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TRPV1 receptor agonist

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https://www.readbyqxmd.com/read/29342359/semiconducting-photothermal-nanoagonist-for-remote-controlled-specific-cancer-therapy
#1
Xu Zhen, Chen Xie, Yuyan Jiang, Xiangzhao Ai, Bengang Xing, Kanyi Pu
Nanomedicines have shown success in cancer therapy, but the pharmacological actions of most nanomedicine are often nonspecific to cancer cells because of utilization of the therapeutic agents that induce cell apoptosis from inner organelles. We herein report the development of semiconducting photothermal nanoagonists that can remotely and specifically initiate the apoptosis of cancer cells from cell membrane. The organic nanoagonists comprise semiconducting polymer nanoparticles (SPNs) and capsaicin (Cap) as the photothermally-responsive nanocarrier and the agonist for activation of transient receptor potential cation channel subfamily V member 1 (TRPV1), respectively...
January 17, 2018: Nano Letters
https://www.readbyqxmd.com/read/29338068/single-and-combined-effects-of-plant-derived-thc-cbd-and-synthetic-win-55-212-cannabinoids-on-cognition-and-cannabinoid-associated-withdrawal-signs-in-mice
#2
Alyssa M Myers, Patrick B Siegele, Jeffrey D Foss, Ronald F Tuma, Sara Jane Ward
BACKGROUND AND PURPOSE: It has been suggested that the non-euphorogenic phytocannabinoid cannabidiol (CBD) can ameliorate adverse effects of delta-9-tetrahydrocannabinol (THC). We determined whether CBD ameliorates cognitive deficits and withdrawal signs induced by cannabinoid CB1/CB2 receptor agonists or produces these pharmacological effects on its own. EXPERIMENTAL APPROACH: The effects of THC or the CB1/CB2 receptor full agonist WIN55212 (WIN) alone, CBD alone, or their combination were tested across a range of doses...
January 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29317663/trpv1-enhances-the-afferent-response-to-p2x-receptor-activation-in-the-mouse-urinary-bladder
#3
Luke Grundy, Donna M Daly, Christopher Chapple, David Grundy, Russ Chess-Williams
Both TRPV1 and P2X receptors present on bladder sensory nerve fibres have been implicated in mechanosensation during bladder filling. The aim of this study was to determine possible interactions between these receptors in modulating afferent nerve activity. In wildtype (TRPV1+/+) and TRPV1 knockout (TRPV1-/-) mice, bladder afferent nerve activity, intravesical pressure, and luminal ATP and acetylcholine levels were determined and also intracellular calcium responses of dissociated pelvic DRG neurones and primary mouse urothelial cells (PMUCs)...
January 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29306760/effect-of-acetaminophen-on-osteoblastic-differentiation-and-migration-of-mc3t3-e1-cells
#4
Yoshihiro Nakatsu, Fumio Nakagawa, Sen Higashi, Tomoko Ohsumi, Shunji Shiiba, Seiji Watanabe, Hiroshi Takeuchi
BACKGROUND: N-acetyl-p-aminophenol (APAP, acetaminophen, paracetamol) is a widely used analgesic/antipyretic with weak inhibitory effects on cyclooxygenase (COX) compared to non-steroidal anti-inflammatory drugs (NSAIDs). The mechanism of action of APAP is mediated by its metabolite that activates transient receptor potential channels, including transient receptor potential vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1) or the cannabinoid receptor type 1 (CB1). However, the exact molecular mechanism and target underlying the cellular actions of APAP remain unclear...
July 15, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29304162/adrenergic-receptors-inhibit-trpv1-activity-in-the-dorsal-root-ganglion-neurons-of-rats
#5
Yumi Matsushita, Miki Manabe, Naoki Kitamura, Izumi Shibuya
Transient receptor potential vanilloid type 1 (TRPV1) is a polymodal receptor channel that responds to multiple types of stimuli, such as heat, acid, mechanical pressure and some vanilloids. Capsaicin is the most commonly used vanilloid to stimulate TRPV1. TRPV1 channels are expressed in dorsal root ganglion neurons that extend to Aδ- and C-fibers and have a role in the transduction of noxious inputs to the skin into the electrical signals of the sensory nerve. Although noradrenergic nervous systems, including the descending antinociceptive system and the sympathetic nervous system, are known to modulate pain sensation, the functional association between TRPV1 and noradrenaline in primary sensory neurons has rarely been examined...
