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transient receptor vanilloid 1

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https://www.readbyqxmd.com/read/28104916/trpv1-activation-counters-diet-induced-obesity-through-sirtuin-1-activation-and-prdm-16-deacetylation-in-brown-adipose-tissue
#1
P Baskaran, V Krishnan, K Fettel, P Gao, Z Zhu, J Ren, B Thyagarajan
BACKGROUND/OBJECTIVE: An imbalance between energy intake and expenditure leads to obesity. Increasing metabolism and thermogenesis in brown adipose tissue (BAT) can help in overcoming obesity. Here, we investigated the effect of activation of transient receptor potential vanilloid subfamily 1 (TRPV1) in the upregulation of thermogenic proteins in BAT to counter diet-induced obesity. SUBJECTS/METHODS: We investigated the effect of dietary supplementation of capsaicin (TRPV1 agonist) on the expression of metabolically important thermogenic proteins in BAT of wild type and TRPV1(-/-) mice that received either a normal chow or high fat (±capsaicin; TRPV1 activator) diet by immunoblotting...
January 20, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28103434/analgesic-effect-of-quetiapine-in-a-mouse-model-of-cancer-induced-bone-pain
#2
Mi Hwa Heo, Jin Young Kim, Ilseon Hwang, Eunyoung Ha, Keon Uk Park
Background/Aims: Cancer-induced bone pain (CIBP) is one of the most common pains in patients with advanced neoplasms. Because of treatment-associated side effects, more than half of cancer patients are reported to have inadequate and undermanaged pain control. New mechanism-based therapies must be developed to reduce cancer pain. Quetiapine is a commonly used atypical antipsychotic drug. We report a study of the potential analgesic effects of quetiapine in a mouse model of CIBP and examine the mechanism of bone pain by analyzing the expression of various nociceptors...
January 20, 2017: Korean Journal of Internal Medicine
https://www.readbyqxmd.com/read/28102026/piperine-a-pungent-alkaloid-from-black-pepper-inhibits-b-lymphocyte-activation-and-effector-functions
#3
David A Soutar, Carolyn D Doucette, Robert S Liwski, David W Hoskin
Piperine has several well-documented anti-inflammatory properties; however, little is known regarding its effect on humoral immunity. In this study, we describe the immunosuppressive effect of piperine on B lymphocytes, which are integral to the humoral immune response. Mouse B cells were cultured in the absence or presence of non-cytotoxic concentrations (25, 50, and 100 μM) of piperine during T-dependent or T-independent stimulation. Piperine inhibited B cell proliferation by causing G0/G1 phase cell cycle arrest in association with reduced expression of cyclin D2 and D3...
January 19, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28100643/fluid-shear-stress-increases-transepithelial-transport-of-ca2-in-ciliated-distal-convoluted-and-connecting-tubule-cells
#4
Sami G Mohammed, Francisco J Arjona, Femke Latta, René J M Bindels, Ronald Roepman, Joost G J Hoenderop
In kidney, transcellular transport of Ca(2+) is mediated by transient receptor potential vanilloid 5 and Na(+)-Ca(2+) exchanger 1 proteins in distal convoluted and connecting tubules (DCT and CNT, respectively). It is not yet understood how DCT/CNT cells can adapt to differences in tubular flow rate and, consequently, Ca(2+) load. This study aims to elucidate the molecular mechanisms by which DCT/CNT cells sense fluid dynamics to control transepithelial Ca(2+) reabsorption and whether their primary cilia play an active role in this process...
January 18, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28097492/activation-of-trpm2-and-trpv1-channels-in-dorsal-root-ganglion-by-nadph-oxidase-and-protein-kinase-c-molecular-pathways-a-patch-clamp-study
#5
Mustafa Nazıroğlu
Despite considerable research, the mechanisms of neuropathic pain induced by excessive oxidative stress production and overload calcium ion (Ca(2+)) entry in dorsal root ganglion (DRG) remain substantially unidentified. The transient receptor potential melastatin 2 (TRPM2) and vanilloid 1 (TRPV1) channels are activated with different stimuli including oxidative stress. TRPM2 and TRPV1 have been shown to be involved in induction of neuropathic pain. However, the activation mechanisms of TRPM2 and TRPV1 via NADPH oxidase and protein kinase C (PKC) pathways are poorly understood...
