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https://www.readbyqxmd.com/read/29352512/trpv1-antagonists-that-cause-hypothermia-instead-of-hyperthermia-in-rodents-compounds-pharmacological-profiles-in-vivo-targets-thermoeffectors-recruited-and-implications-for-drug-development
#1
Andras Garami, Eszter Pakai, Heath A McDonald, Regina M Reilly, Arthur Gomtsyan, Joshua J Corrigan, Erika Pinter, Dawn X D Zhu, Sonya G Lehto, Narender R Gavva, Philip R Kym, Andrej A Romanovsky
AIM: Thermoregulatory side effects hinder the development of transient receptor potential vanilloid-1 (TRPV1) antagonists as new painkillers. While many antagonists cause hyperthermia, a well-studied effect, some cause hypothermia. The mechanisms of this hypothermia are unknown and were studied herein. METHODS: Two hypothermia-inducing TRPV1 antagonists, the newly synthesized A-1165901 and the known AMG7905, were used in physiological experiments in rats and mice...
January 20, 2018: Acta Physiologica
https://www.readbyqxmd.com/read/29351423/role-of-trpv1-in-acupuncture-modulation-of-reflex-excitatory-cardiovascular-responses
#2
Zhi-Ling Guo, Liang-Wu Fu, Hou-Fen Su, Stephanie C Tjen-A-Looi, John C Longhurst
Acupuncture, including manual and electroacupuncture (MA and EA), at the P5-6 acupoints stimulates afferents in the median nerve (MN) to modulate sympathoexcitatory cardiovascular reflexes. Transient receptor potential vanilloid type-1 (TRPV1) is present in afferents distributed in the region of acupoints. However, contribution of TRPV1 to activation of sensory nerves by acupuncture, leading to modulation of pressor responses has not been studied. We hypothesized that TRPV1 participates in acupuncture's activation of sensory fibers and neurons to modulate pressor reflexes...
January 3, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/29343767/blockade-of-trpv1-inhibits-methamphetamine-induced-rewarding-effects
#3
Yu-Hua Tian, Shi-Xun Ma, Kwang-Wook Lee, Sunmee Wee, George F Koob, Seok-Yong Lee, Choon-Gon Jang
Methamphetamine (MAP) is the most widely used psychostimulant in the world, but the exact mechanisms underlying MAP addiction are not yet fully understood. Recent studies have identified the distribution of TRPV1 in several brain regions that are related to drug addiction, including nucleus accumbens (NAc) and dorsal striatum (DSt). In the present study, we performed conditioned place preference (CPP) and self-administration tests to examine the effects of capsazepine (CPZ) and SB366791 (SB) on MAP reward. We found that both CPZ and SB significantly inhibited MAP-induced CPP and self-administration; in contrast, TRPV1 knock-out (KO) mice did not develop MAP-induced CPP...
January 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29343055/genetically-encoded-circuit-for-remote-regulation-of-cell-migration-by-magnetic-fields
#4
Abdullah Al Mosabbir, Kevin Truong
Magneto-reception can be generally defined as the ability to transduce the effects of a magnetic field into a cellular response. Magnetic stimulation at the cellular level is particularly attractive due to its ability for deep penetration and minimal invasiveness, allowing remote regulation of engineered biological processes. Previously, a magnetic-responsive genetic circuit was engineered using the transient receptor potential vanilloid 1 (TRPV1) and the iron containing ferritin protein (i.e. the TF circuit)...
January 17, 2018: ACS Synthetic Biology
https://www.readbyqxmd.com/read/29342359/semiconducting-photothermal-nanoagonist-for-remote-controlled-specific-cancer-therapy
#5
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/29339762/supra-pharmacological-concentration-of-capsaicin-stimulates-brown-adipogenesis-through-induction-of-endoplasmic-reticulum-stress
#6
Ryosuke Kida, Taiki Noguchi, Masaru Murakami, Osamu Hashimoto, Teruo Kawada, Tohru Matsui, Masayuki Funaba
We previously showed that brown (pre)adipocytes express Trpv1, a capsaicin receptor, and that capsaicin stimulates differentiation of brown preadipocytes in the late stages of brown adipogenesis. The present study revealed that treatment with 100 μM capsaicin stimulates brown adipogenesis by inducing endoplasmic reticulum (ER) stress. Treatment with capsaicin (100 μM) during brown adipogenesis enhanced lipid accumulation and the expression of Ucp1, a gene selectively expressed in brown adipocytes. Capsaicin treatment also caused an increase in the cytosolic calcium concentration even when extracellular calcium was removed...
