate (4α-PDD, 2a ), site-directed mutagenesis, Ca 2+ imaging, and electrophysiology. (acs.org)
  • The transient receptor potential (TRP) vanilloid 4 (TRPV4) member of the TRP superfamily has recently been implicated in numerous physiological processes. (aspetjournals.org)
  • In this study, we describe a small molecule TRPV4 channel activator, ( N -((1 S )-1-{[4-((2 S )-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), which we have used as a valuable tool in investigating the role of TRPV4 in the urinary bladder. (aspetjournals.org)
  • GSK1016790A elicited Ca 2+ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC 50 values of 18 and 2.1 nM, respectively), and it evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. (aspetjournals.org)
  • The auditory threshold shift was significantly larger in the TRPV4 knockout than in the TRPV4+/+ mice 1 week after the acoustic overexposure of 128dB SPL. (nih.gov)
  • Derouiche S, Li T, Sakai Y, Uta D, Aoyagi S, Tominaga M. Inhibition of transient receptor potential vanilloid 1 and transient receptor potential ankyrin 1 by mosquito and mouse saliva . (medicineinnovates.com)
  • 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)
  • Several ion channels, including transient receptor potential (TRP) channels are expressed in these sensory nerve terminals and may detect unpleasant stimuli. (medicineinnovates.com)
  • This provides a molecular basis for understanding the potential action of menthol and other compounds and their ability to produce both a cooling sensation and reduction of pain associated with a variety of painful stimuli and conditions. (cleveland.edu)
  • 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)
  • Recent studies reported that treatment by the extracellular domain of Klotho (KLe) increases cell-surface abundance of transient receptor potential vanilloid type isoform 5, an epithelial Ca 2+ channel critical for Ca 2+ reabsorption in the kidney. (aspetjournals.org)
  • Removal of sialic acids exposes underlying disaccharide galactose- N -acetylglucosamine, a ligand for a ubiquitous galactoside-binding lectin galectin-1. (aspetjournals.org)
  • The new N-terminal peptide is a cryptic ligand for the receptor. (curehunter.com)
  • Transient receptor potential melastin-8 (TRPM8), a cationic ion channel, generates a normal cooling sensation in mammals. (cleveland.edu)
  • The data described herein confirm TRPV3 as a potent inducer of epidermal inflammation, with collaborators revealing a clear link between TRPV3-evoked PAI-1 release and skin-derived itch. (dcu.ie)
  • The molecular underpinnings common to and connecting these disorders are not known, but may include shared genetic risk factors ( 1 , 8 ), regulation of brain cations ( 9 , 10 ), or common receptor signaling events that activate pain ( 11 ), inflammation ( 12 ), or oxidative ( 13 ) pathways. (frontiersin.org)
  • A biphasic effect on metabolic activity was observed on THP-1 cells [EC50, IC50 (95% CI) = 32.9 (19.9-54.3), 219 (144-246) ˜í¬¿M]. U266B1 cells were more resistant to CAP-induced death than THP-1 and U937 cells. (edu.au)
  • Basal p38 Mitogen-Activated Protein Kinase Regulates Unliganded Glucocorticoid Receptor Function in Airway Smooth Muscle Cells. (ndriresource.org)
  • 2009). Functional Transient Receptor Potential Vanilloid 1 is Expressed in Human Urothelial Cells . (up.pt)
  • Cannabinoid type-2 (CB 2 ) receptor activation was shown to reduce the production of the monocyte chemotactic protein-2 (MCP-2) chemokine in polyinosinic-polycytidylic acid [poly-(I:C)]-stimulated human keratinocyte (HaCaT) cells, an in vitro model of allergic contact dermatitis (ACD). (aspetjournals.org)
  • We discuss the current knowledge about sex differences in migraine and its comorbidities, and focus on the potential role of mast cells (MCs) in both. (frontiersin.org)
  • MC-neuron bidirectional communication uniquely positions these cells as potential initiators and/or perpetuators of pain. (frontiersin.org)
  • 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)
