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TRPV1 receptor agonist

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https://www.readbyqxmd.com/read/28213106/oral-treatment-with-essential-oil-of-hyptis-spicigera-lam-lamiaceae-reduces-acute-pain-and-inflammation-in-mice-potential-interactions-with-transient-receptor-potential-trp-ion-channels
#1
Róli Rodrigues Simões, Igor Dos Santos Coelho, Stella Célio Junqueira, Glauce Regina Pigatto, Marcos José Salvador, Adair Roberto Soares Santos, Felipe Meira de Faria
ETHNOPHARMACOLOGICAL RELEVANCE: The genus Hyptis comprehends almost 400 species widespread in tropical and temperate regions of America. The use of Hyptis spicigera Lam. (Lamiaceae) is reported in traditional medicine due to its gastroprotective, anti-inflammatory and analgesic properties. AIM OF THE STUDY: The rationale of this study was to investigate the potential use of the essential oil of H. spicigera (EOHs) as analgesic. MATERIAL AND METHODS: The antinociceptive effect of EOHs was verified analyzing acute nocifensive behavior of mice induced by chemical noxious stimuli [i...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28188777/enhanced-ability-of-trpv1-channels-in-regulating-glutamatergic-transmission-after-repeated-morphine-exposure-in-the-nucleus-accumbens-of-rat
#2
Haitao Zhang, Dong Jia, Yuan Wang, Liang Qu, Xuelian Wang, Jian Song, Lijun Heng, Guodong Gao
Glutamatergic projections to nucleus accumbens (NAc) drive drug-seeking behaviors during opioids withdrawal. Modulating glutamatergic neurotransmission provides a novel pharmacotherapeutic avenue for treatment of opioids dependence. Great deals of researches have verified that transient receptor potential vanilloid 1 (TRPV1) channels alters synaptic transmitter release and regulate neural plasticity. In the present study, whole-cell patch clamp recordings were adopted to examine the activity of TRPV1 Channels in regulating glutamate-mediated excitatory postsynaptic currents (EPSCs) in NAc of rat during morphine withdrawal for 3 days and 3 weeks...
February 7, 2017: Brain Research
https://www.readbyqxmd.com/read/28133727/diet-induced-obesity-enhances-trpv1-mediated-neurovascular-reactions-in-the-dura-mater
#3
Balázs Marics, Barna Peitl, Kitti Pázmándi, Attila Bácsi, József Németh, Orsolya Oszlács, Gábor Jancsó, Mária Dux
OBJECTIVE: Exploring the pathophysiological changes in transient receptor potential vanilloid 1 (TRPV1) receptor of the trigeminovascular system in high-fat, high-sucrose (HFHS) diet-induced obesity of experimental animals. BACKGROUND: Clinical and experimental observations suggest a link between obesity and migraine. Accumulating evidence indicates that metabolic and immunological alterations associated with obesity may potentially modulate trigeminovascular functions...
January 30, 2017: Headache
https://www.readbyqxmd.com/read/28123347/forsythoside-a-exerts-antipyretic-effect-on-yeast-induced-pyrexia-mice-via-inhibiting-transient-receptor-potential-vanilloid-1-function
#4
Cuiling Liu, Hongchang Su, Hongye Wan, Qingxia Qin, Xuan Wu, Xiangying Kong, Na Lin
Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel gated by noxious heat, playing major roles in thermoregulation. Forsythoside A (FT-A) is the most abundant phenylethanoid glycosides in Fructus Forsythiae, which has been prescribed as a medicinal herb for treating fever in China for a long history. However, how FT-A affects pyrexia and what is the underlying molecular mechanism remain largely unknown. Here we found that FT-A exerted apparent antipyretic effect through decreasing the levels of prostaglandin E2 (PGE2) and interleukin 8 (IL-8) in a dose-dependent fashion on the yeast induced pyrexia mice...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/28118665/functional-properties-of-sensory-nerve-terminals-of-the-mouse-cornea
#5
Omar González-González, Federico Bech, Juana Gallar, Jesús Merayo-Lloves, Carlos Belmonte
Purpose: To define the firing properties of sensory nerve terminals innervating the adult mouse cornea in response to external stimuli of differing modality. Methods: Extracellular electrical activity of single corneal sensory nerve terminals was recorded in excised eyes of C57BL/6J mice. Eyes were placed in a recording chamber and were continuously superfused with warm saline solution. Nerve terminal impulse (NTI) activity was recorded by means of a glass pipette (tip ∼ 50 μm), applied on the corneal surface...
