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https://www.readbyqxmd.com/read/27923234/transient-receptor-potential-vanilloid-1-channels-contribute-to-the-regulation-of-acid-and-base-induced-vasomotor-responses
#1
Ivan Ivic, Margit Solymar, Eszter Pakai, Zoltan Rumbus, Erika Pinter, Akos Koller, Andras Garami
pH changes can influence local blood flow, but the mechanisms of how acids and bases affect vascular tone is not fully clarified. Transient receptor potential vanilloid-1 (TRPV1) channels are expressed in vessels and can be activated by pH alterations. Thus, we hypothesized that TRPV1 channels are involved in the mediation of vascular responses to acid-base changes. Vasomotor responses to HCl, NaOH, and capsaicin were measured in isolated murine carotid and tail skin arteries. The function of TRPV1 was blocked by either of three approaches: Trpv1 gene disruption, pharmacological blockade with a TRPV1 antagonist (BCTC), and functional impairment of mainly neural TRPV1 channels (desensitization)...
December 7, 2016: Journal of Vascular Research
https://www.readbyqxmd.com/read/27916453/shank3-deficiency-impairs-heat-hyperalgesia-and-trpv1-signaling-in-primary-sensory-neurons
#2
Qingjian Han, Yong Ho Kim, Xiaoming Wang, Di Liu, Zhi-Jun Zhang, Alexandra L Bey, Mark Lay, Wonseok Chang, Temugin Berta, Yan Zhang, Yong-Hui Jiang, Ru-Rong Ji
Abnormal pain sensitivity is commonly associated with autism spectrum disorders (ASDs) and affects the life quality of ASD individuals. SHANK3 deficiency was implicated in ASD and pain dysregulation. Here, we report functional expression of SHANK3 in mouse dorsal root ganglion (DRG) sensory neurons and spinal cord presynaptic terminals. Homozygous and heterozygous Shank3 complete knockout (Δe4-22) results in impaired heat hyperalgesia in inflammatory and neuropathic pain. Specific deletion of Shank3 in Nav1...
November 24, 2016: Neuron
https://www.readbyqxmd.com/read/27900462/effects-of-a-trpv1-agonist-capsaicin-on-respiratory-rhythm-generation-in-brainstem-spinal-cord-preparation-from-newborn-rats
#3
Mariho Tani, Sayumi Kotani, Chikara Hayakawa, Shih-Tien Lin, Saki Irie, Keiko Ikeda, Kiyoshi Kawakami, Hiroshi Onimaru
The heat-sensitive transient receptor potential vanilloid 1 (TRPV1) channels are expressed in the peripheral and central nervous systems. However, there is no report on how the activation of TRPV1 causes the modulation of neuronal activity in the medullary respiratory center. We examined effects of capsaicin, a specific agonist of TRPV1 channels, on respiratory rhythm generation in brainstem-spinal cord preparation from newborn rats. Capsaicin induced a biphasic response in the respiratory rhythm (a transient decrease followed by an increase in the C4 rate)...
November 29, 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27899097/antinociception-of-petroleum-ether-fraction-derived-from-crude-methanol-extract-of-melastoma-malabathricum-leaves-and-its-possible-mechanisms-of-action-in-animal-models
#4
Z A Zakaria, E S Jaios, M H Omar, S Abd Rahman, S S A Hamid, S M Ching, L K Teh, M Z Salleh, S Deny, M Taher
BACKGROUND: Melastoma malabathricum L. (family Melastomaceae) has been traditionally used as remedies against various ailments including those related to pain. The methanol extract of M. malabathricum leaves has been proven to show antinociceptive activity. Thus, the present study aimed to determine the most effective fraction among the petroleum ether- (PEMM), ethyl acetate- (EAMM) and aqueous- (AQMM) fractions obtained through successive fractionation of crude, dried methanol extract of M...
