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transient receptor vanilloid 1

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https://www.readbyqxmd.com/read/28542001/acetaminophen-metabolite-n-acylphenolamine-induces-analgesia-via-transient-receptor-potential-vanilloid-1-receptors-expressed-on-the-primary-afferent-terminals-of-c-fibers-in-the-spinal-dorsal-horn
#1
Nobuko Ohashi, Daisuke Uta, Mika Sasaki, Masayuki Ohashi, Yoshinori Kamiya, Tatsuro Kohno
BACKGROUND: The widely used analgesic acetaminophen is metabolized to N-acylphenolamine, which induces analgesia by acting directly on transient receptor potential vanilloid 1 or cannabinoid 1 receptors in the brain. Although these receptors are also abundant in the spinal cord, no previous studies have reported analgesic effects of acetaminophen or N-acylphenolamine mediated by the spinal cord dorsal horn. We hypothesized that clinical doses of acetaminophen induce analgesia via these spinal mechanisms...
May 25, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28539997/interaction-between-the-cannabinoid-and-vanilloid-systems-on-anxiety-in-male-rats
#2
Nafiseh Faraji, Alireza Komaki, Iraj Salehi
INTRODUCTION: Previous studies have shown that the cannabinoid system is involved in anxiety. In addition, transient receptor potential vanilloid type-1 (TRPV1) channels are new targets for the development of anxiolytics. The present study investigated the possible interaction between the cannabinoid and vanilloid systems on anxiety-like behavior in rats. METHODS: Four different groups of male Wistar rats received intraperitoneal (IP) injections of (1) vehicle (DMSO+saline), (2) cannabinoid receptor agonist WIN55212-2 (WIN) (1 mg/kg), (3) TRPV1 receptor antagonist capsazepine (CPZ) (5 mg/kg), or (4) combined WIN (1 mg/kg) and CPZ (5 mg/kg) treatment 30 minutes before testing in the elevated plus maze...
March 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28534850/exploration-of-the-esophageal-mucosal-barrier-in-non-erosive-reflux-disease
#3
Nicolaas F Rinsma, Ricard Farré, Fred J Troost, Montserrat Elizalde, Daniel Keszthelyi, Zsuzsanna Helyes, Ad A Masclee, José M Conchillo
In the absence of visible mucosal damage, it is hypothesized that the esophageal mucosal barrier is functionally impaired in patients with non-erosive reflux disease (NERD). The aim of the present study was to perform an exploratory analysis of the mucosal barrier in NERD compared to erosive esophagitis (EE) and controls. A second aim was to explore TRPV1 gene transcription in relation to the mucosal barrier function and heartburn symptoms. In this prospective study, 10 NERD patients, 11 patients with active erosive esophagitis and 10 healthy volunteers were included...
May 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28532013/exercise-enhance-the-ectopic-bone-formation-of-calcium-phosphate-biomaterials-in-muscles-of-mice
#4
Lijia Cheng, Shuo Yan, Jiang Zhu, Peiling Cai, Ting Wang, Zheng Shi
OBJECTIVE: To investigate whether exercise can enhance ectopic bone formation of calcium phosphate (Ca-P) biomaterials in muscles of mice. METHODS: Firstly, ten transient receptor potential vanilloid subfamily member 1 (TRPV1) knockout mice (group KO) and ten C57BL/6 mice (group WT) were randomly chosen, 10μg Ca-P biomaterials were implanted into the thigh muscle pouch of each mouse which was far away from femur; after that, all animals were kept in open field for free exploration 5min, and the movement time and distance were automatically analyzed...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28528668/trpv1-channels-in-immune-cells-and-hematological-malignancies
#5
Sofia A Omari, Murray J Adams, Dominic P Geraghty
Transient receptor potential vanilloid-1 (TRPV1) is a member of the TRP family of channels that are responsible for nociceptive, thermal, and mechanical sensations. Originally associated exclusively with sensory neurons, TRPV1 is now known to be present in almost all organs, including cells of the immune system, where TRPV1 has been shown to play a pivotal role in inflammation and immunity. Monocytes, macrophages, and dendritic cells express TRPV1, with both mouse and human studies suggesting that TRPV1 activation protects against endotoxin-induced inflammation...
