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transient receptor vanilloid 1

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https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#1
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
September 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28905239/expression-and-distribution-of-three-transient-receptor-potential-vanilloid-trpv-channel-proteins-in-human-odontoblast-like-cells
#2
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
#3
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/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/28888821/-11-c-bctc-radiosynthesis-and-in-vivo-binding-to-transient-receptor-potential-vanilloid-subfamily-member-1-trpv1-receptor-in-the-mouse-trigeminal-nerve
#7
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/28861768/capsaicin-protects-against-oxidative-insults-and-alleviates-behavioral-deficits-in-rats-with-6-ohda-induced-parkinson-s-disease-via-activation-of-trpv1
#8
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/28861502/cannabinoids-in-parkinson-s-disease
#9
REVIEW
Mario Stampanoni Bassi, Andrea Sancesario, Roberta Morace, Diego Centonze, Ennio Iezzi
The endocannabinoid system plays a regulatory role in a number of physiological processes and has been found altered in different pathological conditions, including movement disorders. The interactions between cannabinoids and dopamine in the basal ganglia are remarkably complex and involve both the modulation of other neurotransmitters (γ-aminobutyric acid, glutamate, opioids, peptides) and the activation of different receptors subtypes (cannabinoid receptor type 1 and 2). In the last years, experimental studies contributed to enrich this scenario reporting interactions between cannabinoids and other receptor systems (transient receptor potential vanilloid type 1 cation channel, adenosine receptors, 5-hydroxytryptamine receptors)...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/28859929/cutaneous-and-renal-vasodilatory-response-to-local-pressure-application-a-comparative-study-in-mice
#10
Anne-Laure Begey, Kiao Ling Liu, Ming Lo, Audrey Josset-Lamaugarny, Nicolas Picard, Catherine Gauthier, Berengere Fromy, Dominique Sigaudo-Roussel, Laurence Dubourg
BACKGROUND AND AIM: We have reported a novel relationship involving mechanical stimulation and vasodilation in rodent and human skin, referred to as pressure-induced vasodilation (PIV). It is unknown whether this mechanism exists in kidney and reflects the microcirculation in deep organs. Therefore, we compared the skin and kidney PIV to determine whether their changes were similar. METHODS: In anesthetized mice fed a normal salt-diet, laser Doppler flux (LDF) signals were measured when an increase in local pressure was applied to the surface of the head skin with the rate of 2...
August 30, 2017: Microvascular Research
https://www.readbyqxmd.com/read/28854971/sini-san-improves-duodenal-tight-junction-integrity-in-a-rat-model-of-functional-dyspepsia
#11
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
#12
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
https://www.readbyqxmd.com/read/28842279/itch-induces-conditioned-place-aversion-in-mice
#13
Di Mu, Yan-Gang Sun
Itch sensation consists of both sensory and emotional components. The molecular and cellular mechanisms underlying the transduction and transmission of itch sensation have been studied extensively in rodents. However, whether itch induces emotional responses in mice still remains unknown. We found that pruritogens induced conditioned place aversion (CPA) in mice, and that the CPA lasted for at least two weeks. Disruption of itch signal transmission by depletion of peripheral sensory fibers expressing TRPV1 (transient receptor potential vanilloid subfamily, member 1) attenuated chloroquine-induced CPA...
August 24, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28831207/intrathecal-resiniferatoxin-modulates-trpv1-in-drg-neurons-and-reduces-tnf-induced-pain-related-behavior
#14
M Leo, M Schulte, L-I Schmitt, M Schäfers, C Kleinschnitz, T Hagenacker
Transient receptor potential vanilloid-1 (TRPV1) is a nonselective cation channel, predominantly expressed in sensory neurons. TRPV1 is known to play an important role in the pathogenesis of inflammatory and neuropathic pain states. Previous studies suggest interactions between tumor necrosis factor- (TNF-) alpha and TRPV1, resulting in a modulation of ion channel function and protein expression in sensory neurons. We examined the effect of intrathecal administration of the ultrapotent TRPV1 agonist resiniferatoxin (RTX) on TNF-induced pain-associated behavior of rats using von Frey and hot plate behavioral testing...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28827659/tdag8-trpv1-and-asic3-involved-in-establishing-hyperalgesic-priming-in-experimental-rheumatoid-arthritis
#15
Wei-Shan Hsieh, Chia-Chi Kung, Shir-Ly Huang, Shih-Chang Lin, Wei-Hsin Sun
Rheumatoid arthritis (RA), characterized by chronic inflammation of synovial joints, is often associated with ongoing pain and increased pain sensitivity. High hydrogen ion concentration (acidosis) found in synovial fluid in RA patients is associated with disease severity. Acidosis signaling acting on proton-sensing receptors may contribute to inflammation and pain. Previous studies focused on the early phase of arthritis (<5 weeks) and used different arthritis models, so elucidating the roles of different proton-sensing receptors in the chronic phase of arthritis is difficult...