January 17, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28095752/isolation-and-identification-of-a-humantrpv1-activating-compound-from-soy-sauce
#6
Mayu Oshida, Yasunori Matsuura, Shinnosuke Hotta, Jun Watanabe, Yoshinobu Mogi, Tatsuo Watanabe
Transient receptor potential vanilloid 1 (TRPV1) was identified as a receptor of capsaicin, which is a pungent ingredient in hot red peppers. Due to its relevance for nociception, a physiological and pharmacological study of TRPV1 has also been developed. Therefore, it is important to enrich scientific knowledge regarding the TRPV1 activating or inhibiting compounds. In this study, we fractionated soy sauce based on the human TRPV1 (hTRPV1) activity using column chromatography and purified 5-(9H-pyrido[3,4-b]indol-1-yl)-2-furanmethanol (perlolyrine) as an hTRPV1-activating compound...
January 18, 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28094445/presynaptic-inhibition-of-transient-receptor-potential-vanilloid-type-1-trpv1-receptors-by-norepinephrine-in-nociceptive-neurons
#7
Saikat Chakraborty, Vincent Elvezio, Martin Kaczocha, Mario Rebecchi, Michelino Puopolo
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a well-known contributor to nociceptor excitability. To address whether norepinephrine can down-regulate TRPV1 channel activity in nociceptors and reduce their synaptic transmission, the effects of norepinephrine and clonidine were tested on the capsaicin-activated current recorded from acutely dissociated small diameter (<27 μm) dorsal root ganglia (DRG) neurons and on miniature excitatory postsynaptic currents (mEPSCs) recorded from large lamina I neurons in horizontal spinal cord slices...
January 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28092830/trpv1-antagonism-by-piperazinyl-aryl-compounds-a-topomer-comfa-study-and-its-use-in-virtual-screening-for-identification-of-novel-antagonists
#8
Rajendra Kristam, Shashidhar N Rao, Anne Sudha D'Cruz, Vijayalakshmi Mahadevan, Vellarkad N Viswanadhan
Transient Receptor Potential Vanilloid, member 1 (TRPV1), is a non-selective cation channel belonging to the transient receptor potential (TRP) family of ion channels. It occurs in the peripheral and central nervous system, activated by a variety of exogenous and endogenous stimuli, thus playing a key role in transmission of pain. This has been a target for chronic pain since more than a decade and a number of antagonists that progressed into clinical trials have failed due to the unexpected side effect of core body temperature rise, thus halting progress in this field...
January 7, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28088386/trypsin-induces-biphasic-muscle-contraction-and-relaxation-via-transient-receptor-potential-vanilloid-1-and-neurokinin-receptors-1-2-in-porcine-esophageal-body
#9
Bai Xiaopeng, Yoshimasa Tanaka, Eikichi Ihara, Katsuya Hirano, Kayoko Nakano, Mayumi Hirano, Yoshinao Oda, Kazuhiko Nakamura
Duodenal reflux of fluids containing trypsin relates to refractory gastroesophageal reflux disease (GERD). Esophageal peristalsis and clearance are important factors in GERD pathogenesis. However, the function of trypsin in esophageal body contractility is not fully understood. In this study, effects of trypsin on circular smooth muscle (CSM) and longitudinal smooth muscle (LSM) of the porcine esophageal body were examined. Trypsin elicited a concentration dependent biphasic response, a major contraction and a subsequent relaxation only in CSM...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28073835/mechanosensitive-transient-receptor-potential-vanilloid-4-regulates-dermatophagoides-farinae-induced-airway-remodeling-via-2-distinct-pathways-modulating-matrix-synthesis-and-degradation
#10
Farai Gombedza, Vinay Kondeti, Nosayba Al-Azzam, Stephanie Koppes, Ernest Duah, Prachi Patil, Madison Hexter, Daniel Phillips, Charles K Thodeti, Sailaja Paruchuri
Contributions of mechanical signals to airway remodeling during asthma are poorly understood. Transient receptor potential vanilloid 4 (TRPV4), a mechanosensitive ion channel, has been implicated in cardiac and pulmonary fibrosis; however, its role in asthma remains elusive. Employing a Dermatophagoides farinae-induced asthma model, we report here that TRPV4 knockout mice were protected from D. farinae-induced airway remodeling. Furthermore, lung fibroblasts that were isolated from TRPV4 knockout mice showed diminished differentiation potential compared with wild-type mice...
