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capsaicin receptor

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https://www.readbyqxmd.com/read/29328505/substance-p-as-a-putative-efferent-transmitter-mediates-gabaergic-inhibition-in-mouse-taste-buds
#1
Anthony Y Huang, Sandy Y Wu
BACKGROUND AND PURPOSE: Capsaicin-mediated modulation on taste nerve responses is thought to be produced indirectly by actions of neuropeptides, e.g., calcitonin gene-related peptide (CGRP) and substance P (SP), onto taste cells implying playing a role in taste sensitivity. During processing gustatory information in taste buds, CGRP shapes peripheral taste signals via serotonergic signaling. The underlying assumption has been that SP exerts its effects on taste transmitter secretion in taste buds of mice...
January 12, 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
#2
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/29317149/phenylquinoline-transient-receptor-potential-vanilloid-1-antagonists-for-the-treatment-of-pain-discovery-of-1-2-phenylquinoline-4-carbonyl-n-4-trifluoromethyl-phenyl-pyrrolidine-3-carboxamide
#3
Chen Liao, Yan Liu, Chunxia Liu, Jiaqi Zhou, Huilan Li, Nasi Wang, Jieming Li, Taiyu Liu, Hesham Ghaleb, Wenlong Huang, Hai Qian
Reported herein is the design, synthesis, and pharmacologic characterization of a class of TRPV1 antagonists constructed on a phenylquinoline platform that evolved from Cinchophen lead. This design composes three sections: a phenylquinoline headgroup attached to an aliphatic carboxamides, which is tethered at a phenyl tail group. Optimization of this design led to the identification of 37, comprising a pyrrolidine linker and a trifluoromethyl-phenyl tail. In the TRPV1 functional assay, using cells expressed hTRPV1, 37 antagonized capsaicin-induced Ca2+ influx, with an IC50 value of 10...
December 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29305649/sensing-the-heat-with-trpm3
#4
REVIEW
Joris Vriens, Thomas Voets
Heat sensation, the ability to detect warm and noxious temperatures, is an ancient and indispensable sensory process. Noxious temperatures can have detrimental effects on the physiology and integrity of cells, and therefore, the detection of environmental hot temperatures is absolutely crucial for survival. Temperature-sensitive ion channels, which conduct ions in a highly temperature-dependent manner, have been put forward as molecular thermometers expressed at the endings of sensory neurons. In particular, several temperature-sensitive members of the transient receptor potential (TRP) superfamily of ion channels have been identified, and a multitude of in vivo studies have shown that the capsaicin-sensitive TRPV1 channel plays a key role as a noxious heat sensor...
January 5, 2018: Pflügers Archiv: European Journal of Physiology
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/29288742/the-research-of-the-possible-mechanism-and-the-treatment-for-capsaicin-induced-cough
#6
Li Zhang, Tieying Sun, Longteng Liu, Lifang Wang
Unexplained chronic cough (UCC) affects millions of patients worldwide. New therapeutic approaches to this condition are urgently needed, since current treatment options provide only symptomatic relief. Cough reflex hypersensitivity has been shown to play an important role in the pathogenesis of UCC. The transient receptor potential vanilloid type 1 (TRPV1) is present on peripheral terminals of airway sensory nerves and modulation of its activity represents a potential target for the pharmacological treatment of UCC...
December 27, 2017: Pulmonary Pharmacology & Therapeutics
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/29280941/superoxide-anions-and-no-in-the-paraventricular-nucleus-modulate-the-cardiac-sympathetic-afferent-reflex-in-obese-rats
#8
Qing-Bo Lu, Jing Sun, Ying Kang, Hai-Jian Sun, Hui-Shan Wang, Yuan Wang, Guo-Qing Zhu, Ye-Bo Zhou
This study was conducted to explore the hypothesis that the endogenous superoxide anions (O₂-) and nitric oxide (NO) system of the paraventricular nucleus (PVN) regulates the cardiac sympathetic afferent reflex (CSAR) contributing to sympathoexcitation in obese rats induced by a high-fat diet (42% kcal as fat) for 12 weeks. CSAR was evaluated by monitoring the changes of renal sympathetic nerve activity (RSNA) and the mean arterial pressure (MAP) responses to the epicardial application of capsaicin (CAP) in anaesthetized rats...
