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TRPV1 receptor agonist

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https://www.readbyqxmd.com/read/29156899/modulating-the-endocannabinoid-pathway-as-treatment-for-peripheral-neuropathic-pain-a-selected-review-of-preclinical-studies
#1
Shannon O'Hearn, Patrick Diaz, Bo Angela Wan, Carlo DeAngelis, Nicholas Lao, Leila Malek, Edward Chow, Alexia Blake
Chemotherapy-induced neuropathic pain is a distressing and commonly occurring side effect of many commonly used chemotherapeutic agents, which in some cases may prevent cancer patients from being able to complete their treatment. Cannabinoid based therapies have the potential to manage or even prevent pain associated with this syndrome. Pre-clinical animal studies that investigate the modulation of the endocannabinoid system (endogenous cannabinoid pathway) are being conducted to better understand the mechanisms behind this phenomenon...
August 31, 2017: Annals of Palliative Medicine
https://www.readbyqxmd.com/read/29134561/cannabinoid-receptor-type-1-agonist-acea-protects-neurons-from-death-and-attenuates-endoplasmic-reticulum-stress-related-apoptotic-pathway-signaling
#2
Talita A Vrechi, Fernanda Crunfli, Andressa P Costa, Andréa S Torrão
Neurodegeneration is the result of progressive destruction of neurons in the central nervous system, with unknown causes and pathological mechanisms not yet fully elucidated. Several factors contribute to neurodegenerative processes, including neuroinflammation, accumulation of neurotoxic factors, and misfolded proteins in the lumen of the endoplasmic reticulum (ER). Endocannabinoid signaling has been pointed out as an important modulatory system in several neurodegeneration-related processes, inhibiting the inflammatory response and increasing neuronal survival...
November 13, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29130364/fluorescent-labeling-and-2-photon-imaging-of-mouse-tooth-pulp-nociceptors
#3
A Kadala, P Sotelo-Hitschfeld, Z Ahmad, P Tripal, B Schmid, A Mueller, L Bernal, Z Winter, S Brauchi, U Lohbauer, K Messlinger, J K Lennerz, K Zimmermann
Retrograde fluorescent labeling of dental primary afferent neurons (DPANs) has been described in rats through crystalline fluorescent DiI, while in the mouse, this technique was achieved with only Fluoro-Gold, a neurotoxic fluorescent dye with membrane penetration characteristics superior to the carbocyanine dyes. We reevaluated this technique in the rat with the aim to transfer it to the mouse because comprehensive physiologic studies require access to the mouse as a model organism. Using conventional immunohistochemistry, we assessed in rats and mice the speed of axonal dye transport from the application site to the trigeminal ganglion, the numbers of stained DPANs, and the fluorescence intensity via 1) conventional crystalline DiI and 2) a novel DiI formulation with improved penetration properties and staining efficiency...
November 1, 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/29129206/differential-cytotoxicity-and-intracellular-calcium-signalling-following-activation-of-the-calcium-permeable-ion-channels-trpv1-and-trpa1
#4
Thomas Stueber, Mirjam J Eberhardt, Yaki Caspi, Shaya Lev, Alexander Binshtok, Andreas Leffler
Several members of the transient receptor channel (TRP) family can mediate a calcium-dependent cytotoxicity. In sensory neurons, vanilloids like capsaicin induce neurotoxicity by activating TRPV1. The closely related ion channel TRPA1 is also activated by irritants, but it is unclear if and how TRPA1 mediates cell death. In the present study we explored cytotoxicity and intracellular calcium signalling resulting from activation of TRPV1 and TRPA1, either heterologously expressed in HEK 293 cells or in native mouse dorsal root ganglion (DRG) neurons...