January 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28112976/effects-of-cannabinoid-and-vanilloid-receptor-agonists-and-their-interaction-on-learning-and-memory-in-rats
#6
Mariam Shiri, Alireza Komaki, Shahrbanoo Oryan, Masoumeh Taheri, Hamidreza Komaki, Farshid Etaee
Despite previous findings on the effects of cannabinoid and vanilloid systems on learning and memory, the effects of the combined stimulation of these 2 systems on learning and memory have not been studied. Therefore, in this study, we tested the interactive effects of cannabinoid and vanilloid systems on learning and memory in rats by using passive avoidance learning (PAL) tests. Forty male Wistar rats were divided into the following 4 groups: (1) control (DMSO+saline), (2) WIN55,212-2, (3) capsaicin, and (4) WIN55,212-2 + capsaicin...
November 2, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28104916/trpv1-activation-counters-diet-induced-obesity-through-sirtuin-1-activation-and-prdm-16-deacetylation-in-brown-adipose-tissue
#7
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/28088386/trypsin-induces-biphasic-muscle-contraction-and-relaxation-via-transient-receptor-potential-vanilloid-1-and-neurokinin-receptors-1-2-in-porcine-esophageal-body
#8
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/28087250/pharmacology-of-cannabinoids-in-the-treatment-of-epilepsy
#9
REVIEW
Tyler E Gaston, Daniel Friedman
The use of cannabis products in the treatment of epilepsy has long been of interest to researchers and clinicians alike; however, until recently very little published data were available to support its use. This article summarizes the available scientific data of pharmacology from human and animal studies on the major cannabinoids which have been of interest in the treatment of epilepsy, including ∆9-tetrahydrocannabinol (∆9-THC), cannabidiol (CBD), ∆9-tetrahydrocannabivarin (∆9-THCV), cannabidivarin (CBDV), and ∆9-tetrahydrocannabinolic acid (Δ9-THCA)...
January 10, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28076819/full-spectral-multiplexing-of-bioluminescence-resonance-energy-transfer-in-three-trpv-channels
#10
Hermanus Johannes Ruigrok, Guillaume Shahid, Bertrand Goudeau, Florence Poulletier de Gannes, Emmanuelle Poque-Haro, Annabelle Hurtier, Isabelle Lagroye, Pierre Vacher, Stéphane Arbault, Neso Sojic, Bernard Veyret, Yann Percherancier
Multiplexed bioluminescence resonance energy transfer (BRET) assays were developed to monitor the activation of several functional transient receptor potential (TRP) channels in live cells and in real time. We probed both TRPV1 intramolecular rearrangements and its interaction with Calmodulin (CaM) under activation by chemical agonists and temperature. Our BRET study also confirmed that: (1) capsaicin and heat promoted distinct transitions, independently coupled to channel gating, and that (2) TRPV1 and Ca(2+)-bound CaM but not Ca(2+)-free CaM were preassociated in resting live cells, while capsaicin activation induced both the formation of more TRPV1/CaM complexes and conformational changes...
