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capsaicin receptor

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 tools for understanding pain mechanisms and for the discovery of pain treatments. Here, we hypothesized that Phα1β, a peptide purified from the armed spider Phoneutria nigriventer venom, produces analgesia by blocking the transient receptor potential ankyrin 1 (TRPA1) channel. EXPERIMENTAL APPROACH: Cultured rat dorsal root ganglion (DRG) neurons, human IMR90 fibroblasts or HEK293 cells expressing the human TRPA1 (hTRPA1-HEK293), TRPV1 (hTRPV1-HEK293) or TRPV4 (hTRPV4-HEK293), were used for calcium imaging and electrophysiology...
October 19, 2016: British Journal of Pharmacology
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...
October 12, 2016: Respiratory Physiology & Neurobiology
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
Damir Omerbašić, Ewan St J Smith, Mirko Moroni, Johanna Homfeld, Ole Eigenbrod, Nigel C Bennett, Jane Reznick, Chris G Faulkes, Matthias Selbach, Gary R Lewin
The naked mole-rat is a subterranean rodent lacking several pain behaviors found in humans, rats, and mice. For example, nerve growth factor (NGF), an important mediator of pain sensitization, fails to produce thermal hyperalgesia in naked mole-rats. The sensitization of capsaicin-sensitive TRPV1 ion channels is necessary for NGF-induced hyperalgesia, but naked mole-rats have fully functional TRPV1 channels. We show that exposing isolated naked mole-rat nociceptors to NGF does not sensitize TRPV1. However, the naked mole-rat NGF receptor TrkA displays a reduced ability to engage signal transduction pathways that sensitize TRPV1...
October 11, 2016: Cell Reports
Shi-Xun Ma, Seung-Hwan Kwon, Jee-Yeon Seo, Ji-Young Hwang, Sa-Ik Hong, Hyoung-Chun Kim, Seok-Yong Lee, Choon-Gon Jang
Transient receptor potential vanilloid type 1 (TRPV1), the archetypal member of the vanilloid TRP family, was initially identified as the receptor for capsaicin, the pungent ingredient in hot chili peppers. We previously demonstrated that TRPV1 in the dorsal striatum significantly contributes to morphine reward by using the conditioned place preference paradigm in mice; however, it is unknown whether TRPV1 has the same effect in other reward models. In this study, we investigated the role of TRPV1 in morphine reward by using a self-administration paradigm in rats...
October 11, 2016: Addiction Biology
Tao Liu, Gang Wang, Huangheng Tao, Zhonghua Yang, Yongzhi Wang, Zhe Meng, Rui Cao, Yu Xiao, Xinghuan Wang, Jiajie Zhou
BACKGROUND: Renal cell carcinoma (RCC) is one of the tumors most refractory to chemotherapy to date. Therefore, novel therapeutic agents are urgently needed for this disease. Capsaicin (CPS), a natural active ingredient of green and red peppers, and a ligand of transient receptor potential vanilloid type 1 (TRPV1), has been showed potential in suppression of tumorigenesis of several cancers. Nonetheless, the anti-cancer activity of CPS has never been studied in human RCC. METHODS: CCK8 analysis, LDH release activity and ROS generation analysis, flow cytometry analysis, and nuclear staining test were performed to test the influence of CPS in cultured cells in vitro, meanwhile western blot was done to uncover the precise molecular mechanisms...
October 12, 2016: BMC Cancer
Maxi Weyer, Heinz-Georg Jahnke, Dana Krinke, Franziska D Zitzmann, Kerstin Hill, Michael Schaefer, Andrea A Robitzki
The analysis of receptor activity, especially in its native cellular environment, has always been of great interest to evaluate its intrinsic but also downstream biological activity. An important group of cellular receptors are ion channels. Since they are involved in a broad range of crucial cell functions, they represent important therapeutic targets. Thus, novel analytical techniques for the quantitative monitoring and screening of biological receptor activity are of great interest. In this context, we developed an impedance spectroscopy-based label-free and non-invasive monitoring system that enabled us to analyze the activation of the transient receptor potential channel Vanilloid 1 (TRPV1) in detail...
October 8, 2016: Analytical and Bioanalytical Chemistry
Sara L Morales-Lázaro, Itzel Llorente, Félix Sierra-Ramírez, Ana E López-Romero, Miguel Ortíz-Rentería, Barbara Serrano-Flores, Sidney A Simon, León D Islas, Tamara Rosenbaum
The transient receptor potential vanilloid 1 (TRPV1) ion channel is mainly found in primary nociceptive afferents whose activity has been linked to pathophysiological conditions including pain, itch and inflammation. Consequently, it is important to identify naturally occurring antagonists of this channel. Here we show that a naturally occurring monounsaturated fatty acid, oleic acid, inhibits TRPV1 activity, and also pain and itch responses in mice by interacting with the vanilloid (capsaicin)-binding pocket and promoting the stabilization of a closed state conformation...
