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https://www.readbyqxmd.com/read/28905239/expression-and-distribution-of-three-transient-receptor-potential-vanilloid-trpv-channel-proteins-in-human-odontoblast-like-cells
#1
Wen Wen, Kehua Que, Chengcheng Zang, Jing Wen, Guangxu Sun, Zhiying Zhao, Yanzhong Li
Odontoblasts have been suggested to contribute to nociceptive sensation in the tooth via expression of the transient receptor potential (TRP) channels. The TRP channels as a family of nonselective cation permeable channels play an important role in sensory transduction of human. In this study, we examined the expression of transient receptor potential vanilloid-1 (TRPV1), transient receptor potential vanilloid-2 (TRPV2) and transient receptor potential vanilloid-3 (TRPV3) channels in native human odontoblasts (HODs) and long-term cultured human dental pulp cells with odontoblast phenotyoe (LHOPs) obtained from healthy wisdom teeth with the use of immunohistochemistry (IHC), immunofluorescence (IF), quantitative real-time polymerase chain reaction (qRT-PCR),western blotting (WB) and immunoelectron microscopy (IEM) assay...
September 13, 2017: Journal of Molecular Histology
https://www.readbyqxmd.com/read/28903355/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#2
Francesca Punzo, Chiara Tortora, Daniela Di Pinto, Iolanda Manzo, Giulia Bellini, Fiorina Casale, Francesca Rossi
Osteosarcoma is the most common and aggressive bone tumor in children. The Endocannabinoid/Endovanilloid system has been proposed as anticancer target in tumor of different origins. This system is composed of two receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel and their ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells. We investigated the effects of JWH-133 (CB2 agonist) and RTX (TRPV1 agonist) in six human Osteosarcoma cell lines: MG-63, U-2OS, MNNG/HOS, Saos-2, KHOS/NP, Hs888Lu, by Apoptosis and Migration-Assay...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28903060/effects-of-curcumin-and-curcumin-analogues-on-trp-channels
#3
Marianna Nalli, Giorgio Ortar, Aniello Schiano Moriello, Vincenzo Di Marzo, Luciano De Petrocellis
A series of 33 curcumin analogues was synthesized and tested on TRPA1, TRPM8, and TRPV1 channels. Twenty of them acted as good modulators of TRPA1 channels. None was able to significantly activate TRPM8 channels, while curcumin itself and six curcuminoids belonging to the 1,3-dicarbonyl and acyclic series behaved as 'true' antagonists with IC50 values<5μM. Only few curcuminoids were able to modulate TRPV1 channels with EC50 and IC50 values ranging from 3.4 and 6.0μM.
September 10, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28901432/effects-of-coadministration-of-low-dose-cannabinoid-type-2-receptor-agonist-and-morphine-on-vanilloid-receptor-1-expression-in-a-rat-model-of-cancer-pain
#4
Mingyue Zhang, Meng Chi, Huichao Zou, Songyu Tian, Zhaodi Zhang, Guonian Wang
Morphine is widely used as an analgesic to treat moderate to severe pain, but chronic morphine use is associated with development of tolerance and dependence, which limits its analgesic efficacy. Our previous research has showed that nonanalgetic dose of a cannabinoid type 2 (CB2) receptor agonist reduced morphine tolerance in cancer pain. A previous study showed the colocalization of CB2 and transient receptor potential vanilloid 1 (TRPV1) in human and rat dorsal root ganglia (DRG) sensory neurons. Whether coadministration of a CB2 receptor agonist and morphine could reduce TRPV1 expression in morphine‑induced antinociception and tolerance in cancer pain is unclear...
September 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28899508/pellitorine-an-extract-of-tetradium-daniellii-is-an-antagonist-of-the-ion-channel-trpv1
#5
Zoltán Oláh, Dóra Rédei, László Pecze, Csaba Vizler, Katalin Jósvay, Péter Forgó, Zoltán Winter, György Dombi, Gerda Szakonyi, Judit Hohmann
BACKGROUND: Transient Receptor Potential Vanilloid 1 (TRPV1) confers noxious heat and inflammatory pain signals in the peripheral nervous system. Clinical trial of resiniferatoxin from Euphorbia species is successfully aimed at TRPV1 in cancer pain management and heading toward new selective painkiller status that further validates this target for drug discovery efforts. Evodia species, used in traditional medicine for hundreds of years, are a recognised source of different TRPV1 agonists, but no antagonist has yet been reported...