January 10, 2017: Biophysical Journal
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/28062311/trpa1-and-trpv1-antagonists-do-not-inhibit-human-acidosis-induced-pain
#12
Matthias G Schwarz, Barbara Namer, Peter W Reeh, Michael J M Fischer
: Acidosis occurs in a variety of pathophysiological and painful conditions where it is thought to excite or contribute to excitation of nociceptive neurons. Despite potential clinical relevance the principal receptor for sensing acidosis is unclear, but several receptors have been proposed. We investigated the contribution of the acid sensing ion channels, TRPV1 and TRPA1 to peripheral pain signaling. We first established a human pain model using intra-epidermal injection of TRPA1 agonist carvacrol...
January 3, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28038937/cellular-permeation-of-large-molecules-mediated-by-trpm8-channels
#13
Daniel D McCoy, Radhika Palkar, Yuening Yang, Serra Ongun, David D McKemy
While most membrane channels are only capable of passing small ions, certain non-selective cation channels have been recently shown to have the capacity to permeate large cations. The mechanisms underlying large molecule permeation are unclear, but this property has been exploited pharmacologically to target molecules, such as nerve conduction blockers, to specific subsets of pain-sensing neurons (nociceptors) expressing the heat-gated transient receptor potential (TRP) channel TRPV1. However, it is not clear if the principal mediator of cold stimuli TRPM8 is capable of mediating the permeation large molecules across cell membranes, suggesting that TRPM8-positive nerves cannot be similarly targeted...
February 3, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28008282/expression-and-functionality-of-trpv1-in-breast-cancer-cells
#14
Lea V Weber, Klaudia Al-Refae, Gerhard Wölk, Gabriele Bonatz, Janine Altmüller, Christian Becker, Günter Gisselmann, Hanns Hatt
Transient receptor potential (TRP) channels contribute to the regulation of intracellular calcium, which can promote cancer hallmarks in cases of dysregulation of gene transcription and calcium-dependent pro-proliferative or anti-apoptotic mechanisms. Several studies have begun to elucidate the roles of TRPV1, TRPV6, TRPM8, and TRPC1 in cancer progression; however, no study has examined the expression profiles of human TRP channels in breast cancer on a large scale. This study focused on the expression and functionality of TRPV1, a nonselective cation channel that was found to be expressed in different carcinoma tissues...
2016: Breast Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/27992447/heat-sensing-receptor-trpv1-is-a-mediator-of-thermotaxis-in-human-spermatozoa
#15
Luca De Toni, Andrea Garolla, Massimo Menegazzo, Sabina Magagna, Andrea Di Nisio, Iva Šabović, Maria Santa Rocca, Valentina Scattolini, Andrea Filippi, Carlo Foresta
The molecular bases of sperm thermotaxis, the temperature-oriented cell motility, are currently under investigation. Thermal perception relies on a subclass of the transient receptor potential [TRP] channels, whose member TRPV1 is acknowledged as the heat sensing receptor. Here we investigated the involvement of TRPV1 in human sperm thermotaxis. We obtained semen samples from 16 normozoospermic subjects attending an infertility survey programme, testis biopsies from 6 patients with testicular germ cell cancer and testis fine needle aspirates from 6 patients with obstructive azoospermia undergoing assisted reproductive technologies...
2016: PloS One
https://www.readbyqxmd.com/read/27979980/heat-induces-interleukin-6-in-skeletal-muscle-cells-via-trpv1-pkc-creb-pathways
#16
Syotaro Obi, Toshiaki Nakajima, Takaaki Hasegawa, Hironobu Kikuchi, Gaku Oguri, Masao Takahashi, Fumitaka Nakamura, Tatsuya Yamasoba, Masashi Sakuma, Shigeru Toyoda, Chuwa Tei, Teruo Inoue
Interluekin-6 (IL-6) is released from skeletal muscle cells and induced by exercise, heat, catecholamine, glucose, lipopolysaccharide, reactive oxygen species, and inflammation. However, the mechanism, which induces release of IL-6 from skeletal muscle cells, remains unknown. Thermo-sensitive transient receptor potential (TRP) proteins such as TRPV1-4 play vital roles in cellular functions. In this study we hypothesized that TRPV1 senses heat, transmits a signal into the nucleus, and produces IL-6. The purpose of the present study is to investigate the underlying mechanisms, where skeletal muscle cells sense heat and respond to it...