October 10, 2016: Nature Communications
Jun Ren, Xiuqing Ding, John J Greer
Inhalation of capsaicin based sprays can cause central respiratory depression and lethal apneas. There are contradictory reports regarding the sites of capsaicin action. Further, an understanding of the neurochemical mechanisms underlying capsaicin-induced apneas and the development of pharmacological interventions are lacking. The main objectives were to perform a systematic study of the mechanisms of action of capsaicin-induced apneas and to provide insights relevant to pharmacological intervention. In vitro and in vivo rat and TRPV1-null mouse models were used to measure respiratory parameters and seizure-like activity in the presence of capsaicin and compounds that modulate glutamatergic neurotransmission...
October 6, 2016: American Journal of Respiratory Cell and Molecular Biology
Muhammad Laklouk, Ganesan Baranidharan
Capsaicin is a naturally occurring irritant active ingredient found in hot peppers. It is a ligand for transient receptor potential channel vanilloid receptors, which are found in nociceptive nerve terminals in the skin. Initial exposure to topical capsaicin leads to excitation of these receptors, release of vasoactive mediators, erythema, intense burning, pain, and thereafter desensitization of sensory neurons resulting in inhibition of pain transmission. Capsaicin 8% has been licensed for the treatment of postherpetic neuralgia pain in recent years...
2016: Patient Preference and Adherence
Masayuki Saito, Takeshi Yoneshiro, Mami Matsushita
Since the recent re-discovery of brown adipose tissue (BAT) in adult humans, this thermogenic tissue has attracted increasing interest. The inverse relationship between the BAT activity and body fatness suggests that BAT, because of its energy dissipating activity, is protective against body fat accumulation. Cold exposure activates and recruits BAT in association with increased energy expenditure and decreased body fatness. The stimulatory effects of cold are mediated through transient receptor potential channels (TRP), most of which are also chemesthetic receptors for various food ingredients...
August 2016: Best Practice & Research. Clinical Endocrinology & Metabolism
Esmaeal Tamaddonfard, Amir Erfanparast, Hamid Ghasemi, Farzin Henareh-Chareh, Mansoor Hadidi, Navideh Mirzakhani, Sahar Seyedin, Mina Taati, Reza Salighedar, Sara Salimi, Farshad Safaei
Histamine receptors are involved in supraspinal modulation of pain. In the present study, we investigated the effects of microinjection of histamine H1, H2 and H3 receptor antagonists and agonists into the ventral posteromedial (VPM) nucleus of the thalamus on two models of trigeminal pain. Right and left sides of VPM were implanted with two guide cannulas. Corneal pain was induced by local corneal surface application of hypertonic saline and the number of eye wipes was recorded. The duration of face rubbing, as an orofacial pain measure, was recorded after subcutaneous (s...
September 29, 2016: European Journal of Pharmacology
Kazuaki Yamagata, Mitsutaka Sugimura, Miki Yoshida, Shinichi Sekine, Akiyo Kawano, Aiko Oyamaguchi, Hiroharu Maegawa, Hitoshi Niwa
Several trigeminal pain disorders show sex differences, and high levels of estrogens may underlie these differences. The interaction between transient receptor potential vanilloid 1 (TRPV1) and anoctamin 1 (ANO1) plays an important role in peripheral nociception. However, whether TRPV1 and ANO1 are involved in estrogen-modulated trigeminal pain sensitivity is unclear. In this study, we examined 17β-estradiol (E2) modulation of nociception through behavioral and immunohistological experiments following application of capsaicin (Cap), a selective TRPV1 agonist, onto the ocular surface in ovariectomized rats treated with high- (HE) or low-dose E2 (LE) for 2 days...
September 30, 2016: Endocrinology
Carl M Hurt, Yao Lu, Creed M Stary, Honit Piplani, Bryce A Small, Travis J Urban, Nir Qvit, Garrett J Gross, Daria Mochly-Rosen, Eric R Gross
BACKGROUND: The transient receptor potential vanilloid 1 (TRPV1) mediates cellular responses to pain, heat, or noxious stimuli by calcium influx; however, the cellular localization and function of TRPV1 in the cardiomyocyte is largely unknown. We studied whether myocardial injury is regulated by TRPV1 and whether we could mitigate reperfusion injury by limiting the calcineurin interaction with TRPV1. METHODS AND RESULTS: In primary cardiomyocytes, confocal and electron microscopy demonstrates that TRPV1 is localized to the mitochondria...