October 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28892388/novel-radiolabeled-vanilloid-with-enhanced-specificity-for-human-transient-receptor-potential-vanilloid-1-trpv1
#6
Larry V Pearce, Jihyae Ann, Aeran Jung, Shivaji A Thorat, Brienna K A Herold, Amelework D Habtemichael, Peter M Blumberg, Jeewoo Lee
Transient receptor potential vanilloid 1 (TRPV1) has emerged as a promising therapeutic target. While radiolabeled resiniferatoxin (RTX) has provided a powerful tool for characterization of vanilloid binding to TRPV1, TRPV1 shows 20-fold weaker binding to the human TRPV1 than to the rodent TRPV1. We now describe a tritium radiolabeled synthetic vanilloid antagonist, 1-((2-(4-(methyl-[(3)H])piperidin-1-yl-4-[(3)H])-6-(trifluoromethyl)pyridin-3-yl)methyl)-3-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-8-yl)urea ([(3)H]MPOU), that embodies improved absolute affinity for human TRPV1 and improved synthetic accessibility...
September 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28891864/photosensitization-of-trpa1-and-trpv1-by-7-dehydrocholesterol-implications-for-the-smith-lemli-opitz-syndrome
#7
Alexandru Babes, Cosmin I Ciotu, Tal Hoffmann, Tatjana I Kichko, Tudor Selescu, Cristian Neacsu, Susanne K Sauer, Peter W Reeh, Michael J M Fischer
Loss of function mutations in the enzyme 7-dehydrocholesterol reductase are responsible for the Smith-Lemli-Opitz syndrome, in which 7-dehydrocholesterol (7-DHC) levels are markedly increased in the plasma and tissues of patients. This increase in 7-DHC is probably associated with the painful and itchy photosensitivity reported by the large majority of Smith-Lemli-Opitz syndrome patients. In order to identify the molecular targets involved in the activation and photosensitization of primary afferents by 7-DHC we focused on TRPA1 and TRPV1, two ion channels expressed in nociceptive nerve endings and previously shown to respond to ultraviolet and visible light under pathophysiological circumstances...
September 1, 2017: Pain
https://www.readbyqxmd.com/read/28890155/antibiotic-induced-microbiota-perturbation-causes-gut-endocannabinoidome-changes-hippocampal-neuroglial-reorganization-and-depression-in-mice
#8
F Guida, F Turco, M Iannotta, D De Gregorio, I Palumbo, G Sarnelli, A Furiano, F Napolitano, S Boccella, L Luongo, M Mazzitelli, A Usiello, F De Filippis, F A Iannotti, F Piscitelli, D Ercolini, V de Novellis, V Di Marzo, R Cuomo, S Maione
The microbiota-gut-brain axis (MGBA) regulates the reciprocal interaction between chronic inflammatory bowel and psychiatric disorders. This interaction involves multiple pathways that are highly debated. We examined the behavioural, biochemical and electrophysiological alterations, as well as gut microbiota composition in a model of antibiotic-induced experimental dysbiosis. Inflammation of the small intestine was also assessed. Mice were exposed to a mixture of antimicrobials for 2weeks. Afterwards, they received Lactobacillus casei DG (LCDG) or a vehicle for up to 7days via oral gavage...
September 7, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28888821/-11-c-bctc-radiosynthesis-and-in-vivo-binding-to-transient-receptor-potential-vanilloid-subfamily-member-1-trpv1-receptor-in-the-mouse-trigeminal-nerve
#9
Katsushi Kumata, Joji Yui, Yiding Zhang, Yusuke Kurihara, Masanao Ogawa, Wakana Mori, Masayuki Fujinaga, Ming-Rong Zhang
The purpose of this study was to synthesize a new positron emission tomography radiotracer, N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-[(11)C]carboxamide ([(11)C]BCTC, [(11)C]1), and assess its in vivo binding to the transient receptor potential vanilloid subfamily member 1 (TRPV1) receptor in mice. [(11)C]BCTC was synthesized by reacting the hydrochloride of 4-tertiarybutylaniline (2·HCl) with [(11)C]phosgene ([(11)C]COCl2) to give isocyanate [(11)C]4, followed by reaction with 4-(3-chloropyridin-2-yl)tetrahydropyrazine (3)...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28884838/review-article-transient-receptor-potential-channels-as-possible-therapeutic-targets-in-irritable-bowel-syndrome
#10
REVIEW
A B Beckers, Z Z R M Weerts, Z Helyes, A A M Masclee, D Keszthelyi
BACKGROUND: Abdominal pain in irritable bowel syndrome (IBS) remains challenging to treat effectively. Researchers have attempted to elucidate visceral nociceptive processes in order to guide treatment development. Transient receptor potential (TRP) channels have been implied in the generation (TRPV1, TRPV4, TRPA1) and inhibition (TRPM8) of visceral pain signals. Pathological changes in their functioning have been demonstrated in inflammatory conditions, and appear to be present in IBS as well...