2018: PloS One
https://www.readbyqxmd.com/read/29285308/decisive-role-of-p42-44-mitogen-activated-protein-kinase-in-%C3%AE-9-tetrahydrocannabinol-induced-migration-of-human-mesenchymal-stem-cells
#6
Ellen Lüder, Robert Ramer, Kirsten Peters, Burkhard Hinz
In past years, medical interest in Δ9-tetrahydrocannabinol (THC), the major psychoactive ingredient of the Cannabis plant, has been renewed due to the elucidation of the endocannabinoid system and diverse other receptor targets involved in biological cannabinoid effects. The present study therefore investigates the impact of THC on the migration of mesenchymal stem cells (MSCs) which are known to be involved in various regenerative processes such as bone healing. Using Boyden chamber assays, THC was found to increase the migration of adipose-derived MSCs...
December 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/29282753/possible-involvement-of-transient-receptor-potential-ankyrin-1-in-ca2-signaling-via-t-type-ca2-channel-in-mouse-sensory-neurons
#7
Yuki Nishizawa, Kenji Takahashi, Naoko Oguma, Makoto Tominaga, Toshio Ohta
T-type Ca2+ channels and TRPA1 are expressed in sensory neurons and both are associated with pain transmission, but their functional interaction is unclear. Here we demonstrate that pharmacological evidence of the functional relation between T-type Ca2+ channels and TRPA1 in mouse sensory neurons. Low concentration of KCl at 15 mM (15K) evoked increases of intracellular Ca2+ concentration ([Ca2+ ]i ), which were suppressed by selective T-type Ca2+ channel blockers. RT-PCR showed that mouse sensory neurons expressed all subtypes of T-type Ca2+ channel...
December 28, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/29274880/cb1-cannabinoid-receptor-agonist-mouse-vd-hemopressin-%C3%AE-produced-supraspinal-analgesic-activity-in-the-preclinical-models-of-pain
#8
Ting Zheng, Run Zhang, Ting Zhang, Meng-Na Zhang, Biao Xu, Jing-Jing Song, Ning Li, Hong-Hai Tang, Pei Wang, Rui Wang, Quan Fang
Mouse VD-hemopressin(α) (VD-Hpα) is an undecapeptide that selectively activates CB1 cannabinoid receptor in in vitro functional tests, and exerts CB1-mediated central antinociception in the mouse tail-flick assay. The aim of the present study was to further investigate the analgesic properties of supraspinal mouse VD-Hpα in a range of preclinical pain models. Our results indicated that the classical cannabinoid agonist WIN 55,212-2 produced supraspinal analgesia in preclinical pain models, which was selectively antagonized by the CB1 antagonist/inverse agonist AM251, but not by the CB2 antagonist AM630...
December 21, 2017: Brain Research
https://www.readbyqxmd.com/read/29273526/activation-of-the-capsaicin-receptor-trpv1-by-the-acetaminophen-metabolite-n-arachidonoylaminophenol-results-in-cytotoxicity
#9
Thomas Stueber, Susanne Meyer, Annette Jangra, Axel Hage, Mirjam Eberhardt, Andreas Leffler
AIMS: The anandamide reuptake inhibitor N-arachidonoylaminophenol (AM404) and the reactive substance N-acetyl-p-benzoquinone imine (NAPQI) are both metabolites of acetaminophen and may contribute to acetaminophen-induced analgesia by acting at TRPV1 expressed in the peripheral or central nervous system. While NAPQI slowly sensitizes and activates TRPV1 by interacting with distinct intracellular cysteine residues, detailed properties of AM404 as an agonist of TRPV1 have not yet been reported on...
December 19, 2017: Life Sciences
https://www.readbyqxmd.com/read/29237478/am404-paracetamol-metabolite-prevents-prostaglandin-synthesis-in-activated-microglia-by-inhibiting-cox-activity
#10
Soraya Wilke Saliba, Ariel R Marcotegui, Ellen Fortwängler, Johannes Ditrich, Juan Carlos Perazzo, Eduardo Muñoz, Antônio Carlos Pinheiro de Oliveira, Bernd L Fiebich
BACKGROUND: N-arachidonoylphenolamine (AM404), a paracetamol metabolite, is a potent agonist of the transient receptor potential vanilloid type 1 (TRPV1) and low-affinity ligand of the cannabinoid receptor type 1 (CB1). There is evidence that AM404 exerts its pharmacological effects in immune cells. However, the effect of AM404 on the production of inflammatory mediators of the arachidonic acid pathway in activated microglia is still not fully elucidated. METHOD: In the present study, we investigated the effects of AM404 on the eicosanoid production induced by lipopolysaccharide (LPS) in organotypic hippocampal slices culture (OHSC) and primary microglia cultures using Western blot, immunohistochemistry, and ELISA...