2017: Advances in Pharmacology
https://www.readbyqxmd.com/read/28527062/the-prokineticin-system-an-interface-between-neural-inflammation-and-pain
#6
Silvia Franchi, Paola Sacerdote, Alberto Panerai
Prokineticins (PK) 1 and 2 belong to a new family of chemokines capable to interact with two different G coupled receptors: Prokineticin receptor (PKR)1 and 2. Both prokineticins and their receptors are widely distributed in different tissues and regulate several biological functions. In particular, a role of the PK system in inflammation and nociception has been established. PKRs are expressed in regions of the nervous system associated with pain and in primary sensitive neurons they colocalize with transient potential receptor vanilloid-TRPV1 providing an anatomical interaction in nociceptor sensitization...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28523109/discovery-of-gsk2193874-an-orally-active-potent-and-selective-blocker-of-transient-receptor-potential-vanilloid-4
#7
Mui Cheung, Weike Bao, David J Behm, Carl A Brooks, Michael J Bury, Sarah E Dowdell, Hilary S Eidam, Ryan M Fox, Krista B Goodman, Dennis A Holt, Dennis Lee, Theresa J Roethke, Robert N Willette, Xiaoping Xu, Guosen Ye, Kevin S Thorneloe
Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barrier. Increased pulmonary vascular pressure evokes TRPV4-dependent pulmonary edema, and therefore, inhibition of TRPV4 represents a novel approach for the treatment of pulmonary edema associated with conditions such as congestive heart failure. Herein we report the discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4'-bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28522805/nitric-oxide-donor-protects-against-acetic-acid-induced-gastric-ulcer-in-rats-via-s-nitrosylation-of-trpv1-on-vagus-nerve
#8
Ting Han, Yan Tang, Jing Li, Bing Xue, Liping Gong, Jingxin Li, Xiao Yu, Chuanyong Liu
This study was conducted to investigate the effects of nitric oxide (NO) in acetic acid-induced gastric ulcer of rats and the underlying mechanisms. We found that peritoneal injection of sodium nitroprusside (SNP), a NO donor, decreased the ulcer area, inflammatory cell infiltration and MPO degree in acetic acid-induced gastric ulcer in rats. This effect was abolished by a transient receptor potential vanilloid 1 (TRPV1) antagonist or prior subdiaphragmatic vagotomy. SNP increased the jejunal mesenteric afferent discharge in a dose-depended manner, which was largely diminished by pretreatment of S-nitrosylation blocker N-ethylmaleimide, TRPV1 antagonist capsazepine, genetic deletion of TRPV1, or vagotomy...
May 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28522561/immediate-and-delayed-potentiating-effects-of-tumor-necrosis-factor-alpha-on-trpv1-sensitivity-of-rat-vagal-pulmonary-sensory-neurons
#9
Chun-Chun Hsu, You Shuei Lin, Ruei-Lung Lin, Lu-Yuan Lee
We studied acute effects of tumor necrosis factor-alpha (TNFα) on the sensitivity of isolated rat vagal pulmonary sensory neurons. Our results showed: 1) A brief pretreatment with a low dose of TNFα (1.44 nM, 9 min) enhanced the sensitivity of transient receptor potential vanilloid type 1 (TRPV1) receptors in these neurons in two distinct phases: the inward current evoked by capsaicin was amplified (∆=247%) immediately following the TNFα pretreatment, which gradually declined toward control and then increased again reaching another peak (∆=384%) after 60-90 min...
May 18, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28516219/decreased-sensory-nerve-excitation-and-bone-pain-associated-with-mouse-lewis-lung-cancer-in-trpv1-deficient-mice
#10
Hiroki Wakabayashi, Satoshi Wakisaka, Toru Hiraga, Kenji Hata, Riko Nishimura, Makoto Tominaga, Toshiyuki Yoneda
Bone pain is one of the most common and life-limiting complications of cancer metastasis to bone. Although the mechanism of bone pain still remains poorly understood, bone pain is evoked as a consequence of sensitization and excitation of sensory nerves (SNs) innervating bone by noxious stimuli produced in the microenvironment of bone metastases. We showed that bone is innervated by calcitonin gene-related protein (CGRP)(+) SNs extending from dorsal root ganglia (DRG), the cell body of SNs, in mice. Mice intratibially injected with Lewis lung cancer (LLC) cells showed progressive bone pain evaluated by mechanical allodynia and flinching with increased CGRP(+) SNs in bone and augmented SN excitation in DRG as indicated by elevated numbers of pERK- and pCREB-immunoreactive neurons...