November 29, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27899046/chili-pepper-as-a-body-weight-loss-food
#5
Sharon Varghese, Peter Kubatka, Luis Rodrigo, Katarina Gazdikova, Martin Caprnda, Julia Fedotova, Anthony Zulli, Peter Kruzliak, Dietrich Büsselberg
Chili has culinary as well as medical importance. Studies in humans, using a wide range of doses of chili intake (varying from a single meal to a continuous uptake for up to 12 weeks), concluded that it facilitates weight loss. In regard to this, the main targets of chili are fat metabolism, energy expenditure, and thermogenesis. To induce weight loss, the active substance of chili, capsaicin, activates Transient Receptor Potential Cation Channel sub-family V member 1 (TRPV1) channels) receptors causing an increase in intracellular calcium levels and triggering the sympathetic nervous system...
November 29, 2016: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/27886264/sigma-1-receptor-agonism-promotes-mechanical-allodynia-after-priming-the-nociceptive-system-with-capsaicin
#6
J M Entrena, C Sánchez-Fernández, F R Nieto, R González-Cano, S Yeste, E J Cobos, J M Baeyens
Sigma-1 receptor antagonists promote antinociception in several models of pain, but the effects of sigma-1 agonists on nociception (particularly when the nociceptive system is primed) are not so well characterized; therefore we evaluated the effects of sigma-1 agonists on pain under different experimental conditions. The systemic administration of the selective sigma-1 agonists (+)-pentazocine and PRE-084, as well as the nonselective sigma-1 agonist carbetapentane (used clinically as an antitussive drug), did not alter sensitivity to mechanical stimulation under baseline conditions...
November 25, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27883196/grifolin-derivatives-from-albatrellus-ovinus-as-trpv1-receptor-blockers-for-cosmetic-applications
#7
Stefan Hettwer, Stefan Bänziger, Brigit Suter, Barbara Obermayer
OBJECTIVE: Blocking the TRPV1 receptor is an interesting approach for the treatment of sensitive skin. Here we investigated the potential of grifolin derivatives from Albatrellus ovinus to act as TRPV1 receptor blockers and their potential to serve as cosmetic active ingredients. METHODS: Binding characteristics of grifolin derivatives from Albatrellus ovinus were determined in competitive and functional in vitro assays to achieve IC50 values. The TRPV1 receptor was activated in vivo with capsaicin and noxious heat to investigate skin reddening, microcirculation, skin sensations and heat pain thresholds...
November 24, 2016: International Journal of Cosmetic Science
https://www.readbyqxmd.com/read/27871896/gastroprotective-and-ulcer-healing-effects-of-hydroethanolic-extract-of-leaves-of-caryocar-coriaceum-mechanisms-involved-in-the-gastroprotective-activity
#8
Luis Jardelino de Lacerda Neto, Andreza Guedes Barbosa Ramos, Valterlucio Santos Sales, Severino Denicio Gonçalves de Souza, Antonia Thassya Lucas Dos Santos, Larissa Rolim de Oliveira, Marta Regina Kerntopf, Thais Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Lucindo Jose Quintans-Júnior, Almir Gonçalves Wanderley, Irwin Rose Alencar de Menezes
This work aimed to determine the chemical fingerprint of hydroethanolic extract of leaves of Caryocar coriaceum (HELCC) and the gastroprotective activity. The chemical fingerprint of HELCC was analyzed by HPLC-DAD, to quantify total phenols and flavonoids were carried out by Folin-Ciocalteu reagent and aluminum chloride assay, while in vitro antioxidant activity was evaluated by the DPPH method. The methods used to determine pharmacological activity were: gastroprotective screening test in classical models of induced acute and chronic gastric lesions and physical barrier test...