January 16, 2018: Scientific Reports
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
#7
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/29338036/static-magnetic-field-enhances-the-anticancer-efficacy-of-capsaicin-on-hepg2-cells-via-capsaicin-receptor-trpv1
#8
Wei-Ting Chen, Guan-Bo Lin, Shu-Hui Lin, Chueh-Hsuan Lu, Chih-Hsiung Hsieh, Bo-Lun Ma, Chih-Yu Chao
Static magnetic field (SMF) has shown some possibilities for cancer therapies. In particular, the combinational effect between SMF and anti-cancer drugs has drawn scientists' attentions in recent years. However, the underlying mechanism for the drug-specific synergistic effect is far from being understood. Besides, the drugs used are all conventional chemotherapy drugs, which may cause unpleasant side effects. In this study, our results demonstrate for the first time that SMF could enhance the anti-cancer effect of natural compound, capsaicin, on HepG2 cancer cells through the mitochondria-dependent apoptosis pathway...
2018: PloS One
https://www.readbyqxmd.com/read/29335450/copper-sulfide-nanoparticles-as-a-photothermal-switch-for-trpv1-signaling-to-attenuate-atherosclerosis
#9
Wen Gao, Yuhui Sun, Michelle Cai, Yujie Zhao, Wenhua Cao, Zhenhua Liu, Guanwei Cui, Bo Tang
Atherosclerosis is characterized by the accumulation of lipids within the arterial wall. Although activation of TRPV1 cation channels by capsaicin may reduce lipid storage and the formation of atherosclerotic lesions, a clinical use for capsaicin has been limited by its chronic toxicity. Here we show that coupling of copper sulfide (CuS) nanoparticles to antibodies targeting TRPV1 act as a photothermal switch for TRPV1 signaling in vascular smooth muscle cells (VSMCs) using near-infrared light. Upon irradiation, local increases of temperature open thermo-sensitive TRPV1 channels and cause Ca2+ influx...
January 15, 2018: Nature Communications
https://www.readbyqxmd.com/read/29335353/kchip3-n-terminal-31-50-fragment-mediates-its-association-with-trpv1-and-alleviates-inflammatory-hyperalgesia-in-rats
#10
Na-Xi Tian 田纳西, Yu Xu 徐煜, Jin-Yu Yang 杨瑾裕, Lu Li 李璐, Xiao-Hong Sun 孙晓红, Yun Wang 王韵, Ying Zhang 张瑛
Potassium channel interacting protein 3 (KChIP3), also termed downstream regulatory element antagonist modulator (DREAM) and calsenilin, is a multi-functional protein belonging to the neuronal calcium sensor (NCS) family. Recent studies revealed the expression of KChIP3 in dorsal root ganglion (DRG) neurons, suggesting the potential role of KChIP3 in peripheral sensory processing. Herein, we show that KChIP3 co-localizes with TRPV1, a critical molecule involved in peripheral sensitization during inflammatory pain...
January 15, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29334670/genetic-ablation-of-trpv1-exacerbates-pressure-overload-induced-cardiac-hypertrophy
#11
Beihua Zhong, Jack Rubinstein, Shuangtao Ma, Donna H Wang
Transient receptor potential vanilloid 1 (TRPV1) channels expressed in sensory nerves may regulate vascular tone and cardiovascular function via their anti-inflammatory effects by releasing neuropeptide calcitonin gene-related peptide (CGRP). Inflammation plays a role in the progression of cardiac hypertrophy and TRPV1 activation may be key to cardiac inflammatory processes. The aim of this study was to test the hypothesis that TRPV1 modulates inflammatory processes to protect the heart from pressure overload-induced hypertrophy and inflammatory responses...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29332300/long-term-exposure-to-cell-phone-frequencies-900-and-1800%C3%A2-mhz-induces-apoptosis-mitochondrial-oxidative-stress-and-trpv1-channel-activation-in-the-hippocampus-and-dorsal-root-ganglion-of-rats
#12
Kemal Ertilav, Fuat Uslusoy, Serdar Ataizi, Mustafa Nazıroğlu
Mobile phone providers use electromagnetic radiation (EMR) with frequencies ranging from 900 to 1800 MHz. The increasing use of mobile phones has been accompanied by several potentially pathological consequences, such as neurological diseases related to hippocampal (HIPPON) and dorsal root ganglion neuron (DRGN). The TRPV1 channel is activated different stimuli, including CapN, high temperature and oxidative stress. We investigated the contribution TRPV1 to mitochondrial oxidative stress and apoptosis in HIPPON and DRGN following long term exposure to 900 and 1800 MHz in a rat model...