December 13, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29225040/differential-neuromodulatory-role-of-endocannabinoids-in-the-rodent-trigeminal-sensory-ganglion-and-cerebral-cortex-relevant-to-pain-processing
#11
Francesca Eroli, Inge C M Loonen, Arn M J M van den Maagdenberg, Else A Tolner, Andrea Nistri
Endocannabinoids are suggested to control pain, even though their clinical use is not fully validated and the underlying mechanisms are incompletely understood. To clarify the targets of endocannabinoid actions, we studied how activation of the endocannabinoid CB1 receptor (CB1R) affects neuronal responses in two in vitro preparations of rodents, namely the trigeminal sensory ganglion (TG) in culture and a coronal slice of the cerebral cortex. On TG small-medium size neurons, we tested whether submicromolar concentrations of the endogenous CB1R agonist anandamide (AEA) modulated inhibitory GABAA receptors and excitatory ATP-gated P2X3 receptors...
December 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29209900/effect-of-testosterone-on-trpv1-expression-in-a-model-of-orofacial-myositis-pain-in-the-rat
#12
Xiaofeng Bai, Xia Zhang, Qing Zhou
Recent clinical studies have revealed sex differences in response to transient receptor potential vanilloid 1 (TRPV1) agonist-induced pain. However, the mechanism of these differences in TRPV1-related chronic pain remains unclear. In the present study, we investigate the effects of inflammation and gonadal hormones on TRPV1 expression in trigeminal ganglia. Inflammatory pain was modeled by injecting complete Freund's adjuvant (CFA) into the left masseter muscle in rats. TRPV1 mRNA and protein levels in the trigeminal ganglia of male and female rats following CFA injection were assessed...
December 5, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/29198921/research-progress-of-capsaicin-responses-to-various-pharmacological-challenges
#13
REVIEW
Pompy Patowary, Manash Pratim Pathak, Kamaruz Zaman, P S Raju, Pronobesh Chattopadhyay
Capsaicin, a well known vanilloid, has shown evidence of an ample variety of biological effects which make it the target of extensive research ever since its identification. In spite of the fact that capsaicin causes health hazards in quite a few ways, yet, the verity cannot be ignored that capsaicin has several therapeutic implications. In patients with hypersensitive bladders, vesical instillation of 1 mM capsaicin markedly improved urinary frequency and urge incontinence. Again, administration of capsaicin favors an augmentation in lipid mobilization and a decrease in adipose tissue mass...
December 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29185571/capsaicin-inhibits-the-metastasis-of-human-papillary-thyroid-carcinoma-bcpap-cells-through-the-modulation-of-the-trpv1-channel
#14
Shichen Xu, Li Zhang, Xian Cheng, Huixin Yu, Jiandong Bao, Rongrong Lu
Capsaicin (CAP), a potent transient receptor potential vanilloid type 1 (TRPV1) agonist, is a major ingredient of red pepper. Recently, capsaicin has attracted increasing attention owing to its multiple biological activities. However, the anticancer effects of capsaicin against various types of cancers, especially on thyroid carcinoma, have not been completely elucidated. TRPV1, which can be activated by capsaicin, plays a key role in many biological and physiological processes. In the present study, the anticancer properties of capsaicin against papillary thyroid cancer BCPAP cells were investigated...
November 29, 2017: Food & Function
https://www.readbyqxmd.com/read/29180855/aural-stimulation-with-capsaicin-ointment-improved-swallowing-function-in-elderly-patients-with-dysphagia-a-randomized-placebo-controlled-double-blind-comparative-study
#15
Eiji Kondo, Osamu Jinnouchi, Seiichi Nakano, Hiroki Ohnishi, Ikuji Kawata, Hidehiko Okamoto, Noriaki Takeda
Objective: The aim of this study was to assess whether aural stimulation with ointment containing capsaicin improves swallowing function in elderly patients with dysphagia. Study design: A randomized, placebo-controlled, double-blind, comparative study. Settings: Secondary hospital. Patients and methods: Twenty elderly dysphagic patients with a history of cerebrovascular disorder or Parkinson's disease were randomly divided into two groups: 10 receiving aural stimulation with 0...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/29169961/the-cannabinoid-transporter-inhibitor-omdm-2-reduces-social-interaction-further-evidence-for-transporter-mediated-endocannabinoid-release
#16
Alexandre Seillier, Andrea Giuffrida
Experimental evidence suggests that the transport of endocannabinoids might work bi-directionally. Accordingly, it is possible that pharmacological blockade of the latter affects not only the re-uptake, but also the release of endocannabinoids, thus preventing them from stimulating CB1 receptors. We used biochemical, pharmacological, and behavioral approaches to investigate the effects of the transporter inhibitor OMDM-2 on social interaction, a behavioral assay that requires activation of CB1 receptors. The underlying mechanisms of OMDM-2 were compared with those of the Fatty Acid Amide Hydrolase (FAAH) inhibitor URB597...
November 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29156899/modulating-the-endocannabinoid-pathway-as-treatment-for-peripheral-neuropathic-pain-a-selected-review-of-preclinical-studies
#17
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
#18
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
#19
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
#20
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
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