November 18, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27864110/antinociceptive-activity-and-mechanism-of-action-of-hydroalcoholic-extract-and-dichloromethane-fraction-of-amphilophium-crucigerum-seeds-in-mice
#9
Samira Dal Toé De Prá, Paula Ronsani Ferro, Alessandra Marcon Milioli, Flávia Karine Rigo, Orlando Justo Chipindo, Camila Camponogara, Rosana Casoti, Melânia Palermo Manfron, Sara Marchesan de Oliveira, Juliano Ferreira, Gabriela Trevisan
ETHNOPHARMACOLOGICAL RELEVANCE: The medicinal plant generally known as monkey's comb (Amphilophium crucigerum) has been popularly described for the treatment of neuropathic and inflammatory pain, specially seeds preparations. AIM OF THE STUDY: The goal of the present study was to evaluate the antinociceptive effect of the crude extract (Crd) and dichloromethane fraction (Dcm) of A. crucigerum seeds, and investigate the involvement of transient receptor potential vanilloid 1 (TRPV1) receptor in this effect...
November 15, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27827430/lactate-is-a-potent-inhibitor-of-the-capsaicin-receptor-trpv1
#10
Jeanne de la Roche, Isabella Walther, Waleria Leonow, Axel Hage, Mirjam Eberhardt, Martin Fischer, Peter W Reeh, Susanne Sauer, Andreas Leffler
Tissue ischemia results in an accumulation of lactate and local or systemic lactic acidosis. In nociceptive sensory neurons, lactate was reported to sensitize or activate the transient receptor potential ion channel TRPA1 and acid-sensing ion channels (ASICs). However, it is unclear how lactate modulates the TRPV1 regarded as the main sensor for acidosis in sensory neurons. In this study we investigated the effects of lactate (LA) on recombinant and native TRPV1 channels and on TRPV1-mediated release of neuropeptides from mouse nerves...
November 9, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27821307/in%C3%A2-vitro-activation-of-the-neuro-transduction-mechanism-in-sensitive-organotypic-human-skin-model
#11
Francesca Martorina, Costantino Casale, Francesco Urciuolo, Paolo A Netti, Giorgia Imparato
Recent advances in tissue engineering have encouraged researchers to endeavor the production of fully functional three-dimensional (3D) thick human tissues in vitro. Here, we report the fabrication of a fully innervated human skin tissue in vitro that recapitulates and replicates skin sensory function. Previous attempts to innervate in vitro 3D skin models did not demonstrate an effective functionality of the nerve network. In our approach, we initially engineer functional human skin tissue based on fibroblast-generated dermis and differentiated epidermis; then, we promote rat dorsal root ganglion (DRG) neurons axon ingrowth in the de-novo developed tissue...
January 2017: Biomaterials
https://www.readbyqxmd.com/read/27816008/in-silico-investigation-into-the-interactions-between-murine-5-ht3-receptor-and-the-principle-active-compounds-of-ginger-zingiber-officinale
#12
Anna E Lohning, Wolfgang Marx, Liz Isenring
Gingerols and shogaols are the primary non-volatile actives within ginger (Zingiber officinale). These compounds have demonstrated in vitro to exert 5-HT3 receptor antagonism which could benefit chemotherapy-induced nausea and vomiting (CINV). The site and mechanism of action by which these compounds interact with the 5-HT3 receptor is not fully understood although research indicates they may bind to a currently unidentified allosteric binding site. Using in silico techniques, such as molecular docking and GRID analysis, we have characterized the recently available murine 5-HT3 receptor by identifying sites of strong interaction with particular functional groups at both the orthogonal (serotonin) site and a proposed allosteric binding site situated at the interface between the transmembrane region and the extracellular domain...