September 8, 2017: Alimentary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28882752/mechanosensitive-ion-channels-msics-in-articular-nociceptors-drive%C3%A2-mechanical-allodynia-in-osteoarthritis-oa
#11
B H He, M Christin, S Mouchbahani-Constance, A Davidova, R Sharif-Naeini
OBJECTIVE: Osteoarthritis (OA) is a disabling and highly prevalent condition affecting millions worldwide. Pain is the major complaint of OA patients and is presently inadequately managed. It manifests as mechanical allodynia, a painful response to innocuous stimuli such as joint movement. Allodynia is due in part to the sensitization of articular nociceptors to mechanical stimuli. These nociceptors respond to noxious mechanical stimuli applied to their terminals via the expression of depolarizing high-threshold mechanosensitive ion channels (MSICs) that convert painful mechanical forces into electrical signals...
September 5, 2017: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/28879245/effects-of-high-dose-capsaicin-on-tmd-subjects-a-randomized-clinical-study
#12
B K Campbell, R B Fillingim, S Lee, R Brao, D D Price, J K Neubert
Temporomandibular joint disorder (TMD) is a complex musculoskeletal disorder that presents with pain, limited jaw opening, and abnormal noises in the temporomandibular joint. Despite the significant impact that TMD has in terms of suffering and financial burden, relatively few new treatments have emerged; therefore, development of novel treatments to treat TMD pain remains a high priority. The rationale of this study was to use a double-blind, vehicle-controlled clinical trial to evaluate the effects of a high-concentration (8%) capsaicin cream on TMD...
January 2017: JDR Clinical and Translational Research
https://www.readbyqxmd.com/read/28867580/ethanol-potentiates-heat-response-in-the-carotid-artery-via-trpv1
#13
Seham Mustafa, Hishaam N Ismael
AIM: Ethanol is one of the most widely used recreational drugs in the world. At high concentrations, it can induce carotid artery vasoconstriction. Hyperthermia potentiates its effects resulting in carotid artery vasoconstriction at any concentration. The aim of this study is to investigate the interaction between ethanol and heating and to understand the underlying mechanisms leading to their synergistic effect. MATERIALS AND METHODS: Isometric tension of rabbit carotid artery ring segments suspended in organ baths filled with Krebs solution was recorded...
August 31, 2017: Life Sciences
https://www.readbyqxmd.com/read/28865353/mechanisms-involved-in-facial-heat-hyperalgesia-induced-by-endothelin-1-in-female-rats
#14
Rafael Fernandes de Souza, Luana Lechenakoski de Oliveira, Carina Fernanda Mattedi Nones, Renata Cristiane Dos Reis, Erika Ivanna Araya, Caroline Machado Kopruszinski, Giles Alexander Rae, Juliana Geremias Chichorro
OBJECTIVE: Pronociceptive responses to endothelins in the trigeminal system seem to be mediated by ETA and ETB receptors, which have been shown to be expressed in neurons of the trigeminal ganglion of humans and rats. The present study aimed to evaluate the ability of endothelin-1 (ET-1) to induce facial heat hyperalgesia in female rats, the contribution of ETA and ETB receptors to this response, as well as the mechanisms underlying heat hyperalgesia induced by ET-1. DESIGN: ET-1 (100pmol/50μL) was injected into the upper lip and heat hyperalgesia was evaluated for up to 6h...
August 30, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/28863818/depletion-of-membrane-cholesterol-suppresses-drosophila-transient-receptor-potential-like-trpl-channel-activity
#15
Maximilian Peters, Ben Katz, Shaya Lev, Rachel Zaguri, Rita Gutorov, Baruch Minke
Cholesterol is an essential compound of higher eukaryotic cell membranes and a known modulator of ion channel activity. Changes in phospholipids and cholesterol composition of cell membranes are known to alter the activity of ion channels. However, there is little knowledge on the effects of cholesterol on transient receptor potential (TRP) channels. In this study, we explore the effects of cholesterol depletion on the Drosophila photoreceptor channel TRP-like (TRPL), when expressed in tissue culture cells...