August 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28826537/actions-and-regulation-of-ionotropic-cannabinoid-receptors
#16
Luciano De Petrocellis, Massimo Nabissi, Giorgio Santoni, Alessia Ligresti
Almost three decades have passed since the identification of the two specific metabotropic receptors mediating cannabinoid pharmacology. Thereafter, many cannabinoid effects, both at central and peripheral levels, have been well documented and characterized. However, numerous evidences demonstrated that these pharmacological actions could not be attributable solely to the activation of CB1 and CB2 receptors since several important cannabimimetic actions have been found in biological systems lacking CB1 or CB2 gene such as in specific cell lines or transgenic mice...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28815372/do-trpv1-antagonists-increase-the-risk-for-skin-tumourigenesis-a-collaborative-in-vitro-and-in-vivo-assessment
#17
Miyoung Park, Anita A Naidoo, Angie Burns, Jin Kyu Choi, Kelly M Gatfield, Martin Vidgeon-Hart, Il-Hong Bae, Chang Seok Lee, Gyeyoung Choi, Andrew J Powell, Young-Ho Park, Rajni Fagg
A recent hypothesis suggesting that the pharmacological target TRPV1 (transient receptor potential vanilloid subfamily, member 1) may function as a tumour suppressor, which potentially impacts the development of TRPV1 antagonist therapeutics for a range of conditions. However, little is known about the long-term physiologic effects of TRPV1 blockade in the skin. In vitro and in vivo studies suggested that the potent TRPV1 competitive antagonist AMG-9810 promoted proliferation in N/TERT1 cells (telomerase-immortalised primary human keratinocytes 1) and tumour development in mouse skin that was mediated through EGFR/Akt/mTOR signalling...
August 16, 2017: Cell Biology and Toxicology
https://www.readbyqxmd.com/read/28814817/conjugated-polymers-mediate-effective-activation-of-the-mammalian-ion-channel-transient-receptor-potential-vanilloid-1
#18
F Lodola, N Martino, G Tullii, G Lanzani, M R Antognazza
Selective and rapid regulation of ionic channels is pivotal to the understanding of physiological processes and has a crucial impact in developing novel therapeutic strategies. Transient Receptor Potential (TRP) channels are emerging as essential cellular switches that allow animals to respond to their environment. In particular, the Vanilloid Receptor 1 (TRPV1), besides being involved in the body temperature regulation and in the response to pain, has important roles in several neuronal functions, as cytoskeleton dynamics, injured neurons regeneration, synaptic plasticity...
August 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28812431/oral-administration-of-curcumin-attenuates-visceral-hyperalgesia-through-inhibiting-phosphorylation-of-trpv1-in-rat-model-of-ulcerative-colitis
#19
Mei Yang, Juan Wang, Chunxue Yang, Hongxiu Han, Weifang Rong, Guohua Zhang
Background Curcumin has been reported to have anti-inflammatory and anti-nociceptive effects. The present study was designed to explore the potential therapeutic effects of curcumin on visceral hyperalgesia and inflammation in a rat model of ulcerative colitis. We observed the effects of orally administered curcumin on the disease activity index, histological change in colon, colorectal distension-induced abdominal withdrawal reflex, the expression of transient receptor potential vanilloid 1 (TRPV1) and phosphorylated TRPV1 in dextran sulfate sodium-induced colitis rats...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28806222/transient-receptor-potential-vanilloid-1-antagonists-prevent-anesthesia-induced-hypothermia-and-decrease-postincisional-opioid-dose-requirements-in-rodents
#20
Andras Garami, Mohab Ibrahim, Kerry Gilbraith, Rajesh Khanna, Eszter Pakai, Alexandra Miko, Erika Pinter, Andrej A Romanovsky, Frank Porreca, Amol M Patwardhan
BACKGROUND: Intraoperative hypothermia and postoperative pain control are two important clinical challenges in anesthesiology. Transient receptor potential vanilloid 1 has been implicated both in thermoregulation and pain. Transient receptor potential vanilloid 1 antagonists were not advanced as analgesics in humans in part due to a side effect of hyperthermia. This study tested the hypothesis that a single, preincision injection of a transient receptor potential vanilloid 1 antagonist could prevent anesthesia-induced hypothermia and decrease the opioid requirement for postsurgical hypersensitivity...
August 14, 2017: Anesthesiology
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