October 26, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27792253/%C3%AE-5gabaa-receptors-mediate-tonic-inhibition-in-the-spinal-cord-dorsal-horn-and-contribute-to-the-resolution-of-hyperalgesia
#13
Jimena Perez-Sanchez, Louis-Etienne Lorenzo, Irene Lecker, Agnieszka A Zurek, Charalampos Labrakakis, Erica M Bridgwater, Beverley A Orser, Yves De Koninck, Robert P Bonin
Neuronal inhibition mediated by GABAA receptors constrains nociceptive processing in the spinal cord, and loss of GABAergic inhibition can produce allodynia and hyperalgesia. Extrasynaptic α5 subunit-containing GABAA receptors (α5GABAA Rs) generate a tonic conductance that inhibits neuronal activity and constrains learning and memory; however, it is unclear whether α5GABAA Rs similarly generate a tonic conductance in the spinal cord dorsal horn to constrain nociception. We assessed the distribution of α5GABAA Rs in the spinal cord dorsal horn by immunohistochemical analysis, and the activity and function of α5GABAA Rs in neurons of the superficial dorsal horn using electrophysiological and behavioral approaches in male, null-mutant mice lacking the GABAA R α5 subunit (Gabra5-/-) and wild-type mice (WT)...
October 28, 2016: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/27775662/capsaicin-suppresses-cell-proliferation-induces-cell-cycle-arrest-and-ros-production-in-bladder-cancer-cells-through-foxo3a-mediated-pathways
#14
Kaiyu Qian, Gang Wang, Rui Cao, Tao Liu, Guofeng Qian, Xinyuan Guan, Zhongqiang Guo, Yu Xiao, Xinghuan Wang
Capsaicin (CAP), a highly selective agonist for transient receptor potential vanilloid type 1 (TRPV1), has been widely reported to exhibit anti-oxidant, anti-inflammation and anticancer activities. Currently, several therapeutic approaches for bladder cancer (BCa) are available, but accompanied by unfavorable outcomes. Previous studies reported a potential clinical effect of CAP to prevent BCa tumorigenesis. However, its underlying molecular mechanism still remains unknown. Our transcriptome analysis suggested a close link among calcium signaling pathway, cell cycle regulation, ROS metabolism and FOXO signaling pathway in BCa...
October 21, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27774580/trpv1-attenuates-intracranial-arteriole-remodeling-through-inhibiting-vsmc-phenotypic-modulation-in-hypertension
#15
Ming-Jie Zhang, Yun Liu, Zi-Cheng Hu, Yi Zhou, Yan Pi, Lu Guo, Xu Wang, Xue Chen, Jing-Cheng Li, Li-Li Zhang
The phenotypic modulation of contractile vascular smooth muscle cell (VSMC) is widely accepted as the pivotal process in the arterial remodeling induced by hypertension. This study aimed to investigate the potential role of transient receptor potential vanilloid type 1 (TRPV1) on regulating VSMC plasticity and intracranial arteriole remodeling in hypertension. Spontaneously hypertensive rats (SHR), Wistar-Kyoto (WKY) rats and TRPV1(-/-) mice on a C57BL/6J background were used. By microscopic observation of the histopathological sections of vessels from hypertensive SHR and age-matched normotensive WKY control rats, we found that hypertension induced arterial remodeling...
October 24, 2016: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/27774522/the-effect-of-treatment-with-resiniferatoxin-and-capsaicin-on-dynamic-weight-bearing-measures-and-evoked-pain-responses-in-a-chronic-inflammatory-arthritis-murine-model
#16
Joseph Bert, Maren L Mahowald, Sandra Frizelle, Christopher W Dorman, Sonia C Funkenbusch, Hollis E Krug
OBJECTIVE: Capsaicin (CAP) and Resiniferatoxin (RTX) are vanilloid receptor agonists that can normalize Evoked Pain Scores (EPS) and Automated Dynamic Weight Bearing (ADWB) measures in murine acute inflammatory arthritis when given by intra-articular (IA) injection. To determine whether these vanilloid receptor agonists have benefit in Complete Freund's Adjuvant (CFA) induced chronic inflammatory arthritis pain, we measured changes in ADWB and EPS in arthritic mice with and without treatment with IA CAP and RTX...