January 10, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28062485/activation-of-bitter-taste-receptors-in-pulmonary-nociceptors-sensitizes-trpv1-channels-through-plc-and-pkc-signaling-pathway
#11
Qihai Gu, Deanna S Joe, Carolyn A Gilbert
Bitter taste receptors (T2Rs), a G-protein-coupled receptor family capable of detecting numerous bitter-tasting compounds, have recently been shown to be expressed and play diverse roles in many extraoral tissues. Here we report the functional expression of T2Rs in rat pulmonary sensory neurons. In anesthetized spontaneously breathing rats, intratracheal instillation of T2Rs agonist chloroquine (10 mM, 0.1 ml) significantly augmented chemoreflexes evoked by right-atrial injection of capsaicin, a specific activator for transient receptor potential vanilloid receptor 1 (TRPV1); whereas intravenous infusion of chloroquine failed to significantly affect capsaicin-evoked reflexes...
January 6, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28059868/a-novel-inhibitor-of-active-protein-kinase-g-attenuates-chronic-inflammatory-and-osteoarthritic-pain
#12
Ying-Ju Sung, Nelson Sofoluke, Mary Nkamany, Shixian Deng, Yuli Xie, Jeremy Greenwood, Ramy Farid, Donald W Landry, Richard T Ambron
Activating Protein kinase-1α (PKG-1α) induces a long-term hyperexcitability (LTH) in nociceptive neurons. Since the LTH correlates directly with chronic pain in many animal models we tested the hypothesis that inhibiting PKG-1α would attenuate LTH-mediated pain. We first synthesized and characterized compound N46 (propoxybenzoyl)benzamidopyrrolidin-3-yl)-1H-indazole-5-carboxamide). N46 inhibits PKG-1α with an IC50 of 7.5nmol, was highly selective when tested against a panel of 274 kinases, and tissue distribution studies indicate that it does not enter the CNS...
December 30, 2016: Pain
https://www.readbyqxmd.com/read/28044278/understand-spiciness-mechanism-of-trpv1-channel-activation-by-capsaicin
#13
REVIEW
Fan Yang, Jie Zheng
Capsaicin in chili peppers bestows the sensation of spiciness. Since the discovery of its receptor, transient receptor potential vanilloid 1 (TRPV1) ion channel, how capsaicin activates this channel has been under extensive investigation using a variety of experimental techniques including mutagenesis, patch-clamp recording, crystallography, cryo-electron microscopy, computational docking and molecular dynamic simulation. A framework of how capsaicin binds and activates TRPV1 has started to merge: capsaicin binds to a pocket formed by the channel's transmembrane segments, where it takes a "tail-up, head-down" configuration...
January 2, 2017: Protein & Cell
https://www.readbyqxmd.com/read/28030558/loss-of-trpv4-function-suppresses-inflammatory-fibrosis-induced-by-alkali-burning-mouse-corneas
#14
Yuka Okada, Kumi Shirai, Masayasu Miyajima, Peter S Reinach, Osamu Yamanaka, Takayoshi Sumioka, Masahide Kokado, Katsuo Tomoyose, Shizuya Saika
In humans suffering from pulmonary disease and a mouse model, transient receptor potential vanilloid 4 (TRPV4) channel activation contributes to fibrosis. As a corneal alkali burn induces the same response, we determined if such an effect is also attributable to TRPV4 activation in mice. Accordingly, we determined if the alkali burn wound healing responses in wild-type (WT) mice are different than those in their TRPV4-null (KO) counterpart. Stromal opacification due to fibrosis in KO (n = 128) mice was markedly reduced after 20 days relative to that in WT (n = 157) mice...
2016: PloS One
https://www.readbyqxmd.com/read/28028935/renoprotection-focus-on-trpv1-trpv4-trpc6-and-trpm2
#15
REVIEW
L Markó, M Mannaa, T N Haschler, S Krämer, M Gollasch
Members of the transient receptor potential (TRP) cation channel receptor family have unique sites of regulatory function in the kidney which enables them to promote regional vasodilatation and controlled Ca(2+) influx into podocytes and tubular cells. Activated TRP vanilloid 1 receptor channels (TRPV1) have been found to elicit renoprotection in rodent models of acute kidney injury following ischaemia/reperfusion. Transient receptor potential cation channel, subfamily C, member 6 (TRPC6) in podocytes is involved in chronic proteinuric kidney disease, particularly in focal segmental glomerulosclerosis (FSGS)...