December 2017: Cell Calcium
https://www.readbyqxmd.com/read/29117570/oxytocin-modulates-nociception-as-an-agonist-of-pain-sensing-trpv1
#5
Yelena Nersesyan, Lusine Demirkhanyan, Deny Cabezas-Bratesco, Victoria Oakes, Ricardo Kusuda, Tyler Dawson, Xiaohui Sun, Chike Cao, Alejandro Martin Cohen, Bharath Chelluboina, Krishna Kumar Veeravalli, Katharina Zimmermann, Carmen Domene, Sebastian Brauchi, Eleonora Zakharian
Oxytocin is a hormone with various actions. Oxytocin-containing parvocellular neurons project to the brainstem and spinal cord. Oxytocin release from these neurons suppresses nociception of inflammatory pain, the molecular mechanism of which remains unclear. Here, we report that the noxious stimulus receptor TRPV1 is an ionotropic oxytocin receptor. Oxytocin elicits TRPV1 activity in native and heterologous expression systems, regardless of the presence of the classical oxytocin receptor. In TRPV1 knockout mice, DRG neurons exhibit reduced oxytocin sensitivity relative to controls, and oxytocin injections significantly attenuate capsaicin-induced nociception in in vivo experiments...
November 7, 2017: Cell Reports
https://www.readbyqxmd.com/read/29102918/non-steroidal-anti-inflammatory-drugs-attenuate-agonist-evoked-activation-of-transient-receptor-potential-channels
#6
M G Tsagareli, I Nozadze, N Tsiklauri, G Gurtskaia
Transient receptor potential (TRP) cation channels are the largest group of sensory detector proteins expressed in the nerve terminals of many receptors including nociceptors, and are activated by temperature and chemicals that elicit hot or cold sensations. Antagonists of these channels are likely promising targets for new analgesic drugs at the peripheral and central levels. Because some non-steroidal anti-inflammatory drugs (NSAIDs) are structural analogs of prostaglandins and NSAIDs attenuate heat nociception and mechanical allodynia in models of inflammatory and neuropathic pain, we investigated whether three widely used NSAIDs (diclofenac, ketorolac, and xefocam) affect thermal and mechanical hyperalgesia following the activation of TRPA1 and TRPV1 channels...
November 2, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29100756/trpv1-alterations-in-urinary-bladder-dysfunction-in-a-rat-model-of-stz-induced-diabetes
#7
Bizhan R Sharopov, Kseniya L Gulak, Igor B Philyppov, Anna V Sotkis, Yaroslav M Shuba
AIMS: More than half of diabetic patients experience voiding disorder termed diabetic urinary bladder dysfunction (DBD). Here we have investigated how the alterations in transient receptor potential vanilloid 1 (TRPV1) ion channel expressed in bladder-innervating afferents may contribute to DBD pathogenesis. MAIN METHODS: The rat model of streptozotocin (STZ)-induced diabetes was used. The functional profile of TRPV1 in retrogradely labeled afferent, bladder-innervating dorsal root ganglia (DRG) neurons was examined using patch clamp...
October 31, 2017: Life Sciences
https://www.readbyqxmd.com/read/29100528/silica-nanoparticles-inhibit-the-cation-channel-trpv4-in-airway-epithelial-cells
#8
Alicia Sanchez, Julio L Alvarez, Kateryna Demydenko, Carole Jung, Yeranddy A Alpizar, Julio Alvarez-Collazo, Stevan M Cokic, Miguel A Valverde, Peter H Hoet, Karel Talavera
BACKGROUND: Silica nanoparticles (SiNPs) have numerous beneficial properties and are extensively used in cosmetics and food industries as anti-caking, densifying and hydrophobic agents. However, the increasing exposure levels experienced by the general population and the ability of SiNPs to penetrate cells and tissues have raised concerns about possible toxic effects of this material. Although SiNPs are known to affect the function of the airway epithelium, the molecular targets of these particles remain largely unknown...
November 3, 2017: Particle and Fibre Toxicology
https://www.readbyqxmd.com/read/29082315/n-arachidonoyl-dopamine-a-novel-endocannabinoid-and-endovanilloid-with-widespread-physiological-and-pharmacological-activities
#9
REVIEW
Urszula Grabiec, Faramarz Dehghani
N-arachidonoyl dopamine (NADA) is a member of the family of endocannabinoids to which several other N-acyldopamines belong as well. Their activity is mediated through various targets that include cannabinoid receptors or transient receptor potential vanilloid (TRPV)1. Synthesis and degradation of NADA are not yet fully understood. Nonetheless, there is evidence that NADA plays an important role in nociception and inflammation in the central and peripheral nervous system. The TRPV1 receptor, for which NADA is a potent agonist, was shown to be an endogenous transducer of noxious heat...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/29065362/pharmacological-augmentation-of-endocannabinoid-signaling-reduces-the-neuroendocrine-response-to-stress
#10
Pablo Nicolás Surkin, Sofia Ludmila Gallino, Valeria Luce, Fernando Correa, Javier Fernandez-Solari, Andrea De Laurentiis
Activation of the hypothalamic-pituitary-adrenal axis (HPA) is critical for survival when the organism is exposed to a stressful stimulus. The endocannabinoid system (ECS) is currently considered an important neuromodulator involved in numerous pathophysiological processes and whose primary function is to maintain homeostasis. In the tissues constituting the HPA axis, all the components of the ECS are present and the activation of this system acts in parallel with changes in the activity of numerous neurotransmitters, including nitric oxide (NO)...