2016: Internal Medicine Review (Washington, D.C.: Online)
https://www.readbyqxmd.com/read/27759880/ph%C3%AE-1%C3%AE-acts-as-a-trpa1-antagonist-with-antinociceptive-effects-in-mice
#17
Raquel Tonello, Camilla Fusi, Serena Materazzi, Ilaria M Marone, Francesco De Logu, Silvia Benemei, Muryel C Gonçalves, Elisabetta Coppi, Celio J Castro-Junior, Marcus Vinicius Gomez, Pierangelo Geppetti, Juliano Ferreira, Romina Nassini
BACKGROUND AND PURPOSE: Peptides from venomous animals have long been important for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide from the venom of the armed spider Phoneutria nigriventer, produces analgesia by blocking the TRPA1 channel. EXPERIMENTAL APPROACH: Cultured rat dorsal root ganglion (DRG) neurons, human fetal lung fibroblasts (IMR90) or HEK293 cells expressing the human TRPA1 (hTRPA1-HEK293), human TRPV1 (hTRPV1-HEK293) or human TRPV4 channels (hTRPV4-HEK293), were used for calcium imaging and electrophysiology...
October 19, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27758864/characterization-of-transient-receptor-potential-vanilloid-1-trpv1-variant-activation-by-coal-fly-ash-particles-and-associations-with-altered-transient-receptor-potential-ankyrin-1-trpa1-expression-and-asthma
#18
Cassandra E Deering-Rice, Chris Stockmann, Erin G Romero, Zhenyu Lu, Darien Shapiro, Bryan L Stone, Bernhard Fassl, Flory Nkoy, Derek A Uchida, Robert M Ward, John M Veranth, Christopher A Reilly
Transient receptor potential (TRP) channels are activated by environmental particulate materials. We hypothesized that polymorphic variants of transient receptor potential vanilloid-1 (TRPV1) would be uniquely responsive to insoluble coal fly ash compared with the prototypical soluble agonist capsaicin. Furthermore, these changes would manifest as differences in lung cell responses to these agonists and perhaps correlate with changes in asthma symptom control. The TRPV1-I315M and -T469I variants were more responsive to capsaicin and coal fly ash...
November 25, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27743812/mu-opioid-receptors-in-the-caudomedial-nts-are-critical-for-respiratory-responses-to-stimulation-of-bronchopulmonary-c-fibers-and-carotid-body-in-conscious-rats
#19
Jianguo Zhuang, Xiuping Gao, Franklin Gao, Fadi Xu
We tested the hypothesis that mu-opioid receptors (MORs) in the caudomedial nucleus tractus solitarius (cmNTS) are important for the ventilatory responses to stimulation of bronchopulmonary C-fibers (PCFs), the carotid body-mediated hypoxia, and hypercapnia independent of the carotid body. First, we used immunohistochemistry to map MORs distribution in the caudal medulla. Then we compared the effects of intra-cmNTS microinjection of DAMGO (a MOR agonist) with or without a combination of CTAP (a MOR antagonist) on the ventilatory responses to: 1) right atrial injection of capsaicin (to stimulation of PCFs) and 2) acute hypoxia (HVR, to stimulate the carotid body) in awake intact rats; and 3) hypercapnia (HCVR) in the carotid body ablated rats...
January 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/27739618/stimulating-trpv1-externalization-and-synthesis-in-dorsal-root-ganglion-neurons-contributes-to-pge2-potentiation-of-trpv1-activity-and-nociceptor-sensitization
#20
W Ma, B St-Jacques, U Rudakou, Y N Kim
BACKGROUND: Persistent peripheral sensitization contributes to chronic pain. Plasticity of nociceptive dorsal root ganglion (DRG) neurons (nociceptors) induced by pro-inflammatory mediators contributes to sensitization. Prostaglandin E2 (PGE2) enriched in injured tissues is known not only directly to sensitize DRG neurons, but also to potentiate sensitizing effects of other pain mediators such as capsaicin and its receptor transient receptor potential vanilloid-1 (TRPV1). It remains unknown whether PGE2 potentiates TRPV1 activity by stimulating its synthesis, cell surface and axonal trafficking in DRG neurons...
October 14, 2016: European Journal of Pain: EJP
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