November 7, 2016: Acta Physiologica
https://www.readbyqxmd.com/read/28017670/presynaptic-facilitation-by-tetracaine-of-glutamatergic-spontaneous-excitatory-transmission-in-the-rat-spinal-substantia-gelatinosa-involvement-of-trpa1-channels
#16
Lian-Hua Piao, Tsugumi Fujita, Ting Yu, Eiichi Kumamoto
The amide-type local anesthetic (LA) lidocaine activates transient receptor potential (TRP) ankyrin-1 (TRPA1) channels to facilitate spontaneous L-glutamate release onto spinal substantia gelatinosa (SG) neurons, which play a crucial role in regulating nociceptive transmission. In contrast, the ester-type LA procaine reduces the spontaneous release of L-glutamate in SG neurons. In order to determine whether TRPA1 activation by LAs is specific to amide-types, we examined the actions of tetracaine, another ester-type LA, and other amide-type LAs on glutamatergic spontaneous excitatory transmission in SG neurons by focusing on TRP activation...
December 22, 2016: Brain Research
https://www.readbyqxmd.com/read/27997038/inflammation-of-peripheral-tissues-and-injury-to-peripheral-nerves-induce-diferring-effects-in-the-expression-of-the-calcium-sensitive-anandamide-synthesising-enzyme-and-related-molecules-in-rat-primary-sensory-neurons
#17
João Sousa-Valente, Angelika Varga, Jose Vicente Torres Perez, Agnes Jenes, John Wahba, Ken Mackie, Benjamin Cravatt, Natsuo Ueda, Kazuhito Tsuboi, Peter Santha, Gabor Jancso, Hiren Tailor, António Avelino, Istvan Nagy
Elevation of intracellular Ca(2+) concentration induces the synthesis of N-arachydonoylethanolamine (anandamide) in a sub-population of primary sensory neurons. N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is the only known enzyme, which synthesises anandamide in a Ca(2+) -dependent manner. NAPE-PLD mRNA, as well as anandamide's main targets, the excitatory transient receptor potential vanilloid type 1 ion channel (TRPV1) and the inhibitory cannabinoid type 1 (CB1) receptor and the main anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) are all expressed by sub-populations of nociceptive primary sensory neurons...
December 20, 2016: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/27989582/expression-of-cannabinoid-type-1-receptors-in%C3%A2-human-odontoblast-cells
#18
Kehua Que, Dan He, Ying Jin, Ligeng Wu, Fang Wang, Zhiying Zhao, Jing Yang, Jiayin Deng
INTRODUCTION: The aim of this study was to investigate the functional expression of cannabinoid type 1 (CB1) receptors in human odontoblasts (HODs) and the possible internal mechanism. METHODS: In the present study, we examined the molecular and functional expression of the CB1 receptors in cultured HOD-like cells and native HODs obtained from healthy wisdom teeth. RESULTS: Immunohistochemistry and immunofluorescence revealed that CB1 receptors localize to native HODs and HOD-like cells, respectively...
December 15, 2016: Journal of Endodontics
https://www.readbyqxmd.com/read/27986808/activation-of-transient-receptor-potential-vanilloid-1-by-lipoxygenase-metabolites-depends-on-pkc-phosphorylation
#19
Rakesh Kumar, Adina Hazan, Matan Geron, Rebbeca Steinberg, Lital Livni, Henry Matzner, Avi Priel
Peripheral neuronal activation by inflammatory mediators is a multifaceted physiological response that involves a multitude of regulated cellular functions. One key pathway that has been shown to be involved in inflammatory pain is Gq/GPCR, whose activation by inflammatory mediators is followed by the regulated response of the cation channel transient receptor potential vanilloid 1 (TRPV1). However, the mechanism that underlies TRPV1 activation downstream of the Gq/GPCR pathway has yet to be fully defined. In this study, we employ pharmacological and molecular biology tools to dissect this activation mechanism via perforated-patch recordings and calcium imaging of both neurons and a heterologous system...
December 16, 2016: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/27983679/kunitz-type-peptide-hcrg21-from-the-sea-anemone-heteractis-crispa-is-a-full-antagonist-of-the-trpv1-receptor
#20
Margarita Monastyrnaya, Steve Peigneur, Elena Zelepuga, Oksana Sintsova, Irina Gladkikh, Elena Leychenko, Marina Isaeva, Jan Tytgat, Emma Kozlovskaya
Sea anemone venoms comprise multifarious peptides modulating biological targets such as ion channels or receptors. The sequence of a new Kunitz-type peptide, HCRG21, belonging to the Heteractis crispa RG (HCRG) peptide subfamily was deduced on the basis of the gene sequence obtained from the Heteractis crispa cDNA. HCRG21 shares high structural homology with Kunitz-type peptides APHC1-APHC3 from H. crispa, and clusters with the peptides from so named "analgesic cluster" of the HCGS peptide subfamily but forms a separate branch on the NJ-phylogenetic tree...
December 15, 2016: Marine Drugs
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