  • The analysis of CGRP release data was combined with immunohistochemistry in order to study the cellular localization of CB1, cannabinoid receptor type 2 (CB2), CGRP and receptor activity modifying protein 1 (RAMP1), a subunit of the functional CGRP receptor, in the TG. (lu.se)
  • Here, we report that KLe treatment increases the cell-membrane abundance of the renal K + channel renal outer medullary potassium channel 1 (ROMK1) by removing terminal sialic acids from N -glycan of the channel. (aspetjournals.org)
  • Binding to galectin-1 at the extracellular surface prevents clathrin-mediated endocytosis of ROMK1 and leads to accumulation of functional channel on the plasma membrane. (aspetjournals.org)
  • Interestingly, acid-sensing ion channel (ASIC) 1, 2a, 2b, and 3 mRNAs were decreased in the DRG, and this reduction was strongest in females. (jneurosci.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)
  • Unsupervised clustering analyses revealed the phasic nature of TRPV3- induced calcium flux and highlighted the role of SNARE-mediated receptor cycling in normal TRPV3 activity. (dcu.ie)
  • The extracellular domain of Klotho, a type-1 membrane protein, is secreted into urine and blood and may function as an endocrine or paracrine hormone. (aspetjournals.org)
  • As with all medicines, the potential harms - and the risk of developing a substance abuse disorder - should be considered, especially for this patient group [ 5 ]. (karger.com)
  • MCs can secrete nociceptor sensitizing and activating agents, such as serotonin, prostaglandins, histamine, and proteolytic enzymes that can also activate the pain-mediating transient receptor potential vanilloid channels. (frontiersin.org)
  • Hypoxic pulmonary vasoconstriction (HPV), also known as the von Euler-Liljestrand mechanism, is an intrinsic mechanism of the pulmonary vasculature in response to alveolar hypoxia, to match ventilation to perfusion and optimise pulmonary gas exchange ( figure 1 ). (ersjournals.com)
  • Transient receptor potential vanilloid 4 activation constricts the human bronchus via the release of cysteinyl leukotrienes. (ndriresource.org)
  • Our findings indicate that glucocorticoid-induced adhesion is dependent on CB(1) /CB(2) /TRPV-1 activation. (uni-regensburg.de)
  • This activation of neurokin-1 results in an increased activation of the sympathetic nervous system, leading to the release of epinephrine (EPI) and norepinephrine (NE) from adrenal gland [ 20 ]. (biomedcentral.com)
  • Mu-Opioid Receptors (MORs) are well-known for participating in analgesia, sedation, drug addiction, and other physiological functions. (researchgate.net)
  • pharmacodynamic effects such as desensitization of adenyl cyclase and down-regulation of beta-adrenergic receptors and serotonin receptors also appear to play role in its mechanisms of action. (medscape.com)
  • Journal of Pharmacology and Experimental Therapeutics 349(1): 118-125. (ndriresource.org)
  • The most common side effects with Qutenza (seen in more than 1 patient in 10) are pain and redness at the site of application. (europa.eu)
  • Chronic itch affects about to 1 in 5 people worldwide (Hay et al. (dcu.ie)
  • 1 , 2 Menthol adds a fresh, cooling and minty taste, sensations that are reminiscent of other tobacco products such as menthol cigarettes and of confectionary products such as chewing gum and mint lozenges. (bmj.com)
  • Common migraine comorbidities affect multiple organ systems in addition to the CNS ( 1 ). (frontiersin.org)
  • Journal of Urology, 181 (1), 379 - 386. (up.pt)
  • human testis tissue were subjected to SDS PAGE followed by western blot with 55388-1-AP (PKA C-alpha speicifc antibody) at dilution of 1:500 incubated at room temperature for 1.5 hours. (ptglab.com)
  • Immunohistochemical analysis of paraffin-embedded human colon cancer slide using 55388-1-AP (PKA C-alpha speicifc antibody at dilution of 1:50. (ptglab.com)
  • 1 A series of high-throughput methods have changed cancer research and therapy. (dovepress.com)