2017: Current Topics in Membranes
https://www.readbyqxmd.com/read/28861768/capsaicin-protects-against-oxidative-insults-and-alleviates-behavioral-deficits-in-rats-with-6-ohda-induced-parkinson-s-disease-via-activation-of-trpv1
#16
ZhenXiang Zhao, JianFeng Wang, LingLing Wang, XiaoMei Yao, YiLin Liu, Ye Li, Si Chen, Tao Yue, XiaoTang Wang, WenFei Yu, YiMing Liu
Increasing evidence suggests that capsaicin may play a role in modulating neuronal function and controlling motor behavior. However, the underlying mechanism is still unclear and the activation of transient receptor potential vanilloid 1 (TRPV1) might be involved in. This study investigated the potential neuroprotective role of capsaicin in a rat model of 6-hydroxydopamine (6-OHDA)-induced Parkinson's disease (PD). Capsaicin was treated intraperitoneally for the 6-OHDA induced PD rats and the locomotor activity and abnormal involuntary movements were found alleviated...
August 31, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28861042/3-iodothyronamine-a-novel-endogenous-modulator-of-transient-receptor-potential-melastatin-8
#17
REVIEW
Noushafarin Khajavi, Stefan Mergler, Heike Biebermann
The decarboxylated and deiodinated thyroid hormone (TH) derivative, 3-iodothyronamine (3-T1AM), is suggested to be involved in energy metabolism and thermoregulation. G protein-coupled receptors (GPCRs) are known as the main targets for 3-T1AM; however, transient receptor potential channels (TRPs) were also recently identified as new targets of 3-T1AM. This article reviews the current knowledge of a putative novel role of 3-T1AM in the modulation of TRPs. Specifically, the TRP melastatin 8 (TRPM8) was identified as a target of 3-T1AM in different cell types including neoplastic cells, whereby 3-T1AM significantly increased cytosolic Ca(2+) through TRPM8 activation...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28856444/mechanisms-of-curcumin-induced-gastroprotection-against-ethanol-induced-gastric-mucosal-lesions
#18
Renata Czekaj, Jolanta Majka, Katarzyna Magierowska, Zbigniew Sliwowski, Marcin Magierowski, Robert Pajdo, Agata Ptak-Belowska, Marcin Surmiak, Slawomir Kwiecien, Tomasz Brzozowski
BACKGROUND: Curcumin, a pleiotropic substance used for centuries in traditional medicine, exhibits antioxidant, anti-inflammatory and antiproliferative efficacy against various tumours, but the role of curcumin in gastroprotection is little studied. We determined the effect of curcumin against gastric haemorrhagic lesions induced by 75% ethanol and alterations in gastric blood flow (GBF) in rats with cyclooxygenase-1 (COX-1) and COX-2 activity inhibited by indomethacin, SC-560 or rofecoxib, inhibited NO-synthase activity, capsaicin denervation and blockade of TRPV1 receptors by capsazepine...
August 30, 2017: Journal of Gastroenterology
https://www.readbyqxmd.com/read/28854971/sini-san-improves-duodenal-tight-junction-integrity-in-a-rat-model-of-functional-dyspepsia
#19
Xiongfei Chang, Luqing Zhao, Jiajia Wang, Xiaofang Lu, Shengsheng Zhang
BACKGROUND: Recent reports have demonstrated that impaired barrier function and local microinflammation in the duodenal mucosa contribute to the pathogeneses of functional dyspepsia (FD). Thus, restoring normal barrier integrity becomes a potential therapeutic strategy in the treatment of FD. Sini-San (SNS) is a traditional Chinese prescription that exhibits therapeutic effects in FD, but the underlying mechanisms remain not well understood. METHODS: FD rats were established by tail clamping method and the therapeutic effect of SNS was evaluated by measuring the visceral sensitivity and gastric compliance...
August 30, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28852163/expression-and-purification-of-the-pain-receptor-trpv1-for-spectroscopic-analysis
#20
Phanindra Velisetty, Richard A Stein, Francisco J Sierra-Valdez, Valeria Vásquez, Julio F Cordero-Morales
The transient receptor potential vanilloid 1 (TRPV1) channel is an essential component of the cellular mechanism through which noxious stimuli evoke pain. Functional and structural characterizations of TRPV1 shed light on vanilloid activation, yet the mechanisms for temperature and proton gating remain largely unknown. Spectroscopic approaches are needed to understand the mechanisms by which TRPV1 translates diverse stimuli into channel opening. Here, we have engineered a minimal cysteine-less rat TRPV1 construct (eTRPV1) that can be stably purified and reconstituted for spectroscopic studies...
August 29, 2017: Scientific Reports
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