January 13, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29323279/structural-basis-of-trpv5-channel-inhibition-by-econazole-revealed-by-cryo-em
#13
Taylor E T Hughes, David T Lodowski, Kevin W Huynh, Aysenur Yazici, John Del Rosario, Abhijeet Kapoor, Sandip Basak, Amrita Samanta, Xu Han, Sudha Chakrapani, Z Hong Zhou, Marta Filizola, Tibor Rohacs, Seungil Han, Vera Y Moiseenkova-Bell
The transient receptor potential vanilloid 5 (TRPV5) channel is a member of the transient receptor potential (TRP) channel family, which is highly selective for Ca2+, that is present primarily at the apical membrane of distal tubule epithelial cells in the kidney and plays a key role in Ca2+ reabsorption. Here we present the structure of the full-length rabbit TRPV5 channel as determined using cryo-EM in complex with its inhibitor econazole. This structure reveals that econazole resides in a hydrophobic pocket analogous to that occupied by phosphatidylinositides and vanilloids in TRPV1, thus suggesting conserved mechanisms for ligand recognition and lipid binding among TRPV channels...
January 2018: Nature Structural & Molecular Biology
https://www.readbyqxmd.com/read/29320695/decrypting-the-heat-activation-mechanism-of-trpv1-channel-by-molecular-dynamics-simulation
#14
Han Wen, Wenjun Zheng
As a prototype cellular sensor, the TRPV1 cation channel undergoes a closed-to-open gating transition in response to various physical and chemical stimuli including noxious heat. Despite recent progress, the molecular mechanism of heat activation of TRPV1 gating remains enigmatic. Toward decrypting the structural basis of TRPV1 heat activation, we performed extensive molecular dynamics simulations (with cumulative simulation time of ∼11 μs) for the wild-type channel and a constitutively active double mutant at different temperatures (30, 60, and 72°C), starting from a high-resolution closed-channel structure of TRPV1 solved by cryo-electron microscopy...
January 9, 2018: Biophysical Journal
https://www.readbyqxmd.com/read/29317663/trpv1-enhances-the-afferent-response-to-p2x-receptor-activation-in-the-mouse-urinary-bladder
#15
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/29317264/the-genetics-of-chronic-itch-gene-expression-in-the-skin-of-atopic-dermatitis-and-psoriasis-patients-with-severe-itch
#16
Leigh A Nattkemper, Hong Liang Tey, Rodrigo Valdes-Rodriguez, Helen Lee, Nicholas K Mollanazar, Christian Albornoz, Kristen M Sanders, Gil Yosipovitch
To identify itch-related mediators and receptors that are differentially expressed in pruritic skin, we used RNA sequencing to analyze the complete transcriptome in skin from paired itchy, lesional and non-itchy, non-lesional skin biopsies from 25 atopic dermatitis (AD) and 25 psoriasis patients and site-matched biopsies from 30 healthy controls. This analysis identified 18,000 differentially expressed genes common between itchy atopic and psoriatic skin compared to healthy skin. Of those, almost 2,000 genes were differentially expressed between itchy and non-itchy skin in atopic and psoriatic subjects...
January 6, 2018: Journal of Investigative Dermatology
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
#17
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/29306760/effect-of-acetaminophen-on-osteoblastic-differentiation-and-migration-of-mc3t3-e1-cells
#18
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/29305649/sensing-the-heat-with-trpm3
#19
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/29305012/regulation-of-gene-transcription-following-stimulation-of-transient-receptor-potential-trp-channels
#20
Gerald Thiel, Andrea Lesch, Sandra Rubil, Tobias M Backes, Oliver G Rössler
Transient receptor potential (TRP) channels belong to a heterogeneous superfamily of cation channels that are involved in the regulation of numerous biological functions, including regulation of Ca2+ and glucose homeostasis, tumorigenesis, temperature, and pain sensation. To understand the functions of TRP channels, their associated intracellular signaling pathways and molecular targets have to be identified on the cellular level. Stimulation of TRP channels frequently induces an influx of Ca2+ ions into the cells and the subsequent activation of protein kinases...
2018: International Review of Cell and Molecular Biology
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