December 15, 2016: Journal of Applied Physiology
https://www.readbyqxmd.com/read/27977070/role-of-transient-receptor-potential-ankyrin-1-receptors-in-rodent-models-of-meningeal-nociception-experiments-in%C3%A2-vitro
#17
A C Denner, B Vogler, K Messlinger, R De Col
BACKGROUND: The TRP channel ankyrin type 1 (TRPA1) is a nonselective cation channel known to be activated by environmental irritants, cold and endogenous mediators of inflammation. Activation of TRPA1 in trigeminal afferents innervating meningeal structures has recently been suggested to be involved in the generation of headaches. METHODS: Two in vitro models of meningeal nociception were employed using the hemisected rodent head preparation, (1) recording of single meningeal afferents and (2) release of calcitonin gene-related peptide (CGRP) from the cranial dura mater...
December 15, 2016: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27951473/oleuropein-aglycone-enhances-ucp1-expression-in-brown-adipose-tissue-in-high-fat-diet-induced-obese-rats-by-activating-%C3%AE-adrenergic-signaling
#18
Yuriko Oi-Kano, Yusaku Iwasaki, Toshiyuki Nakamura, Tatsuo Watanabe, Tsuyoshi Goto, Teruo Kawada, Kenichi Watanabe, Kazuo Iwai
Oleuropein is the pungent principle of raw olives. Oleuropein aglycone (OA) is a major phenolic compound in extra virgin olive oil and the absorbed form of oleuropein. We aimed to determine the mechanism underlying the nutritional effects of oleuropein and OA on interscapular brown adipose tissue (IBAT) in rats with high-fat (HF) diet-induced obesity by examining the agonistic activity of oleuropein and OA toward the transient receptor potential ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1). Four-week-old male Sprague-Dawley rats were fed an HF (palm oil 30% wt:wt) diet alone or with oleuropein (HF-O, 1 g/kg diet) for 28 days...
November 23, 2016: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/27938441/a-dual-inhibitor-of-faah-and-trpv1-channels-shows-dose-dependent-effect-on-depression-like-behaviour-in-rats
#19
Christian Kirkedal, Gregers Wegener, Fabricio Moreira, Sâmia Regiane Lourenco Joca, Nico Liebenberg
OBJECTIVE: The cannabinoid receptor 1 (CB1) and transient receptor potential cation channel subfamily V member 1 (TRPV1) are proposed to mediate opposite behavioural responses. Their common denominator is the endocannabinoid ligand anandamide (AEA), which is believed to mediate antidepressant-like effect via CB1-R stimulation and depressive-like effect via TRPV1 activation. This is supposed to explain the bell-shaped dose-response curve for anandamide in preclinical models. METHODS: We investigated this assumption by administering the dual inhibitor of AEA hydrolysis and TRPV1 activation N-arachidonoyl-serotonin (AA-5HT) into the medial prefrontal cortex of rats...
December 12, 2016: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/27919827/pkc%C3%AE-ii-mediated-cross-talk-of-trpv1-cb2-modulates-the-glucocorticoid-induced-osteoclast-overactivity
#20
Giulia Bellini, Marco Torella, Iolanda Manzo, Chiara Tortora, Livio Luongo, Francesca Punzo, Nicola Colacurci, Bruno Nobili, Sabatino Maione, Francesca Rossi
In this study, we investigated the role of the endovanilloid/endocannabinoid system in the glucocorticoid-induced osteoclast overactivity. Receptorial and enzymatic component of the endovanilloid/endocannabinoid system are expressed in bone cells, and dysregulated when bone mass is reduced. Moreover, blockade or desensitization of vanilloid receptor 1 (TRPV1) and/or stimulation of cannabinoid receptor 2 (CB2) are beneficial for reducing number and activity of the bone cells modulating resorption, the osteoclasts...
January 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
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