October 18, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/29054683/the-anthelminthic-drug-praziquantel-is-a-selective-agonist-of-the-sensory-transient-receptor-potential-melastatin-type-8-channel
#11
Ramona-Madalina Babes, Tudor Selescu, Dan Domocos, Alexandru Babes
Praziquantel is the most effective anthelminthic drug for the treatment of schistosomiasis, an infectious disease caused by the platyhelminth Schistosoma mansoni. While praziquantel is known to trigger calcium influx into schisostomes, followed by spastic paralysis of the worms and tegumental disruption, the mechanism of action of the drug is not completely understood. Although relatively well tolerated, praziquantel has been reported to cause mild adverse effects, including nausea, abdominal pain and headaches...
October 18, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29046638/blockade-of-cannabinoid-cb1-receptors-in-the-dorsal-periaqueductal-gray-unmasks-the-antinociceptive-effect-of-local-injections-of-anandamide-in-mice
#12
Diego C Mascarenhas, Karina S Gomes, Tatiani Sorregotti, Ricardo L Nunes-de-Souza
Divergent results in pain management account for the growing number of studies aiming at elucidating the pharmacology of the endocannabinoid/endovanilloid anandamide (AEA) within several pain-related brain structures. For instance, the stimulation of both Transient Receptor Potential Vanilloid type 1 (TRPV1) and Cannabinoid type 1 (CB1) receptors led to paradoxical effects on nociception. Here, we attempted to propose a clear and reproducible methodology to achieve the antinociceptive effect of exogenous AEA within the dorsal periaqueductal gray (dPAG) of mice exposed to the tail-flick test...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29035821/neuronal-nitric-oxide-synthase-is-involved-in-cb-trpv1-signalling-focus-on-control-of-hippocampal-hyperexcitability
#13
Fabio Carletti, Giuditta Gambino, Valerio Rizzo, Giuseppe Ferraro, Pierangelo Sardo
Cannabinoids (CB), transient receptors potential vanilloid type 1 (TRPV1) and nitric oxide (NO) were found to be interlinked in regulating some neuronal functions such as membrane excitability and synaptic transmission. TRPV1 play a fundamental role since it represents a synaptic target for CB that triggers several downstream cellular pathways. In this regard, recent evidence report that TRPV1 could influence NO production by modulating neuronal NO synthase (nNOS) activity. In the present research, we pointed to manipulate nNOS function to assess its role on TRPV1 signalling in hyperexcitability conditions elicited in the dentate gyrus of hippocampal formation...
October 3, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/29019983/human-trpml1-channel-structures-in-open-and-closed-conformations
#14
Philip Schmiege, Michael Fine, Günter Blobel, Xiaochun Li
Transient receptor potential mucolipin 1 (TRPML1) is a Ca(2+)-releasing cation channel that mediates the calcium signalling and homeostasis of lysosomes. Mutations in TRPML1 lead to mucolipidosis type IV, a severe lysosomal storage disorder. Here we report two electron cryo-microscopy structures of full-length human TRPML1: a 3.72-Å apo structure at pH 7.0 in the closed state, and a 3.49-Å agonist-bound structure at pH 6.0 in an open state. Several aromatic and hydrophobic residues in pore helix 1, helices S5 and S6, and helix S6 of a neighbouring subunit, form a hydrophobic cavity to house the agonist, suggesting a distinct agonist-binding site from that found in TRPV1, a TRP channel from a different subfamily...