December 27, 2017: International Journal of Molecular Sciences
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/29259542/capsaicin-enhances-glutamatergic-synaptic-transmission-to-neonatal-rat-hypoglossal-motor-neurons-via-a-trpv1-independent-mechanism
#10
Prajwal P Thakre, Mark C Bellingham
We investigated whether capsaicin modulated synaptic transmission to hypoglossal motor neurons (HMNs) by acting on transient receptor potential vanilloid type 1 (TRPV1) receptors. Using whole-cell patch clamp recording from neonatal rat HMNs, we found that capsaicin increased spontaneous excitatory post-synaptic current (sEPSC) frequency and amplitude. Interestingly, the only effect of capsaicin on spontaneous inhibitory post-synaptic currents (sIPSCs) was a significant decrease in sIPSC amplitude without altering frequency, indicating a post-synaptic mechanism of action...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29258175/capsaicin-friend-or-foe-in-skin-cancer-and-other-related-malignancies
#11
REVIEW
Simona-Roxana Georgescu, Maria-Isabela Sârbu, Clara Matei, Mihaela Adriana Ilie, Constantin Caruntu, Carolina Constantin, Monica Neagu, Mircea Tampa
Capsaicin is the main pungent in chili peppers, one of the most commonly used spices in the world; its analgesic and anti-inflammatory properties have been proven in various cultures for centuries. It is a lipophilic substance belonging to the class of vanilloids and an agonist of the transient receptor potential vanilloid 1 receptor. Taking into consideration the complex neuro-immune impact of capsaicin and the potential link between inflammation and carcinogenesis, the effect of capsaicin on muco-cutaneous cancer has aroused a growing interest...
December 16, 2017: Nutrients
https://www.readbyqxmd.com/read/29247491/the-roles-of-trpv1-trpa1-and-trpm8-channels-in-chemical-and-thermal-sensitivity-of-the-mouse-oral-mucosa
#12
Tatjana I Kichko, Winfried Neuhuber, Gerd Kobal, Peter W Reeh
Spices in food and beverages and compounds in tobacco smoke interact with sensory irritant receptors of the transient receptor potential (TRP) cation channel family. TRPV1 (vanilloid type 1), TRPA1 (ankyrin 1) and TRPM8 (melastatin 8) not only elicit action potential signaling through trigeminal nerves, eventually evoking pungent or cooling sensations, but by their calcium conductance they also stimulate the release of calcitonin gene-related peptide (CGRP). This is measured as an index of neuronal activation to elucidate the chemo- and thermosensory transduction in the isolated mouse buccal mucosa of wildtypes and pertinent knockouts...
December 15, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29246976/glutamate-receptor-glua1-subunit-is-implicated-in-capsaicin-induced-modulation-of-amygdala-ltp-but-not-ltd
#13
Christine Gebhardt, Doris Albrecht
Capsaicin has been shown to modulate synaptic plasticity in various brain regions including the amygdala. Whereas in the lateral amygdala the modulatory effect of capsaicin on long-term potentiation (LA-LTP) is mediated by TRPV1 channels, we have recently shown that capsaicin-induced enhancement of long term depression (LA-LTD) is mediated by TRPM1 receptors. However, the underlying mechanism by which capsaicin modulates synaptic plasticity is poorly understood. In the present study, we investigate the modulatory effect of capsaicin on synaptic plasticity in mice lacking the AMPAR subunit GluA1...
January 2018: Learning & Memory
https://www.readbyqxmd.com/read/29239974/additive-and-subadditive-antiallodynic-interactions-between-%C3%AE-opioid-agonists-and-n-methyl-d-aspartate-antagonists-in-male-rhesus-monkeys
#14
Jeremy C Cornelissen, Floyd F Steele, Kenner C Rice, Katherine L Nicholson, Matthew L Banks
μ-Opioid agonists are clinically effective analgesics, but also produce undesirable effects such as sedation and abuse potential that limit their clinical utility. Glutamatergic systems also modulate nociception and N-methyl D-aspartate (NMDA) receptor antagonists have been proposed as one useful adjunct to enhance the therapeutic effects and/or attenuate the undesirable effects of μ-opioid agonists. Whether NMDA antagonists enhance the antiallodynic effects of μ-agonists in preclinical models of thermal hypersensitivity (i...