May 17, 2017: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/28515697/trpa1-channels-modify-trpv1-mediated-current-responses-in-dorsal-root-ganglion-neurons
#11
Takayoshi Masuoka, Makiko Kudo, Yuka Yamashita, Junko Yoshida, Noriko Imaizumi, Ikunobu Muramatsu, Matomo Nishio, Takaharu Ishibashi
The transient receptor potential vanilloid 1 (TRPV1) channel is highly expressed in a subset of sensory neurons in the dorsal root ganglia (DRG) and trigeminal ganglia of experimental animals, responsible for nociception. Many researches have revealed that some TRPV1-positive neurons co-express the transient receptor potential ankyrin 1 (TRPA1) channel whose activities are closely modulated by TRPV1 channel. However, it is less investigated whether the activities of TRPV1 channel are modulated by the presence of TRPA1 channel in primary sensory neurons...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28494183/resolution-of-cannabis-hyperemesis-syndrome-with-topical-capsaicin-in-the-emergency-department-a-case-series
#12
Laurel Dezieck, Zachary Hafez, Albert Conicella, Eike Blohm, Mark J O'Connor, Evan S Schwarz, Michael E Mullins
BACKGROUND: Cannabinoid hyperemesis syndrome (CHS) is characterized by symptoms of cyclic abdominal pain, nausea, and vomiting in the setting of prolonged cannabis use. The transient receptor potential vanilloid 1 (TRPV1) receptor may be involved in this syndrome. Topical capsaicin is a proposed treatment for CHS; it binds TRPV1 with high specificity, impairing substance P signaling in the area postrema and nucleus tractus solitarius via overstimulation of TRPV1. This may explain its apparent antiemetic effect in this syndrome...
May 11, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28484490/intraluminal-administration-of-resiniferatoxin-protects-against-clostridium-difficile-toxin-a-induced-colitis
#13
Steven R Vigna
Clostridium difficile toxin A is a colonic inflammatory agent that acts partially by activation of TRPV1 (transient receptor potential vanilloid type 1). Resiniferatoxin (RTX) is an excitotoxin that activates TRPV1 at low concentrations and defunctionalizes TRPV1 at high concentrations. RTX at various doses was injected intraluminally into isolated ileal segments in anesthetized rats. After 3 hours, the treated segments were removed and inflammation was assessed. This acute treatment with RTX resulted in biphasic responses: (1) an increase in inflammation similar to that caused by toxin A and capsaicin at low doses of up to 100 ng RTX and (2) no inflammatory effect of RTX at higher doses (1-100 μg), consistent with a defunctionalizing or neurotoxic effect of RTX at high doses...
2017: Gastroenterology Research and Practice
https://www.readbyqxmd.com/read/28481959/trpv2-knockout-mice-demonstrate-an-improved-cardiac-performance-following-myocardial-infarction-due-to-attenuated-activity-of-peri-infarct-macrophages
#14
Michal Entin-Meer, Lena Cohen, Einat Hertzberg-Bigelman, Ran Levy, Jeremy Ben-Shoshan, Gad Keren
BACKGROUND: We have recently shown that the expression of the transient receptor potential vanilloid 2 channel, TRPV2, is upregulated in the peri-infarct zone 3-5 days following an acute myocardial infarction (AMI). Further analysis has demonstrated that invading monocytes maturing to macrophages merely harbor the documented elevated expression of this channel. PURPOSE: Assess cardiac function in TRPV2-KO mice compared to TRPV2-WT following AMI and analyze the potential involvement of TRPV2-expressing macrophages in the recovery process...