October 11, 2017: Nature
https://www.readbyqxmd.com/read/29018170/temperature-activated-ion-channels-in-neural-crest-cells-confer-maternal-fever-associated-birth-defects
#15
Mary R Hutson, Anna L Keyte, Miriam Hernández-Morales, Eric Gibbs, Zachary A Kupchinsky, Ioannis Argyridis, Kyle N Erwin, Kelly Pegram, Margaret Kneifel, Paul B Rosenberg, Pavle Matak, Luke Xie, Jörg Grandl, Erica E Davis, Nicholas Katsanis, Chunlei Liu, Eric J Benner
Birth defects of the heart and face are common, and most have no known genetic cause, suggesting a role for environmental factors. Maternal fever during the first trimester is an environmental risk factor linked to these defects. Neural crest cells are precursor populations essential to the development of both at-risk tissues. We report that two heat-activated transient receptor potential (TRP) ion channels, TRPV1 and TRPV4, were present in neural crest cells during critical windows of heart and face development...
October 10, 2017: Science Signaling
https://www.readbyqxmd.com/read/28963471/supraspinal-selective-trpv1-desensitization-induced-by-intracerebroventricular-treatment-with-resiniferatoxin
#16
Akihiro Fukushima, Kizuku Mamada, Aki Iimura, Hideki Ono
The transient receptor potential vanilloid type 1 (TRPV1) is a thermosensitive cation channel that triggers heat pain in the periphery. Long-term desensitization of TRPV1, which can be induced by excess amounts of agonists, has been a method for investigating the physiological relevance of TRPV1-containing neuronal circuits, and desensitization induced by various routes of administration, including systemic, intrathecal and intraganglionic, has been demonstrated in rodents. In the present study, we examined the effect of intracerebroventricular (i...
September 29, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28949006/calcium-influx-through-trpv4-channels-modulates-the-adherens-contacts-between-retinal-microvascular-endothelial-cells
#17
Tam T T Phuong, Sarah N Redmon, Oleg Yarishkin, Jacob M Winter, Dean Y Li, David Križaj
KEY POINTS: Endothelial cells employ transient receptor potential isoform 4 (TRPV4) channels to sense ambient mechanical and chemical stimuli. In retinal microvascular endothelial cells, TRPV4 channels regulate calcium homeostasis, cytoskeletal signalling and the organization of adherens junctional contacts. Intracellular calcium increases induced by TRPV4 agonists include a significant contribution from calcium release from internal stores. Activation of TRPV4 channels regulates retinal endothelial barriers in vitro and in vivo...
November 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28945920/human-podocytes-express-functional-thermosensitive-transient-receptor-potential-vanilloid-trpv-channels
#18
Lídia Ambrus, Balázs Kelemen, Tamás Szabó, Tamás Bíró, Balázs István Tóth
BACKGROUND AND PURPOSE: Heat sensitive transient receptor potential vanilloid (TRPV) channels are expressed in various epithelial tissues regulating, among else, barrier functions. Their expression is well established in the distal nephron; however, we have no data about their presence in podocytes. Since podocytes are indispensable in the formation of the glomerular filtration barrier, we investigated the presence and function of Ca(2+) -permeable TRPV1-4 channels in human podocyte cultures...
September 25, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28925503/quantitative-analysis-of-mouse-dural-afferent-neurons-expressing-trpm8-vglut3-and-nf200
#19
Lynn Ren, Michelle Jaehee Chang, Zhiyu Zhang, Ajay Dhaka, Zhaohua Guo, Yu-Qing Cao
OBJECTIVE: To quantify the abundance of dural afferent neurons expressing transient receptor potential channel melastatin 8 (TRPM8), vesicular glutamate transporter 3 (VGLUT3), and neurofilament 200 (NF200) in adult mice. BACKGROUND: With the increasing use of mice as a model system to study headache mechanisms, it is important to understand the composition of dural afferent neurons in mice. In a previous study, we have measured the abundance of mouse dural afferent neurons that express neuropeptide calcitonin gene-related peptide as well as two TRP channels TRPV1 and TRPA1, respectively...
September 19, 2017: Headache
https://www.readbyqxmd.com/read/28903355/anti-proliferative-pro-apoptotic-and-anti-invasive-effect-of-ec-ev-system-in-human-osteosarcoma
#20
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
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