December 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29238714/corneal-nerve-fiber-structure-its-role-in-corneal-function-and-its-changes-in-corneal-diseases
#15
REVIEW
Hiroshi Eguchi, Akio Hiura, Hiroshi Nakagawa, Shunji Kusaka, Yoshikazu Shimomura
Recently, in vivo confocal microscopy is used to examine the human corneal nerve fibers morphology. Corneal nerve fiber architecture and its role are studied in healthy and pathological conditions. Corneal nerves of rats were studied by nonspecific acetylcholinesterase (NsAchE) staining. NsAchE-positive subepithelial (stromal) nerve fiber has been found to be insensitive to capsaicin. Besides, NsAchE-negative but capsaicin-sensitive subbasal nerve (leash) fibers formed thick mesh-like structure showing close interconnections and exhibit both isolectin B4- and transient receptor potential vanilloid channel 1- (TRPV1-) positive...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29238213/first-evidence-of-the-conversion-of-paracetamol-to-am404-in-human-cerebrospinal-fluid
#16
Chhaya V Sharma, Jamie H Long, Seema Shah, Junia Rahman, David Perrett, Samir S Ayoub, Vivek Mehta
Paracetamol is arguably the most commonly used analgesic and antipyretic drug worldwide, however its mechanism of action is still not fully established. It has been shown to exert effects through multiple pathways, some actions suggested to be mediated via N-arachidonoylphenolamine (AM404). AM404, formed through conjugation of paracetamol-derived p-aminophenol with arachidonic acid in the brain, is an activator of the capsaicin receptor, TRPV1, and inhibits the reuptake of the endocannabinoid, anandamide, into postsynaptic neurons, as well as inhibiting synthesis of PGE2 by COX-2...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29234417/a-molecular-basis-for-the-inhibition-of-transient-receptor-potential-vanilloid-type-1-by-gomisin-a
#17
Sung Bae Lee, Shinhwa Noh, Hye Duck Yeom, Heejin Jo, Sanung Eom, Yoon Suh Kim, Sangsoo Nam, Hyunsu Bae, Jun-Ho Lee
Transient receptor potential (TRP) channel has critical actions as conditional sensors in primary afferent neurons. We studied the regulatory action of gomisin A on TRPV1 channel current in this report. Schisandra chinensis contains bioactive compounds such as the gomisin derivatives and their related compounds. Coapplication with gomisin A inhibited the capsaicin-mediated inward peak current. This inhibitory effect of gomisin A on capsaicin-induced inward current showed concentration-dependence and was reversible...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29229209/randomized-double-blind-placebo-controlled-dose-escalation-study-investigation-of-the-safety-pharmacokinetics-and-antihyperalgesic-activity-of-l-4-chlorokynurenine-in-healthy-volunteers
#18
Mark Wallace, Alexander White, Kathy A Grako, Randal Lane, Allen Jo Cato, H Ralph Snodgrass
BACKGROUND AND AIMS: Neuropathic pain is a significant medical problem needing more effective treatments with fewer side effects. Overactive glutamatergic transmission via N-methyl-d-aspartate receptors (NMDARs) are known to play a role in central sensitization and neuropathic pain. Although ketamine, a NMDAR channel-blocking antagonist, is often used for neuropathic pain, its side-effect profile and abusive potential has prompted the search for a safer effective oral analgesic. A novel oral prodrug, AV-101 (l-4 chlorokynurenine), which, in the brain, is converted into one of the most potent and selective GlyB site antagonists of the NMDAR, has been demonstrated to be active in animal models of neuropathic pain...
October 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29214107/diet-and-rosacea-the-role-of-dietary-change-in-the-management-of-rosacea
#19
REVIEW
Emma Weiss, Rajani Katta
Dietary change may play a role in the therapy of rosacea. Certain foods and beverages may act as "triggers" for rosacea exacerbations. These may be divided into heat-related, alcohol-related, capsaicin-related, and cinnamaldehyde-related. One potential pathogenic mechanism may be via the activation of transient receptor potential cation channels, which result in neurogenic vasodilatation. Further research is needed on the role of the gut skin connection in rosacea. Epidemiologic studies suggest that patients with rosacea have a higher prevalence of gastrointestinal disease, and one study reported improvement in rosacea following successful treatment of small intestinal bacterial overgrowth...
October 2017: Dermatology Practical & Conceptual
https://www.readbyqxmd.com/read/29209454/kimchi-attenuates-fatty-streak-formation-in-the-aorta-of-low-density-lipoprotein-receptor-knockout-mice-via-inhibition-of-endoplasmic-reticulum-stress-and-apoptosis
#20
Minji Woo, Mijeong Kim, Jeong Sook Noh, Chan Hum Park, Yeong Ok Song
BACKGROUND/OBJECTIVES: Endoplasmic reticulum (ER) stress is positively associated with atherosclerosis via elevating macrophage cell death and plaque formation, in which oxidative stress plays a pivotal role. Antioxidative, lipid-lowering, and anti-atherogenic effects of kimchi, a Korean fermented vegetable, have been established, wherein capsaicin, ascorbic acid, quercetin, 3-(4'-hydroxyl-3',5'-dimethoxyphenyl)propionic acid, and lactic acids were identified. In this study, mechanisms of action of kimchi methanol extracts (KME) on fatty streak formation via suppression of ER stress and apoptosis in aorta were examined in low-density lipoprotein receptor knockout mice...
December 2017: Nutrition Research and Practice
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