2017: PloS One
https://www.readbyqxmd.com/read/28479852/a-first-in-human-double-blind-placebo-controlled-randomized-dose-escalation-study-of-dwp05195-a-novel-trpv1-antagonist-in-healthy-volunteers
#15
Jieon Lee, Bo-Hyung Kim, Kyung-Sang Yu, Hee Sun Kim, Ji Duck Kim, Joo-Youn Cho, SeungHwan Lee, Namyi Gu
OBJECTIVES: DWP05195 is a transient receptor potential vanilloid 1 (TRPV1) antagonist developed for managing pain. The purpose of this study was to evaluate the pharmacodynamics pharmacokinetics, safety, and tolerability of DWP05195 in healthy subjects. This was a first-in-human randomized, double-blinded, placebo-controlled, dose escalation study. SUBJECTS AND METHODS: DWP05195 or placebo was administered as a single dose of 10-600 mg in the single-dose study and as 100-400 mg once daily for 8 days in the multiple-dose studies...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28479722/influence-of-capsaicin-on-inflammatory-cytokines-induced-by-lipopolysaccharide-in-myoblast-cells-under-in-vitro-environment
#16
Ke Shang, Touseef Amna, Musarat Amina, Nawal M Al-Musayeib, Salem S Al-Deyab, Inho Hwang
BACKGROUND: ellular damage initiated by reactive oxygen species (ROS) is the main cause of numerous severe diseases and therefore for this reason, the natural antioxidants have note worthy significance in human health. Capsaicin possesses noteworthy analgesic and anti-inflammatory properties. It also possesses healing effects for treatment of arthritis, diabetic neuropathy, gastric lesions, and cardiac excitability that is why it is incorporated in creams and gels. OBJECTIVE: The present study was carried out to estimate the in vitro antioxidant and ROS scavenging activities of capsaicin against muscle precursor cells...
January 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28478727/local-upregulation-of-transient-receptor-potential-ankyrin-1-and-transient-receptor-potential-vanilloid-1-ion-channels-in-rectosigmoid-deep-infiltrating-endometriosis
#17
Noémi Bohonyi, Krisztina Pohóczky, Bálint Szalontai, Anikó Perkecz, Krisztina Kovács, Béla Kajtár, Lajos Orbán, Tamás Varga, Sarolta Szegedi, József Bódis, Zsuzsanna Helyes, Miklós Koppán
Transient Receptor Potential Vanilloid 1 (TRPV1) and Transient Receptor Potential Ankyrin 1 (TRPA1) expressed mainly by primary sensory neurons function as major nociceptive integrators. They are also present on the rat endometrium in an oestrogen-regulated manner. TRPV1 is upregulated in peritoneal and ovarian endometriosis patients, but there is no information about TRPA1 and their pathophysiological significances. In this study, patients undergoing laparoscopic surgery were investigated: severe dysmenorrhoea due to rectosigmoid deep infiltrating endometriosis ( n = 15), uterine fibroid-induced moderate dysmenorrhoea ( n = 7) and tubal infertility with no pain ( n = 6)...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28467971/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#18
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...
April 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28466657/a-review-on-potential-involvement-of-trpv1-channels-in-ischemia-reperfusion-injury
#19
Puneet Kaur Randhawa, Amteshwar Singh Jaggi
Besides functioning as thermosensors, transient receptor potential vanilloid 1 (TRPV1) channels play a pivotal role in ischemia-reperfusion injury. Transient receptor potential vanilloid 1 channel activation attenuates ischemia-reperfusion-induced injury in various organs including the heart, lungs, kidneys, and the brain. Transient receptor potential vanilloid 1 channels are expressed on the sensory neurons innervating the myocardium, ventricles of the heart, epicardial surface of the heart, endothelial cells, and the vascular smooth muscle cells...
January 1, 2017: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28459715/biphasic-renal-sympathetic-response-to-hemorrhagic-hypotension-in-mice
#20
Tao Zhang, Mamoru Tanida, Kunitoshi Uchida, Yoshiro Suzuki, Wei Yang, Yuhichi Kuda, Yasutaka Kurata, Makoto Tominaga, Toshishige Shibamoto
AIM: The inhibitory responses of renal sympathetic nerve activity (RSNA) and heart rate (HR) to sustained hemorrhagic shock occurred in anesthetized rats, but have not yet been determined in mice. Here, we investigated the responses of RSNA and HR to hemorrhagic hypotension in anesthetized mice, with an emphasis on the molecule-based mechanism for roles of afferent vagal nerves. METHODS: RSNA, HR, and mean systemic arterial pressure (MAP) were continuously measured in male pentobarbital-anesthetized C57BL/6N mice...
April 28, 2017: Shock
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