2016: Journal of the American Heart Association
Chien-Cheng Liu, Yong-Jing Gao, Hao Luo, Temugin Berta, Zhen-Zhong Xu, Ru-Rong Ji, Ping-Heng Tan
It is well known that interferons (IFNs), such as type-I IFN (IFN-α) and type-II IFN (IFN-γ) are produced by immune cells to elicit antiviral effects. IFNs are also produced by glial cells in the CNS to regulate brain functions. As a proinflammatory cytokine, IFN-γ drives neuropathic pain by inducing microglial activation in the spinal cord. However, little is known about the role of IFN-α in regulating pain sensitivity and synaptic transmission. Strikingly, we found that IFN-α/β receptor (type-I IFN receptor) was expressed by primary afferent terminals in the superficial dorsal horn that co-expressed the neuropeptide CGRP...
September 27, 2016: Scientific Reports
Jessica Walker, Jakob P Ley, Johanna Schwerzler, Barbara Lieder, Leopoldo Beltran, Paul M Ziemba, Hanns Hatt, Joachim Hans, Sabine Widder, Gerhard E Krammer, Veronika Somoza
SCOPE: Inflammation-related diseases are a worldwide problem. The counteraction of inflammation with compounds activating the trigeminal nerve is one strategy to fight these diseases. Known trigeminally active compounds found in black or red pepper are the tingling t-pellitorine, the pungent capsaicin and the less pungent nonivamide. The presented study compares the anti-inflammatory potential of nonivamide to the two known anti-inflammatory compounds, elucidating the mechanism of action and the role of transient receptor protein channels...
September 26, 2016: Molecular Nutrition & Food Research
László Pecze, Walter Blum, Thomas Henzi, Beat Schwaller
Sensory neuron subpopulations as well as breast and prostate cancer cells express functional transient receptor potential vanilloid type 1 (TRPV1) ion channels; however little is known how TRPV1 activation leads to biological responses. Agonist-induced activation of TRPV1 resulted in specific spatiotemporal patterns of cytoplasmic Ca(2+) signals in breast and prostate cancer-derived cells. Capsaicin (CAPS; 50μM) evoked intracellular Ca(2+) oscillations and/or intercellular Ca(2+) waves in all cell lines. As evidenced in prostate cancer Du 145 cells, oscillations were largely dependent on the expression of functional TRPV1 channels in the plasma membrane, phospholipase C activation and on the presence of extracellular Ca(2+) ions...
September 20, 2016: Biochimica et Biophysica Acta
Yung-Jen Huang, Kuan H Lee, Lauren Murphy, Sandra M Garraway, James W Grau
Noxious input can sensitize pain (nociceptive) circuits within the spinal cord, inducing a lasting increase in spinal cord neural excitability (central sensitization) that is thought to contribute to chronic pain. The development of spinally-mediated central sensitization is regulated by descending fibers and GABAergic interneurons. The current study provides evidence that spinal cord injury (SCI) transforms how GABA affects nociceptive transmission within the spinal cord, recapitulating an earlier developmental state wherein GABA has an excitatory effect...
November 2016: Experimental Neurology
Willem J Laursen, Eve R Schneider, Dana K Merriman, Sviatoslav N Bagriantsev, Elena O Gracheva
The ability to sense heat is crucial for survival. Increased heat tolerance may prove beneficial by conferring the ability to inhabit otherwise prohibitive ecological niches. This phenomenon is widespread and is found in both large and small animals. For example, ground squirrels and camels can tolerate temperatures more than 40 °C better than many other mammalian species, yet a molecular mechanism subserving this ability is unclear. Transient receptor potential vanilloid 1 (TRPV1) is a polymodal ion channel involved in the detection of noxious thermal and chemical stimuli by primary afferents of the somatosensory system...
October 4, 2016: Proceedings of the National Academy of Sciences of the United States of America
Christine Gebhardt, Oliver von Bohlen Und Halbach, Michael D Hadler, Christian Harteneck, Doris Albrecht
Recently we have shown that capsaicin attenuates the strength of LTP in the lateral amygdala (LA) and demonstrated that this effect is mediated by the transient receptor potential (TRP) channel TRPV1. Here we further show that capsaicin, which is thought to act primarily through TRPV1, modifies long term depression (LTD) in the LA. Yet the application of various TRPV1 antagonists does not reverse this effect and it remains in TRPV1-deficient mice. In addition, voltage gated calcium channels, nitric oxide and CB1 receptors are not involved...
September 12, 2016: Neurobiology of Learning and Memory
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